penicillin,polypeptide and others drug
TRANSCRIPT
ANTIBIOTICS
A PRESENTATION OF PENICILLIN POLYPEPTIDE AND OTHER ANTIBIOTICS
DEFINITION OF ANTIBIOTIC
A substance of biological semisynthetic or synthetic origin of low molecular weight produced by a fungus or bacterium as secondary metabolites that inhibits or stop growth of other microorganisms in vitro and in vivo selectively when it used in low concentration
CLASSIFICATION1 PENICILLINS2 CEPHALOSPORINS AND OTHER BETA-LACTAMS3 TETRACYCLINES4 AMINOGLYCOSIDES5 MACROLIDES6 CLINDAMYCIN7 SOME OTHER ANTIBACTERIALS 8 SULPHONAMIDES AND TRIMETHOPRIM9 ANTITUBERCULOSIS DRUGS10 ANTILEPROTIC DRUGS 11 METRONIDAZOLE AND TINIDAZOLE12 QUINOLONES13 URINARY-TRACT INFECTIONS
Β- LACTAMS CELL WALL INHIBITORS
PENICILLIN TIMELINEbull 1928- ALEXANDER FLEMING DISCOVERED THE PENICILLIN MOLDbull 1929- FLEMING PUBLISHED HIS FINDINGSbull 1939- DOCTORS HOWARD FLOREY AND NORMAN HEATLEY BEGAN
INTENSIVE RESEARCH ON PENICILLIN AND ITS ANTIBACTERIAL PROPERTIES
bull 1940- FLOREY CONVERTED PENICILLIN INTO A DRY STABLE BROWN POWDER
bull JULY 91941- FLOREY AND HEATLEY CAME TO THE US WITH A SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIR RESEARCH AT PEORIA LABS IN ILLINOIS
bull NOVEMBER 26 1941- ANDREW J MOYER SUCCEEDED IN INCREASING THE YIELD OF PENICILLIN TEN TIMES
bull 1943- PENICILLIN WAS TESTED AND PROVEN TO BE THE MOST EFFECTIVE ANTIBACTERIAL AGENT TO DATE
bull 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC FOR 55 CENTS A SHOT
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DEFINITION OF ANTIBIOTIC
A substance of biological semisynthetic or synthetic origin of low molecular weight produced by a fungus or bacterium as secondary metabolites that inhibits or stop growth of other microorganisms in vitro and in vivo selectively when it used in low concentration
CLASSIFICATION1 PENICILLINS2 CEPHALOSPORINS AND OTHER BETA-LACTAMS3 TETRACYCLINES4 AMINOGLYCOSIDES5 MACROLIDES6 CLINDAMYCIN7 SOME OTHER ANTIBACTERIALS 8 SULPHONAMIDES AND TRIMETHOPRIM9 ANTITUBERCULOSIS DRUGS10 ANTILEPROTIC DRUGS 11 METRONIDAZOLE AND TINIDAZOLE12 QUINOLONES13 URINARY-TRACT INFECTIONS
Β- LACTAMS CELL WALL INHIBITORS
PENICILLIN TIMELINEbull 1928- ALEXANDER FLEMING DISCOVERED THE PENICILLIN MOLDbull 1929- FLEMING PUBLISHED HIS FINDINGSbull 1939- DOCTORS HOWARD FLOREY AND NORMAN HEATLEY BEGAN
INTENSIVE RESEARCH ON PENICILLIN AND ITS ANTIBACTERIAL PROPERTIES
bull 1940- FLOREY CONVERTED PENICILLIN INTO A DRY STABLE BROWN POWDER
bull JULY 91941- FLOREY AND HEATLEY CAME TO THE US WITH A SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIR RESEARCH AT PEORIA LABS IN ILLINOIS
bull NOVEMBER 26 1941- ANDREW J MOYER SUCCEEDED IN INCREASING THE YIELD OF PENICILLIN TEN TIMES
bull 1943- PENICILLIN WAS TESTED AND PROVEN TO BE THE MOST EFFECTIVE ANTIBACTERIAL AGENT TO DATE
bull 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC FOR 55 CENTS A SHOT
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CLASSIFICATION1 PENICILLINS2 CEPHALOSPORINS AND OTHER BETA-LACTAMS3 TETRACYCLINES4 AMINOGLYCOSIDES5 MACROLIDES6 CLINDAMYCIN7 SOME OTHER ANTIBACTERIALS 8 SULPHONAMIDES AND TRIMETHOPRIM9 ANTITUBERCULOSIS DRUGS10 ANTILEPROTIC DRUGS 11 METRONIDAZOLE AND TINIDAZOLE12 QUINOLONES13 URINARY-TRACT INFECTIONS
Β- LACTAMS CELL WALL INHIBITORS
PENICILLIN TIMELINEbull 1928- ALEXANDER FLEMING DISCOVERED THE PENICILLIN MOLDbull 1929- FLEMING PUBLISHED HIS FINDINGSbull 1939- DOCTORS HOWARD FLOREY AND NORMAN HEATLEY BEGAN
INTENSIVE RESEARCH ON PENICILLIN AND ITS ANTIBACTERIAL PROPERTIES
bull 1940- FLOREY CONVERTED PENICILLIN INTO A DRY STABLE BROWN POWDER
bull JULY 91941- FLOREY AND HEATLEY CAME TO THE US WITH A SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIR RESEARCH AT PEORIA LABS IN ILLINOIS
bull NOVEMBER 26 1941- ANDREW J MOYER SUCCEEDED IN INCREASING THE YIELD OF PENICILLIN TEN TIMES
bull 1943- PENICILLIN WAS TESTED AND PROVEN TO BE THE MOST EFFECTIVE ANTIBACTERIAL AGENT TO DATE
bull 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC FOR 55 CENTS A SHOT
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Β- LACTAMS CELL WALL INHIBITORS
PENICILLIN TIMELINEbull 1928- ALEXANDER FLEMING DISCOVERED THE PENICILLIN MOLDbull 1929- FLEMING PUBLISHED HIS FINDINGSbull 1939- DOCTORS HOWARD FLOREY AND NORMAN HEATLEY BEGAN
INTENSIVE RESEARCH ON PENICILLIN AND ITS ANTIBACTERIAL PROPERTIES
bull 1940- FLOREY CONVERTED PENICILLIN INTO A DRY STABLE BROWN POWDER
bull JULY 91941- FLOREY AND HEATLEY CAME TO THE US WITH A SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIR RESEARCH AT PEORIA LABS IN ILLINOIS
bull NOVEMBER 26 1941- ANDREW J MOYER SUCCEEDED IN INCREASING THE YIELD OF PENICILLIN TEN TIMES
bull 1943- PENICILLIN WAS TESTED AND PROVEN TO BE THE MOST EFFECTIVE ANTIBACTERIAL AGENT TO DATE
bull 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC FOR 55 CENTS A SHOT
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PENICILLIN TIMELINEbull 1928- ALEXANDER FLEMING DISCOVERED THE PENICILLIN MOLDbull 1929- FLEMING PUBLISHED HIS FINDINGSbull 1939- DOCTORS HOWARD FLOREY AND NORMAN HEATLEY BEGAN
INTENSIVE RESEARCH ON PENICILLIN AND ITS ANTIBACTERIAL PROPERTIES
bull 1940- FLOREY CONVERTED PENICILLIN INTO A DRY STABLE BROWN POWDER
