penicillin piont view
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PenicillinBy : abdelmnaem elgelia
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Classification:
Cell wall synthesis inhibitorsBeta-lactams (penicillins, cephalosporins,
aztreonam, imipenem)Poly-peptides (bacitracin, vancomycin) Protein synthesis inhibitorsAminoglycosidesTetracyclinsMacrolidesChloramphenicol
Clindamycin Folate antagonistsSulfonamidesTrimethoprim Quinolones
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BACTERIAL CELL WALL
Gram-negative (e.g. E.coli, Salmonella)Few peptidoglycan
layers(Lipopolysaccheride)
Gram-positive (e.g. Staphylococci,Listeria)
Many peptidoglycan layers(Lipoteichoicacid)
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Resistance to PenicillinsResistance to Penicillins
1)Production of -lactamases
2)
3)The occurrence of modified penicillin-
binding sites4)
5)Decreased permeability to the drug
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Narrow spectrum penicillinase sensitive
Narrow spectrum penicillinase resistant
Broad spectrum penicillins
Extended-spectrum penicillins
PenicillinsPenicillins
classificationclassification
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Narrow spectrum penicillinase (=Narrow spectrum penicillinase (= --
lactamase) sensitivelactamase) sensitive
Benzylpenicillin
Naturally occuring
Poor oral availability (sensitive to stomach
acid)
given by injection
Active against gram-positive bacteria
Phenoxymethylpenicillin
Better oral availability (acid resistant)
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Narrow spectrum penicillinase (=Narrow spectrum penicillinase (=
-- lactamase) resistantlactamase) resistant
Methicillin
Semisynthetic
Poor oral availability (only parenteral)
Active against gram-pos bacteria
Mostly used for Staphylococcus aureus
Oxacillin
Good oral availability
Cloxacillin
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Broad spectrum penicillinase (=Broad spectrum penicillinase (= --
lactamase) sensitive(= Aminopenicillins)lactamase) sensitive(= Aminopenicillins)
Ampicillin
Semisynthetic
Good oral availability
Active against gram-pos and gram-neg
bacteria
Active against enterobacteria
Amoxicillin
Excellent oral availability
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Extended spectrum penicillinase (= -Extended spectrum penicillinase (= -
lactamase) sensitivelactamase) sensitive (=(=
Carboxypenicillins)Carboxypenicillins) Carbenicillin
Semisynthetic
Poor oral availability Active against gram-pos and gram-neg bacteria
Active against Pseudomonas aeruginosa,
Klebsiella
Ticarcillin
Mezlocillin
Pipercillin
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PHARMACOKINETIC:
bsorbtion orallyDistrubutionBBBPlacentaenal execretion
etabolizetion
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Therapeutic useTherapeutic use
Treatment of:Treatment of:+r a m o c c i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ S t a p h, >>>>t r e p t o a b c e s sr a m _ o c c i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ n i s s e r i a>>>> e n i n g i t i s+r a m a c i l l i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ a n t h r a x, ,e t a n u s g a s g a n g r e n e>>>>p i r o c h e t e s s y p h i l i s>>>>c t i n o m y c e s e a c t i n o m y c o s i sr a m ,a c i l l i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ U T I. ,P y l o r i t y p h o i d f e v e r
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impairment ofplatelet aggregation.
irritative responses to penicillin at site
of injection
phlebitis or thrombophlebitis
nausea, with or without vomiting
Intrathecal injection of penicillin G
may produce arachnoiditis
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PROBENECID
Probenecid is an oral drug used for reducingblood uric acid levels in patients with
hyperuricemia (high uric acid)
Probenecid prevents attacks of gout by
reducing uric acid levels in the blood.
It does this by preventing the reabsorption of
uric acid by the kidney and increasing its
excretion from the body in the urine.
Probenecid also blocks excretion by thekidney of penicillin and related antibiotics
and is used for increasing the levels of the
antibiotics in the blood and increasing
their effectiveness when treating
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PRESCRIBED FOR:PRESCRIBED FOR:
Probenecid is used for the treatment
ofhyperuricemia associated with
gout. It also is used for increasing
blood levels of penicillin-type
antibiotics (for example, ampicillin
and amoxicillin).
http://www.medicinenet.com/script/main/art.asp?articlekey=693http://www.medicinenet.com/script/main/art.asp?articlekey=692http://www.medicinenet.com/script/main/art.asp?articlekey=692http://www.medicinenet.com/script/main/art.asp?articlekey=693 -
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SIDE EFFECTS:
Common side effects of probenecid include
headache, dizziness, nausea, vomiting, skin
rash, sore gums, and fever.
Probenecid may cause a flare of gout and
kidney stones, and it is not started during an
acute attack of gout.Serious but rare side effects include reduced
red blood cell counts (anemia), liver damage
and severe allergic reactions.
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