condensed notes-mech of antibiotic

1
These antimicrobial agents usually interfere with bactral physiology (e.g. Macrolids [erythromicine], Clindamycin, Sulfamethoxazole, Trimethoprim, the Tetracyclines, and Chloramphenicol Bacteriostatic: antimicrobial agents that inhibit growth and/or reproduction of infecting agent, but fail to actually kill the bactra E.g. the β-lactam antibiotics (penicillin & cephalosporin), vancomycin, aminoglycosides (gentamycin), and fluoroquinolones (ciprofloxacin) Bacteriocidal: Antimicrobial agent capable of causing irreversible dmg or death to organism Antimicrobials may be bacteriostatic @ low conc but bacteriocidal @ high conc b/c @ cidal doses, it may be toxic to host too Most commonly, the inhibitory conc is used to quantitate the activity of an agent against an organism (aka Minimal Inhibitory Concentration [MIC]) A factor that affects whether a drug is bacteriostatic or bacteriocidal is the antimicrobial concnetration @ the site Distinguish b/w bacteriostatic and bacteriocidal - Most interfere w/ peptidoglycan synth These agents include the β-lactam antibiotics (penicillin, cephalosporin, monobactams, carbapenems) and the glycopeptides (vancomycin) Polysaccharide portion of peptidoglycan structure is made of repeating units of NAG-NAM However, β-lactam antibiotics, like penicillin, binds irreversibly @ the active site of the enzyme that cross links the peptidoglycan strands --> bactral cell wall is prevented from forming The bactral cell wall is complete when crosslink b/w 2 peptide chains + the NAG-NAM backbone Mech of action: Penicillin (there are different CLASSES of penicillin) Cephalosporin (cephalosporins are categorized by "generations"; each generation gets stronger Monobactams (Aztreonam): active against aerobic gram- bacilli Carbapenems: active against essentially all pathogenic org (these are the tanks of the antibiotics) 4 main β-lactams Glycopeptides (Vancomycin): Effective against ONLY Gram+ Interfere w/ cell wall synthesis (most common) 1. Interfere w/ formation of 30S initiation complex or 50S ribosome = interferes w/ formation of 70S ribosome (found in prokaryotic cells and not euk) Block the elongation process of assembling amino acids into a polypeptide Can interfere w/ protein synthesis of bactra by: Aminoglycosides (gentamycin, tobramycin, amikacin, streptomycin): interferes w/ 30S [bacteriocidal] Linezolid: binds to 23S portion of the 50S subunit [bacteriostatic]; however, should only be used against Gram+ bactra that are resistant to other antibiotics Macrolids (erythromycin, azitheromycin, clarithoromycin): Acts by binding to 23S rRNA of the 50S subunit [bacteriostatic] Lincosamides (clindamycin): similar to macrolids Chloramphenicol: binds 23 rRNA; special note for this is that it is effective against many Salmonella; this is used when othe r antibiotics are contraindicated [bacteriostatic] Tetracyclines: inhibit bactral protein synth by blocking 30S subunit [bacteriostatic] Main antibiotics that interfere in this way: Interfere w/ protein synthesis (second most common mech) 2. Bacitracin (topical): disrupt cytoplasmic membrane Anti-fungals: alter the sterol structure and fxn (cholesterol-like structure found in fungi) Interfere w/ cytoplasmic membrane fxn 3. Quinolones/fluorquinolones (ciprofloxacin "cipro", levofloxacin, norfloxacin): inhibit DNA gyrase or topoisomerase req for DN A supercoiling [bacteriocidal] Metronidazole: metabolic cytotoxic byproducts that disrupt DNA [bacteriocidal] Interferes w/ DNA Used for TB Rifampin: binds to DNA-dependent RNA polymerase --> inhibit RNA synthesis [bacteriocidal] Bacitracin (topical): inhibit RNA transcription [bacteriocidal] Interferes w/ RNA Interfere w/ nucleic acid synth 4. Sulfonamides [bacteriostatic] and Dapsone [bacteriocidal]: prevent synth of folic acid Trimethoprim: prevent synth of folic acid [bcateriostatic] Used to treat UTI, middle ear infections, bronchitis, traveler's diarrhea, and shigellosis Triimethoprim + Sulfamethoxazole used in combination: synergistic effects cause bacteriocidal Interfere w/ metabolic pathway 5. Antibiotics inhibit or kill bactra by one of 5 main mechs List the 5 modes of action of antibiotics drugs on the bactral cell, and give an example of each - Learning Objectives Condensed Notes Saturday, August 23, 2014 8:57 PM Microbiology Page 1