bull JULY 91941- FLOREY AND HEATLEY CAME TO THE US WITH A SMALL SAMPLE OF PENICILLIN TO CONTINUE THEIR RESEARCH AT PEORIA LABS IN ILLINOIS
bull NOVEMBER 26 1941- ANDREW J MOYER SUCCEEDED IN INCREASING THE YIELD OF PENICILLIN TEN TIMES
bull 1943- PENICILLIN WAS TESTED AND PROVEN TO BE THE MOST EFFECTIVE ANTIBACTERIAL AGENT TO DATE
bull 1946- PENICILLIN BECAME AVAILABLE TO THE GENERAL PUBLIC FOR 55 CENTS A SHOT
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PENICILLIN
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PENICILLINSbull THE PENICILLINS ARE AMONG THE MOST WIDELY EFFECTIVE
ANTIBIOTICS AND ALSO THE LEAST TOXIC DRUGS KNOWN BUT INCREASED RESISTANCE HAS LIMITED THEIR USE
bull MEMBERS OF THIS FAMILY DIFFER FROM ONE ANOTHER IN THE R SUBSTITUENT ATTACHED TO THE 6-AMINOPENICILLANIC ACID RESIDUE
bull THE NATURE OF THIS SIDE CHAIN AFFECTS THE ANTIMICROBIAL SPECTRUM STABILITY TO STOMACH ACID AND SUSCEPTIBILITY TO BACTERIAL DEGRADATIVE ENZYMES (Β-LACTAMASES)
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
THE SPORES IN PENICILLIUM OFTEN CONTAIN BLUE OR GREEN PIGMENTS WHICH GIVE THE COLONIES ON FOODS AND FEEDS THEIR CHARACTERISTIC COLOUR
IT IS THE SPORES IN THE BLUE CHEESE THAT GIVE THE COLOUR TO THE CHEESE
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PENICILLIUM
THE NAME PENICILLIUM COMES FROM PENICILLUS = BRUSH AND THIS IS BASED ON THE BRUSH-LIKE APPEARANCE OF THE FRUITING STRUCTURES
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Β-LACTAM RINGbullThe β-lactam ring is a common structure for
bullPenicillinsbullCephalosporinsbullMonobactamsbullCarbapenems
bull Bacteria will target this ring to gain resistance
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION 1
bullSome PBP have transpeptidase activitybull Transpeptidase activity is essential in cell wall synthesis
bullBeta-lactams bind PBP (Penicillin Binding Proteins)
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION OF THE PENICILLINS bull PEPTIDOGLYCAN IS A HETEROPOLYMER THAT PROVIDES RIGID MECHANICAL STABILITY TO THE BACTERIAL CELL
WALL BY VIRTUE OF ITS HIGHLY CROSS-LINKED STRUCTURE IN GRAM-POSITIVE BACTERIA THE CELL WALL IS 50ndash100 MOLECULES THICK IT IS ONLY 1 OR 2 MOLECULES THICK IN GRAM-NEGATIVE BACTERIA
bull THE PEPTIDOGLYCAN IS COMPOSED OF GLYCAN CHAINS WHICH ARE LINEAR STRANDS OF TWO ALTERNATING AMINO SUGARS (N-ACETYLGLUCOSAMINE AND N-ACETYLMURAMIC ACID) CROSS-LINKED BY PEPTIDE CHAINS
bull PEPTIDOGLYCAN PRECURSOR FORMATION TAKES PLACE IN THE CYTOPLASM THE SYNTHESIS OF UDPndashACETYLMURAMYL-PENTAPEPTIDE IS COMPLETED WITH THE ADDITION OF THE DIPEPTIDE D-ALA-D-ALA (FORMED BY RACEMIZATION AND CONDENSATION OF L-ALA) UDP-ACETYLMURAMYL-PENTAPEPTIDE AND UDPACETYLGLUCOSAMINE ARE LINKED TO FORM A LONG POLYMER
bull THE CROSS-LINK IS COMPLETED BY A TRANSPEPTIDATION REACTION THAT OCCURS OUTSIDE THE CELL MEMBRANE THE B-LACTAM ANTIBIOTICS INHIBIT THIS LAST STEP IN PEPTIDOGLYCAN SYNTHESIS PRESUMABLY BY ACYLATING THE TRANSPEPTIDASE VIA CLEAVAGE OF THEmdashCOmdashNmdashBOND OF THE B-LACTAM RING
bull ALTHOUGH INHIBITION OF THE TRANSPEPTIDASE IS DEMONSTRABLY IMPORTANT THERE ARE ADDITIONAL TARGETS FOR THE ACTIONS OF PENICILLINS AND CEPHALOSPORINS THESE COLLECTIVELY ARE TERMED PENICILLINBINDING PROTEINS (PBPS) THE TRANSPEPTIDASE RESPONSIBLE FOR PEPTIDOGLYCAN SYNTHESIS IS ONE OF THESE PBPS OTHER PBPS ARE NECESSARY FOR CELL DIVISION AND CELL SHAPE AND OTHER ESSENTIAL PROCESSES THUS THE LETHALITY OF PENICILLIN FOR BACTERIA INVOLVES BOTH LYTIC AND NONLYTIC MECHANISMS
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
bull Penicillins inhibit a bacterial enzyme called the transpeptidase Penicillins inhibit a bacterial enzyme called the transpeptidase enzyme which is involved in the synthesis of the bacterial cell enzyme which is involved in the synthesis of the bacterial cell wallwall
bull The The -lactam ring is involved in the mechanism of inhibition-lactam ring is involved in the mechanism of inhibitionbull Penicillin becomes covalently linked to the enzymersquos active site Penicillin becomes covalently linked to the enzymersquos active site
leading to irreversible inhibitionleading to irreversible inhibition
Covalent bond formed Covalent bond formed to transpeptidase enzymeto transpeptidase enzymeIrreversible inhibitionIrreversible inhibition
N
S Me
Me
HN
H H
CO2HO
CO
R
Nu
Enz
CHN
C
CO2H
HH
Me
MeS
HN
O
RO
Nu-Enz-H N
S Me
Me
HN
H H
CO2HO
C
H
Enz-Nu
O
R
Mechanism of actionMechanism of action
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
bull Penicillin inhibits final crosslinking stage of cell wall Penicillin inhibits final crosslinking stage of cell wall synthesissynthesis
bull It reacts with the transpeptidase enzyme to form an It reacts with the transpeptidase enzyme to form an irreversible covalent bondirreversible covalent bond
bull Inhibition of transpeptidase leads to a weakened cell wall Inhibition of transpeptidase leads to a weakened cell wall bull Cells swell due to water entering the cell then burst (lysis)Cells swell due to water entering the cell then burst (lysis)bull Penicillin acts as an analogue of the D-Ala-D-Ala portion of Penicillin acts as an analogue of the D-Ala-D-Ala portion of
the pentapeptide chain the pentapeptide chain
