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CLPH873

Antibiotics - MOA/MOR

DrugMOAMOR
Cephalosporins Interfere with cell wall synthesis (binds to and inhibit PBPs in cell walls of bacteria); bactericidal except against Enterococcus 1. Production of beta-lactamase enzymes (plasmid-mediated, chromosomally-mediated, constitutive,inducible) 2. Alteration in structure of PBPs 3. Decreased penetration through outer membrane of gm- bacteria
Penicillins (natural:penG,penVK; pen-ase resistant:nafcillin,dicloxacillin; aminopen:ampicillin,amoxicillin; carboxypen:carbenicillin,ticarcillin; ureidopen:mezlocillin,azlocillin,piperacillin; combo:Augmentin,Unasyn,Zosyn Interfere with cell wall synthesis (binds to and inhibit PBPs in cell walls of bacteria); bactericidal except against Enterococcus 1. Production of beta-lactamase enzymes (plasmid-mediated, chromosomally-mediated, constitutive,inducible) 2. Alteration in structure of PBPs 3. Decreased penetration through outer membrane of gm- bacteria
Carbapenems (imipenem, meropenem, ertapenem, doripenem) 1. Interfere with cell wall synthesis (binds covalently to and inhibits PBP-2-variable affinities); time-dep bactericidal activity except Enterococcus 2. They are zwitterions and are better able to penetrate outer membrane of gm- bacteria to get to PBPs 1. Decreased permeability due to altered membrane porins in gm- bacteria (esp. P.aeruginosa) 2. Production of beta-lactamases-but most display intrinsic resistance to these 3. Alterations in PBPs
Monobactams (aztreonam) 1. Interfere with cell wall synthesis (binds to and inhibits PBPs- prefers PBP-3 in aerobic gm- bacilli); bactericidal 1. Production of beta-lactamase enzymes, but they are relatively stable to plamid/chromosomally-mediated ones
Fluoroquinolones 1. Inhibit DNA synthesis; conc-dep bactericidal activity a. Inhibit DNA gyrase: prevents relaxation of supercoiled DNA (gm-) b. Inhibit topoisomerase IV: interferes with separation of replicated chromosomal DNA into respective daughter cells (gm+) 1. Altered binding sites-mutations in genes that code for subunits of DNA gyrase and topoisomerase IV 2. Efflux pump enhances transfer of FQs out of the cell 3. Altered cell wall permeability-decreased FQ accum in cell-rare 4. Cross-resistance between FQs
Macrolides 1. Suppresses protein synthesis (binds to 50S subunit); bacteriostatic, may be -cidal at higher concentrations (erythro&clarithro-time dep, azithro-conc-dep) 1. Active efflux (mef gene)-confers low-level resistance 2. Alteration in binding site (erm gene)-confers high-level resistance to ALL macrolides AND other antibiotics that bind to 50S ribosome 3. Cross-resistance between macrolides
Aminoglycosides 1. Inhibit initiation of protein synthesis (binds irreversibly to 30S subunit-disruption); rapid conc-dep bactericidal activity; 1. Alteration in AG uptake 2. Synthesis of AG-modifying enzymes 3. Alteration in ribosomal binding sites
Vancomycin
Created by: asuppatk
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