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  • These antimicrobial agents usually interfere with bactral physiology (e.g. Macrolids [erythromicine], Clindamycin, Sulfamethoxazole, Trimethoprim, the Tetracyclines, and Chloramphenicol

    Bacteriostatic: antimicrobial agents that inhibit growth and/or reproduction of infecting agent, but fail to actually kill the bactra

    E.g. the -lactam antibiotics (penicillin & cephalosporin), vancomycin, aminoglycosides (gentamycin), and fluoroquinolones (ciprofloxacin)

    Bacteriocidal: Antimicrobial agent capable of causing irreversible dmg or death to organism

    Antimicrobials may be bacteriostatic @ low conc but bacteriocidal @ high conc

    b/c @ cidal doses, it may be toxic to host tooMost commonly, the inhibitory conc is used to quantitate the activity of an agent against an organism (aka Minimal Inhibitory Concentration [MIC])

    A factor that affects whether a drug is bacteriostatic or bacteriocidal is the antimicrobial concnetration @ the site

    Distinguish b/w bacteriostatic and bacteriocidal-

    Most interfere w/ peptidoglycan synth These agents include the -lactam antibiotics (penicillin, cephalosporin, monobactams, carbapenems) and the glycopeptides (vancomycin)

    Polysaccharide portion of peptidoglycan structure is made of repeating units of NAG-NAM

    However, -lactam antibiotics, like penicillin, binds irreversibly @ the active site of the enzyme that cross links the peptidoglycan st rands --> bactral cell wall is prevented from forming

    The bactral cell wall is complete when crosslink b/w 2 peptide chains + the NAG-NAM backbone

    Mech of action:

    Penicillin (there are different CLASSES of penicillin)

    Cephalosporin (cephalosporins are categorized by "generations"; each generation gets stronger

    Monobactams (Aztreonam): active against aerobic gram- bacilliCarbapenems: active against essentially all pathogenic org (these are the tanks of the antibiotics)

    4 main -lactams

    Glycopeptides (Vancomycin): Effective against ONLY Gram+

    Interfere w/ cell wall synthesis (most common)1.

    Interfere w/ formation of 30S initiation complex or 50S ribosome = interferes w/ formation of 70S ribosome (found in prokaryo tic cells and not euk)Block the elongation process of assembling amino acids into a polypeptide

    Can interfere w/ protein synthesis of bactra by:

    Aminoglycosides (gentamycin, tobramycin, amikacin, streptomycin): interferes w/ 30S [bacteriocidal]

    Linezolid: binds to 23S portion of the 50S subunit [bacteriostatic]; however, should only be used against Gram+ bactra that a re resistant to other antibioticsMacrolids (erythromycin, azitheromycin, clarithoromycin): Acts by binding to 23S rRNA of the 50S subunit [bacteriostatic]

    Lincosamides (clindamycin): similar to macrolidsChloramphenicol: binds 23 rRNA; special note for this is that it is effective against many Salmonella; this is used when othe r antibiotics are contraindicated [bacteriostatic]

    Tetracyclines: inhibit bactral protein synth by blocking 30S subunit [bacteriostatic]

    Main antibiotics that interfere in this way:

    Interfere w/ protein synthesis (second most common mech)2.

    Bacitracin (topical): disrupt cytoplasmic membraneAnti-fungals: alter the sterol structure and fxn (cholesterol-like structure found in fungi)

    Interfere w/ cytoplasmic membrane fxn3.

    Quinolones/fluorquinolones (ciprofloxacin "cipro", levofloxacin, norfloxacin): inhibit DNA gyrase or topoisomerase req for DN A supercoiling [bacteriocidal]

    Metronidazole: metabolic cytotoxic byproducts that disrupt DNA [bacteriocidal]

    Interferes w/ DNA

    Used for TBRifampin: binds to DNA-dependent RNA polymerase --> inhibit RNA synthesis [bacteriocidal]

    Bacitracin (topical): inhibit RNA transcription [bacteriocidal]

    Interferes w/ RNA

    Interfere w/ nucleic acid synth4.

    Sulfonamides [bacteriostatic] and Dapsone [bacteriocidal]: prevent synth of folic acidTrimethoprim: prevent synth of folic acid [bcateriostatic]

    Used to treat UTI, middle ear infections, bronchitis, traveler's diarrhea, and shigellosis

    Triimethoprim + Sulfamethoxazole used in combination: synergistic effects cause bacteriocidal

    Interfere w/ metabolic pathway5.

    Antibiotics inhibit or kill bactra by one of 5 main mechs

    List the 5 modes of action of antibiotics drugs on the bactral cell, and give an example of each-

    Learning Objectives

    Condensed NotesSaturday, August 23, 2014 8:57 PM

    Microbiology Page 1