Mechanism of action - bacterial cell wall synthesisMechanism of action - bacterial cell wall synthesis
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM POS(contrsquod)
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTIONCELL WALL SYNTHESIS INHIBITORS
RESISTANCE TO Β-LACTAMS ndash GRAM NEG
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DRUGS OF PENICILLIN
bull AMOXICILLIN bull AMPICILLINbull DICLOXACILLINbull METHICILLINbull NAFCILLIN bull FLUCLOXACILLINbull PENICILLIN Vbull PENICILLIN Gbull TICARCILLIN
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
LATEST INFORMATION OF PENICILLIN DRUG
bull METHICILLINbull NAFCILLIN
METHICILLIN IT IS NOT USED IN USA NOWADAYS CLINICALLY BECAUSE IT IS PRODUCE SEVERE INTERSTITIAL NEPRITIS
NAFCILLIN IS USED BUT IT ADVERSE EFFECT IS ALSO NEPRITIES
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
AMOXICILLININDICATION
1 UTI 3 SINUSITIS 2 OTITIS MEDIA 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 RASHES 2 NAUSEA 3 VOMITING 4 DIARRHOEA
5 ANTIBIOTIC ASSOCIATED COLITISDOSE
BY MOUTH ADULT 250 MG EVERY 8 HOURS( DOUBLE IN SEVERE INFECTION) FOR CHILD UP TO 10 YEARS 125 MG EVERY 8 HOURSBRAND NAME
MOXACIL (SQUARE) MOXIN (OPSONIN) TYCIL ( BEXIMCO)
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
AMPICILLININDICATION 1 UTI 3 LISTERIAL MENINGITIS 2 HAEMOPHILUS INFLUENZAE INFECTION 4 ENDOCARDITIS PROPHYLAXIS
CONTRAINDICATION 1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENTSIDE EFFECT 1 RAEARLY RASHES (DISCONTINUE TREATMENT) 2 NAUSEA 3 VOMITING 4 DIARRHOEA 5 ANTIBIOTIC ASSOCIATED COLITIS
DOSE ADULT BY MOUTH 025 ndash 1G EVERY 6 HOURS( AT LEAST 30 MIN BEFORE FOOD) CHILD UNDER 10 YEAR HALF OF ADULTBRAND NAME AMPEXIN (OPSONIN) PEN-A (RENETA)
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DICLOXACILLININDICATION
1 IT IS EFFECTIVE AGAINST STEPHYLO COCEAL INFECTION WHICH IS RESISTNAT TO BENZYLPENICILLIN
CONTRAINDICATION
1PENICILLIN HYPERSENSITIVITY 2 PORPHYRIA 3 RENAL IMPAIREMENT
SIDE EFFECT
1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA
DOSE FOR ADULT 125 TO 250 MG EVERY 6 HOURS
FOR CHILDREN 125 TO 25 MGKG DAILY INDIVIDED DOSES
BRAND NAME DICLOX ( NOVARTIS)
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
FLUCLOXACILLININDICATION 1BETA-LACTAMASE-PRODUCING STAPHYLOCOCCI INFECTIONS INCLUDING OTITIS EXTERNA 2 ADJUNCT IN PNEUMONIA 3 IMPETIGO 4 OSTEOMYELITIS
SIDE EFFECT 1 URTICARIA 2 FEVER 3 JOINT PAIN 4 RASHES 5 NEUTROPENIA 6 NEPRITIS 7 DIARRHEA 8 CHOLESTATIC JAUNDICE REPORTED
CONTRAINDICATION
PENICILLIN HYPERSENSITIVITY
DOSE BY MOUTH 250-500 MG EVERY 6 HOURS( 30 MIN BEFORE FOOD) CHILD UNDER 2 YEARS QUARTER OF ADULT DOSE 2-10 YEARS HALF OF ADULT DOSE BRAND NAME FLUBEX ( BEXIMCO) FLUCLOXIN (SK-F) FLUX (OPSONIN)
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PENICILLIN G OR BENZYL PENICLLIN
BENZYLPNICILLIN COMMONLY KNOWN AS PENICILLIN G IS THE GOLD STANDARD TYPE OF PENICILLIN lsquoGrsquo IN THE NAME lsquoPENICILLIN Grsquo REFERS TO lsquoGOLD STANDARDrsquo PENICILLIN G IS TYPICALLY GIVEN BY A PARENTERAL ROUTE OF ADMINISTRATION ( NOT ORALLY) BECAUSE IT IS UNSTABLE IN THE HCL OF THE STOMACHBECAUSE THE DRUG IS GIVEN PARENTERALLY HIGHER TISSUE CONCENTRATIONS OF PENICILLIN G CAN BE ACHIEVED THAN IS POSSIBLE WITH PHENOXYMETHYLPENICILLINTHESE HIGHER CONCENTRATIONS TRANSLATE TO INCREASED ANTIBACTERIAL ACTIVITY
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Properties of Penicillin GProperties of Penicillin G
bull Active vs Gram +ve bacilli and some Gram -ve cocciActive vs Gram +ve bacilli and some Gram -ve coccibull Non toxicNon toxicbull Limited range of activityLimited range of activitybull Not orally active - must be injectedNot orally active - must be injectedbull Sensitive to Sensitive to -lactamases -lactamases
(enzymes which hydrolyse the (enzymes which hydrolyse the -lactam ring)-lactam ring)bull Some patients are allergic Some patients are allergic bull Inactive vs Inactive vs StaphylococciStaphylococci
Drug DevelopmentDrug Development AimsAimsbull To increase chemical stability for oral administrationTo increase chemical stability for oral administrationbull To increase resistance to To increase resistance to -lactamases-lactamasesbull To increase the range of activityTo increase the range of activity
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Problems with Penicillin GProblems with Penicillin G
bull It is sensitive to stomach acids It is sensitive to stomach acids bull It is sensitive to It is sensitive to -lactamases - -lactamases -
enzymes which hydrolyse the enzymes which hydrolyse the --lactam ringlactam ring
bull it has a limited range of activityit has a limited range of activity
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION OF PENICILLIN G
bull CELLULITISbull INFECTIVE ENDOCARDITISbull GONORRHEAbull MENINGITISbull ASPIRATION PNEUMONIALUNG ABSCESSbull SYPHILISbull SEPTIC ARTHRITISbull GANGRENE
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION PENICILLIN SENSITIVITY
ADVERSE EFFECT URTICARIAJOINT PAINS RASHESANAPHYLAXISLEUCOPENIACOAGULATION DISORDERS
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
ADULT OVER 18 YEARSFOR- IM OR SLOW IV 12GDAY IN 4 DIVIDED OR 50 MG KG BODY WEIGHTBRAND NAME PEN-G (OPSONIN) PENICILLIN G SODIUM ( RENATA)
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PHENOXYMETHYL PENICILLIN OR PENICILLIN V
PHENOXYMETHYLPENICILLIN COMMONLY KNOWN AS PENICILLIN IS A PENICILLIN ANTIBIOTIC THAT IS ORALLY ACTIVE PHENOXYMETHYLPENICILLIN HAS A RANGE OF ANTIMICROBIAL ACTIVITY AGAINST GRAM-POSITIVE BACTERIA THAT IS SIMILAR TO THAT OF BEZYLPENICILLIN AND AND A SIMILAR MODE OF ACTION BUT IT IS SUBSTANTIALLY LESS ACTIVE THAN BENZYLPENICILLIN AGAINST GRAM-NEGATIVE BACTERIA
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION
TONSILLITISPHARYNGITISSKIN INGECTIONSANTHRAXLYME DISEASE SPLEEN DISORDERSRHEUMATIC FEVER
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION HYPERSENSITIVITY TO THE DRUG
ADVERSE EFFECT NAUSEAVOMITINGEPIGASTRIC DISTRESSDIARRHEABLACK HAIRY TONGUE
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
ADULT 500MG6HRCHILD UP TO 1 YEARS 6256HRS AND 1-5 YEARS 125MG6HRS
BRAND NAME CRYSTAPEN-V (GSK) PENVIK ( SQUARE)
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
1 METHICILLIN - SENSETIVE TO MOISTURE --- LOSS frac12 OF ITS ACTIVITY AFTER 5 DAYS AT
RT - SOLUTION FOR PARENTAL AD MAY KEPT FOR 24 HR ----- [ AT 5OC ]
2 NAFCILLIN OXACILLIN PARENTRAL SOL STABLE FOR 3 DAYS AT RT ( 96 HR IF REF )
3 DICLOXCILLIN PARENTRAL SOL STABLE FOR 7 DAYS AT RT ( 14 DAY IF REF )
4 CLOXACILLIN PARENTRAL SOL STABLE FOR 14 DAYS ( REF )
5- FLUCLOXACILLIN PARENTRAL SOL STABLE FOR 7 DAYS ( REF )
STORAGE
STORE BETWEEN 15 ndash 30OC
Stability
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
POLYPEPTIDE
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
1THEY INHIBITS ISOPRENYL PYROPHOSPHATEA MOLECULE THAT CARRIES THEE BUILDING BLOCKS OF THE PEPTIDOGLYCAN BACTERIAL CELL WALL OUTSIDE OF THE INNER MEMBRANE2THEY ALSO INTERACT WITH GRAM NEGATIVE BACTERIAL OUTER MEMBRANE AND CYTOPLASMIC MEMBRANE IT DISPLACES BACTERIAL COUNTER IONS WHICH DESTABILIZES OUTER MEMBRANETHEY ACT LIKE A DETERGENT AGAINST THE CYTOPLASMIC MEMBRANEWHICH ALTERS ITS PERMEABILITY POLYMYXIN B AND E ARE BACTERICIDAL EVEN IN AN ISO-OSMOTIC SOLUTION
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DRUGS OF POLYPEPTIDES
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BACITRACIN INDICATION
EYEEAROR BLADDER INFECTION EFFECTIVE FOR LOCAL TREATMENT OF STAPHYLOCOCCAL BLEPHEROCONJUNCTIVITIS
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ADVERSE EFFECT
bull KIDNEY AND NERVE DAMAGE ( WHEN GIVEN BY INJECTION)
bull IT HAS THE PROPENSITY TO INDUCE ALLERGY
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAME
bull NEOBAC (OPSONIN)bull NEBANOL (SQUARE)bull NEOCITIRIN (ACI)
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
POLYMYXINS
bull SURFACE ACTIVE AMPHIPATHIC AGENTS
bull INTERACT STRONGLY WITH PHOSPHOLIPIDS AND DISRUPT THE STRUCTURE OF CELL MEMBRANES
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
POLYMYXIN B
INDICATION
BACTERICIDAL EFFECTIVE PARTICULARLY AGAINST GRAM NEGATIVE ORGANISMS INCLUDING PSEUDOMONAS (PROTEUS IS RESISTANT) IT CANrsquoT PENETRATE IN TO THE EYE
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
bull EYE DROPS INSTILLATION VARIES ACCORDING TO THE
SEVERITY OF INFECTON IT VARIES FROM EVERY MIN TO 2-3 TIMES A DAY
EYE OINTMENT APPLY EITHER AT NIGHT ( IF EYE DROPS
USED DURING THE DAYTIME) OR 3-4 TIMES DAILY ( IF EYE OINTMENT USED ALONE)
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAME
bull NEOSPORIN (GSK)bull RENAMYCIN (RENATA)
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
OTHERS ANTIBIOTIC
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
FUSIDIC ACID
FUSIDIC ACID IS A BACTERIOSTATIC ANTIBIOTIC THAT IS OFTEN USED TOPICALLY IN CREAMS AND EYE-DROPS BUT MAY ALSO BE GIVEN SYSTEMICALLY AS TABLETS OR INJECTIONS THE GLOBAL PROBLEM OF ADVANCING ANTIMICROBIAL RESISTANCE HAS LED TO A RENEWED INTEREST IN ITS USE RECENTLY
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATIONrsquoSbull CERTAIN SKIN DISEASES IT WORKS BY STOPPING THE GROWTH OF CERTAIN
BACTERIA AND REDUCING REDNESS ITCHING CRUSTING AND SWELLING OF THE SKIN SORES
bull BACTERIAL EYE INFECTIONS (CONJUNCTIVITIS)bull THE SUSPENSION OF FUSIDIC ACID FIGHTS INFECTIONS OF THE SKIN WOUNDS
BLOOD (SEPTICAEMIA) BONE HEART TISSUE AND LUNGS (PNEUMONIA) THE SUSPENSION CAN BE INJECTED IF THE DRUG CANNOT BE SWALLOWED
MECHANISM OF ACTION FUSIDIC ACID ACTS AS A BACTERIAL PROTEIN SYNTHESIS INHIBITOR BY
PREVENTING THE TURNOVER OF ELONGATION FACTOR G (EF-G) FROM THE RIBOSOME FUSIDIC ACID IS EFFECTIVE PRIMARILY ON GRAM-POSITIVE BACTERIA SUCH AS STAPHYLOCOCCUS SPECIES STREPTOCOCCUS SPECIES ANDCORYNEBACTERIUM SPECIES FUSIDIC ACID INHIBITS BACTERIAL REPLICATION AND DOES NOT KILL THE BACTERIA AND IS THEREFORE TERMED BACTERIOSTATIC
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION bull WHO IS ALLERGIC TO FUSIDIC ACID AND ITS SALTS OR TO ANY OF THE
INGREDIENTS OF THIS MEDICATION
ADVERSE EFFECTFUSIDIC ACID EYE DROPSbull STINGING OR BURNING FOR A SHORT TIME AFTER USE amp ALLERGIC REACTION
(HYPERSENSITIVITY)
FUSIDIC ACID CREAMbull RASHbull STINGING AND IRRITATIONbull ITCHY RASH AND INFLAMMATIONbull FUSIDIC ACID SUSPENSIONSTOMACH UPSETS
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
bull ADULTSmdash500 MG THREE TIMES DAILYbull CHILDRENmdashUP TO 1 YEAR OF AGE TO 12 YEARS 20
MILLIGRAMSKILOGRAM DAILY DIVIDED INTO 3 EQUAL DOSES INFUSED OVER AT LEAST 2 HOURS
BRAND NAMESFusidic plus Beximco
Facid HC Eskayef
Fusiderm InceptaFusidate H Aristopharma
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
METRONIDAZOLE
bull METRONIDAZOLE IS A NITROIMIDAZOLE ANTIBIOTIC MEDICATION USED PARTICULARLY FOR ANAEROBIC BACTERIA AND PROTOZOA METRONIDAZOLE IS AN ANTIBACTERIAL AGAINST ANAEROBIC ORGANISMS AMOEBICIDE ANDANTIPROTOZOAL IT IS THE DRUG OF CHOICE FOR FIRST EPISODES OF MILD-TO-MODERATE CLOSTRIDIUM DIFFICILE INFECTION
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATIONrsquoS ANAEROBIC INFECTION ACUTE ULCERATIVE GINGIVITIS amp ACUTE DENTAL INFACTION SKIN TREATMENT INVASIVE INTESTINAL AMOEBIASIS UROGENITAL TRICHOMONIASISbull GIANDAISIESbull ANEROBIC INFECTIONS ndash BACTERICIDES CLOSTRIDIUM
bull FUSOBACTERIUM PEPTOCOCCUS PEPTOSIRGSTOCOCCUS
bull EUBACTERIUM H PYLORIS
bull POLYMICROBIAL INFECTIONS
bull PROPHYLAXIS OF POSTOP MIXED BACTERIAL INFECTION
bull PSEUDOMEMBRANOUS COLITIS
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
bull MECHANISM OF ACTION bull ENTERS BACTERIA VIA CELL DIFFUSIONbull ACTIVATED VIA SINGLE REDUCTION STEP BY BACTERIA
FORMS RADICALS REACTS WITH NUCLEIC ACID CELL DEATH
bull SPECTRUM OF ACTIVITYbull ANAEROBIC BACTERIAbull MICROAEROPHILIC BACTERIAbull PROTOZOA
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATIONbull HEPATIC IMPAIRMENTbull HEPATIC ENCEPHALOPATHYbull PREGNANCY AND BREAST FEEDINGbull DISULFIRAM LIKE REACTION MAY OCCUR IF METRONIDAZOLE IS TAKEN
WITH ALCOHOL
ADVERSE EFFECTSbull GI N V EPIGASTRIC DISTRESSbull METALLIC TASTEbull DARKENING OF URINEbull PERIPHERAL NEUROPATHYbull PANCREATITISbull HEPATITISbull FEVERbull REVERSIBLE NEUTROPENIA
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSEIN ANAEROBIC INFECTION-BY MOUTH 800 MG INITIALLY THEN
400 MG 8 HOURLY FOR 7 DAYSCHILD ANY ROUTE-75 MG PER KG IN EVERY 8 HOURSACUTE ULCERATIVE GINGIVITIS 200 MG 8 HOUR FOR 3 DAY
BY MOUTHCHILD100-150 MG PER 8 HOUR FOR 3 DAYSACUTE DENTAL INFECTION 200 MG 8 HOUR FOR 3-7 DAY BY
MOUTH
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAMESAmodis SquareAmotrex ACIDirozyl AcmeFilmet-DS BeximcoFlagyl AventisMetco EskayefMetryl OpsoninNidazyl Orion
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CHLORAMPHENICOL
bull CHLORAMPHENICOL IS AN ANTIBIOTIC PRODUCED BY STREPTOMYCES VENEZUELAE AND OTHER SOIL BACTERIA THAT WAS FIRST DISCOVERED IN 1947 AND IS NOW EXCLUSIVELY
INDICATIONENTERIC FEVER(আনতরিক জবর যাহাSALMONELLA TYPHI দবারা সষটি হয় )BACTERIAL MENINGITIS CAUSED BY HAEMOPHILUS INFLUENZAE(মনতরিষক নতরিনতরি
পরদাহ) IN MOST ANAEROBIC INFECTIONS RESPOND TO CHLORAMPHENICOLSUCH
AS RICKETTSIAL DISEASE(নতরিরকেকটনতরিয়া উদভত ররাগ) AND BRUCELLOSIS(এটি একটি রো ায়াকেকেরাগ যা সহকেampই গবানতরিদপশ র+কেক বনযপশ এমননতরিক মানকের মাকেও সংকরনতরিমত হয়)
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
bull CHLORAMPHENICOL INHIBITS PROTEIN SYNTHESIS IN BACTERIA AND TO A LESSER EXTENT IN EUKARYOTIC CELLS THE DRUG READILY PENETRATES BACTERIAL CELLS PROBABLY BY FACILITATED DIFFUSION
bull CHLORAMPHENICOL ACTS PRIMARILY BY BINDING REVERSIBLY TO THE 50 S RIBOSOMAL SUBUNIT ALTHOUGH BINDING OF TRNA AT THE CODON RECOGNITION SITE ON THE 30 S RIBOSOMAL SUBUNIT IS THUS UNDISTURBED THE DRUG APPEARS TO PREVENT THE BINDING OF THE AMINO-ACID-CONTAINING END OF THE AMINOACYL TRNA TO THE ACCEPTOR SITE ON THE 50 S RIBOSOMAL SUBUNIT THE INTERACTION BETWEEN PEPTIDYLTRANSFERASE AND ITS AMINO ACID SUBSTRATE CANNOT OCCUR AND PEPTIDE BOND FORMATION IS INHIBITED
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
LETrsquoS SEE
PHARMACOKINETICS
RAPIDLY amp COMPLETELY ABSORBED FROM GIT30 PROTEIN BOUNDMETABOLIZED BY LIVER ndash GLUCURONIDATIONWELL DISTRIBUTED INCLUDING CNS AND CSFEXCRETED IN URINE
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATIONS
PREVIOUS ALLERGIC REACTION TO CHLORAMPHENICOLTRIVIAL INFECTIONS(সামানয সঙকরমণ)PREGNANCYHISTORY OF PORPHYRIA(একটি বংানকরনতরিমক যকত সমবনধীয়
রগালকেযাগ)HISTORY OF BONE MARROW SUPRESSION
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ADVERSE EFFECTS
PANCYTOPENIA (DEFICIENCY OF ALL THREE CELLULAR COMPONENTS OF THE BLOOD (RED CELLS WHITE CELLS AND PLATELETS)
SUPER INFECTIONGREY BABY SYNDROMEGASTROINTESTINAL UPSETS
DOSEBY MOUTH OR BY IV 50MGKG DAILY IN FOUR DIVIDED DOSESINFANT UNDER 2 WEEK 25MGKG DAILY IN FOUR DIVIDED DOSES
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAMESOpsomycetin Opsonin
Chlorphen Nipa
Chloromycin Pharmaco
A phenicol ACME
Aristophen Aristopharma
SqMycetic Square
Chloram Ibn sina
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
RIFAXIMINE
bull RIFAXIMINE IS A SEMISYNTHETIC ANTIBIOTIC BASED ON RIFAMYCIN IT HAS POOR ORAL BIOAVAILABILITY MEANING THAT VERY LITTLE OF THE DRUG WILL BE ABSORBED INTO THE BLOOD STREAM WHEN IT IS TAKEN ORALLY RIFAXIMIN IS USED IN THE TREATMENT OF TRAVELERS DIARRHEA ANDHEPATIC ENCEPHALOPATHY FOR WHICH IT RECEIVED ORPHAN DRUG STATUS FROM THE US FOOD AND DRUG ADMINISTRATION IN 1998
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATIONrsquoS
bull TRAVELERS DIARRHEA CAUSED BY E COLI
MECHANISM OF ACTION RIFAXIMIN INTERFERES WITH TRANSCRIPTION BY BINDING TO THE Β-SUBUNIT OF BACTERIAL RNA POLYMERASE THIS RESULTS IN THE BLOCKAGE OF THE TRANSLOCATION STEP THAT NORMALLY FOLLOWS THE FORMATION OF THE FIRST PHOSPHODIESTER BOND WHICH OCCURS IN THE TRANSCRIPTION PROCESS
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION
bull SEVERE LIVER DISEASE bull CLOSTRIDIUM DIFFICILE BACTERIA RELATED COLITISbull HYPERSENSITIVITY
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ADVERSE EFFECT
bull NAUSEAbull STOMACH PAINbull DIZZINESSbull EXCESSIVE TIREDNESSbull HEADACHEbull MUSCLE TIGHTENINGbull JOINT PAIN
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
FOR TRAVELERS DIARRHEA 200 MG TABLET TAKEN ORALLY THREE TIMES A DAY FOR 3 DAYS
FOR HEPATIC ENCEPHALOPATHY 550 MG TABLET TAKEN ORALLY TWO TIMES A
DAYBRAND NAMES
Hepaximin Aristopharma
Rifamax Incepta
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
TINIDAZOLE
bull TINIDAZOLE IS AN ANTI-PARASITIC DRUG USED AGAINST PROTOZOAN INFECTIONS IT IS WIDELY KNOWN THROUGHOUT EUROPE AND THE DEVELOPING WORLD AS A TREATMENT FOR A VARIETY OF AMOEBIC AND PARASITIC INFECTIONS IT WAS DEVELOPED IN 1972
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATIONS
bull INFECTIONS FROM AMOEBAE GIARDIA AND TRICHOMONAS
bull TINIDAZOLE MAY BE A THERAPEUTIC ALTERNATIVE IN THE SETTING OF METRONIDAZOLE TOLERANCE
bull TINIDAZOLE MAY ALSO BE USED TO TREAT A VARIETY OF OTHER BACTERIAL INFECTIONS(EG AS PART OF COMBINATION THERAPY FOR HELICOBACTER PYLORI ERADICATION PROTOCOLS)
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
bull TINIDAZOLE IS A PRODRUG THAT IS CONVERTED TO CYTOTOXIC FORMS IN VIVO IT HAS A LOW MOLECULAR WEIGHT AND PENETRATES THE CELL MEMBRANE OF BOTH AEROBIC AND ANAEROBIC MICROORGANISMS AFTER DIFFUSING INTO THE CELLS OF SUSCEPTIBLE ORGANISMS TINIDAZOLE IS REDUCED AT ITS NITRO GROUP TO SHORT LIVED TOXIC RADICALS BY A FERRIDOXIN-MEDIATED TRANSPORT SYSTEM IT IS THOUGHT THAT THESE TOXIC INTERMEDIATES BIND TO DNA RESULTING IN DNA DAMAGE WHICH ULTIMATELY LEADS TO CELL DEATH
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION
EPILEPTIC SEIZURE NUMBNESS TINGLING OR PAIN OF HANDS OR FEET A MOTHER WHO IS PRODUCING MILK AND BREASTFEEDING DECREASED NEUTROPHILS A TYPE OF WHITE BLOOD CELL HYPERSENSITIVITY
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ADVERSE EFFECT
bull METALIC TASTEbull NAUSEAbull ANOREXIAbull DYSPEPSIAbull VOMITINGbull WEAKNESSbull DIZINESSbull HEADACHE
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
ANAEROBIC INFECTION 2G INITIALLY BY MOUTH FOLLOWED BY 1G DAILY OR 500MG TWICE A DAY FOR 5 DAYS
ACUTE ULCERATIVE GINGIVITIS A SINGLE 2G DOSE BY MOUTH
BRAND NAMEProtogyn Renata
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ANTI-TUBERCULER AGENTS
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MYCOBACTERIUM TUBERCULOSIS
bull SLENDERbull ROD-SHAPEDbull ACID-FAST(CANNOT BE EASILY
DECOLORIZED BY TREATMENT WITH ACIDIFIED ORGANIC SOLVENTS)
bull CAUSE LEPROSY AS WELL AS SEVERAL TUBERCULOSIS-LIKE HUMAN INFECTIONS
bull INFECTIONS ARE INTRACELLULAR bull SLOW-GROWING GRANULOMATOUS
LESIONS THAT ARE RESPONSIBLE FOR MAJOR TISSUE DESTRUCTION
MYCOBACTERIA ARE INTRINSICALLY RESISTANT TO MOST ANTIBIOTICS
THE LIPID-RICH MYCOBACTERIAL CELL WALL IS IMPERMEABLE TO MANY AGENTS
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
TRANSMISSIONbull PULMONARY TUBERCULOSIS IS A
DISEASE OF RESPIRATORY TRANSMISSION PATIENTS WITH THE ACTIVE DISEASE (BACILLI) EXPEL THEM INTO THE AIR BY
ndash COUGHING ndash SNEEZING ndash SHOUTINGndash OR ANY OTHER WAY THAT WILL
EXPEL BACILLI INTO THE AIR
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
STRATEGIES FOR ADDRESSING DRUG RESISTANCE
bull MULTIDRUG THERAPYbull BECAUSESTRAINS OF M TUBERCULOSIS THAT
ARE RESISTANT TO A PARTICULAR AGENT EMERGE DURING TREATMENT WITH A SINGLE DRUG
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
NEWER SECOND LINE DRUGS
FLOUROQUINOLONES ARE ACTIVE AGAINST MTUBERCULOSIS CIPROFLAXACIN OFLAXACIN
NEWER MACROLIDES AND SOME RIFAMPIN CONGENERS ARE THE RECENT ADDITIONS CLARITHROMYCIN AZITHROMYCIN RIFABUTIN
HIGH EFFICACY
LOW TOXICITY
LOW EFFICAC
Y
HIGH TOXICITY
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ISONIAZID (INH)Isoniazid [eye-soe-NYE-a-zid]
the hydrazide of isonicotinic acid is a synthetic analog of
pyridoxine
but is never given as a single agent in the treatment of
active tuberculosis
It is the most potent of the antitubercular drugs
Isoniazid is a prodrug
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTIONbull ISONIAZID INHIBITS SYNTHESIS OF MYCOLIC
ACIDS WHICH ARE ESSENTIAL COMPONENTS OF MYCOBACTERIAL CELL WALLS
bull INH IS A PRODRUG THAT IS ACTIVATED BY KATG THE MYCOBACTERIAL CATALASE-PEROXIDASE
bull THE ACTIVATED FORM OF ISONIAZID FORMS A COVALENT COMPLEX WITH ACYL CARRIER PROTEIN (ACPM) BETA-KETOACYL CARRIER PROTEIN SYNTHETASE (KASA)
bull THIS COMPLEX BLOCKS MYCOLIC ACID SYNTHESIS AND KILLS THE CELL
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION TUBERCULOSIS (IN COMBINATION WITH OTHER DRUGS)CAUTION 1 HEPATIC IMPAIRMENT 2 RENAL IMPAIRMENT 3 EPILEPSY 4 BREAST-FEEDING
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
SIDE EFFECT
bull NAUSEAbull VOMITINGbull PURPURAbull HYPERGLYCAEMIAbull OPTIC NEURITIS
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
DOSE
BY MOUTH ADULT AND CHILD 15MGKG 3 TIMES A WEEK
BRAND NAME ISONIAZID (OPSONIN) SERVIZID ( NOVARTIS)
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
2RIFAMPIN[R]
bull SEMISYNTH DERI OF RIFAMYCIN B-FROM STMEDITARRANEI
bull ACTS BOTH EXTRA ampINTRACELLULARLYbull GOOD STERILISING PROPERTY amp RESISTANCE PREVENTING ACTIONbull BACTERICIDAL EFFICACY asymp INH ampgtANY OTHER 1ST
LINE DRUGbull ANALOGUE OF RIFAMPIN IS RIFABUTIN OBTAINED FROM RIFAMYCIN S
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTIONDNA RIFAMPIN (THE DRUG IS SPECIFIC FOR PROKARYOTES) DNA DEPENDENT RNAPOLYMERASE RNA PROTEIN SYN CELL MULTIPLICATION RIFAMPIN BIND TO Β SU OF DDRP DRUG ndashENZ COMPLEX SUPRESSION OF CHAIN INITIATION
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION
bull TUBERCULOSISbull LEPROSYbull PROPHYLAXIS OF MENINGOCOCCAL MENINGITIS AND H
INFLUENZA INFECTION
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CAUTION
bull HEPATIC IMPAIRMENTbull RENAL IMPAIRMENTbull PREGNANCYbull BREAST-FEEDING
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION
bull HEPATIC FAILUREbull JAUNDICESIDE EFFECTGIT SYMPTOMS INFLUENZA LIKE SYMPTOMSSHORTNESS OF BREATHHAEMOLYTIC ANEMIA
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
bull SYNTHETIC ANALOGUE OF NICOTINAMIDEbull HIGHLY EFFECTIVE DURING 1ST 2MONTHSbull ACTIVE BOTH INTRA amp EXTRACELLULARLYbull THOUGH WEAKLY TUBERCULOCIDAL MORE ACTIVE IN ACIDIC MEDIUM
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTIONPyrazinamide
Mycobacterial Pyrazinamidase Pyrazinoic Acid
Inhibits Mycolic Acid Synthesis
Resistance due to mutation of gene pncA
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION TUBERCULOSIS IN COMBINATION WITH OTHER DRUGCAUTIONHEPATIC IMPAIRMENTRENAL IMPAIRMENTDIABETES MELLITUSGOUT (THE DRUG SHOULD BE AVOIDED IN ACUTE ATTACK)
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATIONbull LIVER IMPAIRMENTbull PORPHYRIASIDE EFFECTbull IMPAIRED LIVER FUNCTIONSbull GI-TRACT UPSETbull ARTHRALGIA
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAME
bull PYZIMIDE (JAMS)bull PZA-CIBA (NOVARTIS)
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
4ETHAMBUTOL[E]
bull TUBERCULOSTATIC ACTIVE AGAINST MTB
MINTRACELLULARAE
bull RAPID GROWERS ARE MORE SUSCEPTIBLEbull HASTENS THE RATE OF SPUTUM CONVERSIONbull PREVENT THE EMERGENCE OF RESISTANT BACILLI
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION
MYCOBACT ARABINOSYL TRANSFERASE
ETHAMBUTOL
POLYMERISATION REACTION OF ARABINOGLYCAN
ESSENTIAL COMPONENT OF MYCOCELLWALL
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PHARMACOKINETICSPK ProfileDRUG INH RMP ETB PZA
ROUTE ORAL ORAL ORAL ORAL
ABSORBTION GUT GUT GUT GIT
DISTRIBUTION BODY FLUID AND CSF
WIDELY BODY FLUID AND CSF BODY TISSUE INFLAMMED MENINGES
METABOLISM ACETYLATION IN LIVER
DEACETYLATIONIN LIVER
LIVER LIVER
EXCRETION URINE(75-95) BILEFAECESURINE
URINE(50)FAECES
URINE
PROTEIN BINDING Very low (0 to 10)
High to very high (89)
Low (10 to 20) Low (20 to 30)
PEAK PLASMA CONCENTRATION
7 to 9 (mcgmL)
3 to 7 mcgmL 19 mcgmL 2 to 5 mcgmL
bull Isoniazid undergoes N-acetylation and hydrolysis bullresulting in inactive products bullA bimodal distribution of fast and slow acetylators existsbullIt is genetically regulated
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
INDICATION
TUBERCULOSIS IN COMBINATION WITH OTHER DRUG
CAUTIONbullRENAL IMPAIRMENTbullVISUAL ACUITY
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATION
bull OPTIC NEURITISbull POOR VISION SIDE EFFECTbull OPTIC NEURITISbull RED OR GREEN COLOR BLINDNESSbull URTICARIAbull THROMBOCYTOPENIA
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
BRAND NAME
bull FIAMBUTOL (FISONS)bull SURAL (AMBEE)
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ANTI-LEPROTIC DRUG
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Leprosy Leprosy is a skin disease characterized by sores and boils caused by Mycobacterium laprae It was discovered in United States but 70 of all causes are located in India
Antileprotic drug Drugs which is used in the treatment of Mycobacterium lapper are called antileprotic drug The following drugs are used in the treatment of leprosy -
Daps one and other sulfones Rifampicin (Rifampin) Clofazimine Amithiozone
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Treatment of leprosy a) Multi-bacillary form -
- Daps one - 100 mgday - Rimfapicin - 600once monthly - Colafazimine ndash 50mgday amp extra 300 mg
monthly
Duration of treatment 2 years minimum
b) For paucibacillary form of leprosy - - Daps one ndash 100 mgday - Rifampicin ndash 600 mg once monthly
Why we use the combination of drug Most effectiveDrug resistance grow incase of single drug Lower the duration of treatment Reduce the risk of adverse reactionPrevent relafs
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Dapsone Dapsone(diaminodiphenylsulfone) is most widely used in the long-term treatment of leprosy
It inhibits folate synthesis
Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Pharmacokinetics
bull Route of administration Oral
bull Absorption 70-90
bull Protein binding 70-80
bull Metabolism Hepatic (mostly CYP2E1 mediated)
bull Half life 20-30 hours
bull Excretion Renal
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Mechanism of action
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Contraindication Patient with allergy Pregnant women
Adverse effects Haemolytic anaemia Sulfhaemoglobinaemia GIT intolarance Nausea Vomiting Diarrhoea Fever Pruritus Rash Headache Nervousness Insomnia Blurring of vision Pariparal neuropathy
Dose Adult 100 mg daily
Child Proportionality less depending on weight
Brand Name Lepsone (Gaco)
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Rifampicin Broad spectrum antibiotics
Bacteriocidal
Kills both extracellur and intracellular mycobacterium Powerful enzyme inducer
ChemistryoRifampicin is a naturally made non-peptide antibiotic
oIt is a derivitive of rifamycin
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Pharmacokinetics
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
MECHANISM OF ACTION OF RIFAMPICIN
IT INHIBITS BACTERIAL RNA SYNTHESIS BY INHIBITING THE ENZYME DNA DEPENDENT RNA POLYMERASE
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
CONTRAINDICATIONbullChronic liver diseasebullOld age bullAlchoholismbullVasculitis
Adverse effects of RifampicinHepatotoxicity
Cholestatic jaundice Hepatitis
Hypersensitivity Rash Fever Nephritis Flu like syndrome
GIT upset Naucea Vomiting Diarrhoea Abdominal cramps
Others Thrombocytpenia Ataxia prurities Urticaria renal insufficiency
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Drug interactionInteraction Possible cause
+ Rifampicin Oral ( )anticoagulents warferin
Decrease effectiveness ofwarfarin
Rifampicin is a potent hepatic enzyme inducer
increases metabolism ofwarferin
+ Rifampicin OCP Decrease effectiveness of
OCP
Rifampicin increases metabolism of estrogen of
OCP+ Rifampicin Steroid
digoxin PropanplolMorphine
Decreased biavailability of these drugs
Rifampicin is a potent hepatic enzyme inducer
increases metabolism of these drugs
DoseParentral 600mg powder for IV injection
Oral 150 300 mg Capsule
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
ClofaziminebullIs an antileprosy agentbullAvailable as soft gelatin capsulebullBacteriostatic and mieldly bactereocidal effect an mycobacterium
ChemistryClofazimine is a phenazine dye with the following formula
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Pharmacokinetics
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Mechanism of action of clofazimine
Clofazimine acts in two mechanisms-1)
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
2)
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
Adverse effectEosinophiolic enteritis GI irritationDiscoloration of the skinDepressionBowel obstruction
ContraindicationDiarrhoeaPeptic ulcerVomitingsteatorrhoea
Dose100 mg daily
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
THANK YOU
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-
PREPARED BYP-121003P-121007P-121015P-121018P-121024P-121038P-121051
- Antibiotics
- Definition of Antibiotic
- PowerPoint Presentation
- Slide 4
- Classification
- β- lactams cell wall inhibitors
- Penicillin Timeline
- Penicillin
- Penicillins
- The spores in Penicillium often contain blue or green pigments which give the colonies on foods and feeds their characteristic colour It is the spores in the blue cheese that give the colour to the cheese
- Penicillium
- β-lactam ring
- Slide 13
- Slide 14
- Mechanism of action
- Slide 16
- Mechanism of action 1
- MECHANISM OF ACTION OF THE PENICILLINS
- Slide 19
- Slide 20
- Slide 21
- Mechanism of Action CELL WALL SYNTHESIS INHIBITORS
- Slide 23
- Drugs of Penicillin
- Latest information of Penicillin Drug
- Amoxicillin
- Ampicillin
- Dicloxacillin
- Flucloxacillin
- Penicillin G or Benzyl penicllin
- Slide 31
- Slide 32
- Indication of Penicillin G
- Contraindication
- Dose
- Phenoxymethyl Penicillin or Penicillin V
- Indication
- Slide 38
- Slide 39
- Slide 40
- Slide 41
- Mechanism of Action
- Slide 43
- Bacitracin
- Adverse Effect
- Slide 46
- Brand Name
- POLYMYXINS
- Polymyxin B
- Slide 50
- Slide 51
- Slide 52
- Fusidic acid
- Indicationrsquos
- Slide 55
- Dose
- Metronidazole
- INDICATIONrsquoS
- Slide 59
- Slide 60
- CONTRAINDICATION
- Slide 62
- BRAND NAMES
- CHLORAMPHENICOL
- Mechanism of action
- Slide 66
- Letrsquos see
- Contraindications
- Adverse effects
- Brand names
- Rifaximine
- Slide 72
- Slide 73
- Adverse effect
- Slide 75
- TINIDAZOLE
- Indications
- Slide 78
- Slide 79
- Slide 80
- Slide 81
- DOSE
- Anti-tuberculer Agents
- Slide 84
- Mycobacterium tuberculosis
- Transmission
- Slide 87
- Strategies for addressing drug resistance
- NEWER SECOND LINE DRUGS Flouroquinolones are active against Mtuberculosis Ciproflaxacin Oflaxacin Newer macrolides and some rifampin congeners are the recent additions Clarithromycin Azithromycin Rifabutin
- Slide 90
- ISONIAZID (INH)
- Slide 92
- Slide 93
- Slide 94
- Side effect
- Slide 96
- 2RIFAMPIN[R]
- Slide 98
- Slide 99
- Caution
- Slide 101
- 3PYRAZINAMIDE[z]
- Slide 103
- Slide 104
- Slide 105
- Slide 106
- 4ETHAMBUTOL[E]
- Slide 108
- Slide 109
- Pharmacokinetics
- Slide 111
- Slide 112
- Slide 113
- Slide 114
- Slide 115
- Slide 116
- Slide 117
- Slide 118
- Slide 119
- Slide 120
- Slide 121
- Slide 122
- Slide 123
- Contraindication
- Slide 125
- Slide 126
- Slide 127
- Slide 128
- Slide 129
- Slide 130
- Slide 131
- Prepared By
-