Antibiotics Flashcard
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| beta-lactam (family) |
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| inhibit cell wall synthesis cidal to actively growing bacteria penicillin, cephalosporins, carbapenems, and monobactam |
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| penicillin (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| beta-lactam some G+ and G-, relatively narrow spectrum bind transpeptidases (PBPs), inhibit PG cross-linking, activate autolysins cidal to actively growing resisted by beta-lactamases, modification of PBPs, changes in permeability of G- OM |
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| cephalosporins (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| beta-lactams five gnerations with greater activity aginst G- and greater B-lactamase resistance inhibit PG cross-linking cidal to actively growing resisted by enterococcal PBPs |
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| carbapenems (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| beta-lactams broad spectrum, effective vs. G+ and G- inhibit PG cross-linking, induces autolysis, resistant to B-lactamases cidal to actively growing no known resistance mechanisms |
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| monobactam (azetronam) (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| beta-lactam effective via aerobic G- inhibits PG cross-linking, induces autolysis, resistant to B-lactamases cidal to actively growing no known resistance mechanism |
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| glycopeptide (family) |
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| inhibits cell wall synthesis binds D-Ala repeat and inhibits PG transglycosylation cidal to actively growing cells vancomycin and telavancin |
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| vancomycin (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| glycopeptide G+ only (too big for G-) binds to D-Ala repeat of PG and inhibits transglycosylation cidal to actively growing resisted by change in 5th amino acid |
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| telavancin (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| glycopeptide G+ skin infections binds D-Ala repeat and prevents PG transglycosylation cidal to actively growing resisted by changes in 5th amino acid |
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| bacitracin (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| bacitracin family G+ only (too big for G-) inhibits dephosphorylation of bactoprenal phosphate, block transfer of Pg monomers across cell membrane cidal to actively growing resisted by G- OM |
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| bacitracin (family) |
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| inhibit cell wall synthesis prevents recycling of bactoprenal phosphate and thereby inhibits transfer of PG monomers across cell membrane cidal to actively growing bacitacin is only member |
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| isoniazid (family) |
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| inhibits cell wall synthesis for mycobacteria blocks mycolic acid synthesis cidal drug INH only member |
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| INH (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| isoniazid effective via mycobacteria inhibits synthesis of mycolic acid cidal resisted by reduced uptake or alteration of target sites |
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| ethambutol (family) |
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| inhibits cell wall synthesis for mycobacetira inhibits arabinoglactan synthesis EMB is only member |
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| EMB (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| ethambutol only mycobacteria inhibits arabinoglactan synthesis static no known resistance mechanisms |
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| polymyxin (family) |
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| disrupt cell membrane cidal polymixin E (colistin) |
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| polymyxin E (colistin) |
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| polymyxin G- only, toxicity limitation binds LPS, inserts into membrane and disrupts integrity causing permeability cidal drug no known resistance mechanism |
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| daptomycin (family) |
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| disrupts cell membrane cidal drugs daptomycin is only member |
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| daptomycin (class, spectrum, mechanism, static/cidal, resistance mechanisms) |
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| daptomycin family G+ only (esp. for vancomycin reistanct) incorporates into membrane in calcium-dependent manner, causes depolarization of membrane cidal drug no known resistance mechanisms |
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| aminoglycosides (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| broad against G+ and G- aerobes, req. O2 dependent transport bind 30S irreversible, cause misread of mRNA and premature release of ribosome; inhibits protein synthesis cidal drugs resisted by plasmid drug-modifying enzymes, modification of target, changes in uptake stretomycin |
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| aminoglycoside members |
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| streptomycin gentamicin tobramycin amikacin |
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| tetracyclines (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| broad, G+ and G- intracellular binds 30S, prevent stable binding of tRNA, blocks elongation and protein synthesis static drugs resisted by plasmid-borne efflux pump and changes in target |
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| tetrcycline members |
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| tetracycline doxycycline tigecycline |
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| chloramphenicol (family/member) (spectrum, mechanism, static/cidal, resistance mechanisms, members) |
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| broad, but toxicity limited; crosses BBB bind 50S, inhibits peptide bond formation, inhibits protein synthesis static drugs resisted by acetyltransferase that modifies drug, mutation in G- porins that change uptake |
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| macrolides (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| primarily G+, alternative to penicillin binds 50S, blocks peptide elongation by blocking translocation or transpeptidation, blocks protein synthesis static drugs resisted by efflux pumps, alteration in binding site, enzymatic modification |
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| macrolide members |
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| erythromycin azithromycin clrithromycin |
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| lincosamides (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| mostly G+, a few G-, anaerobes binds 50S, blocks peptide bond formation, inhibits protein synthesis static drug resisted by efflux pumps, alteration in binding site, enzymatic modification |
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| lincosamide members |
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| clindamycin |
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| oxazolidinones (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| VRE and MRSA bind 50S, inhibits intitiation step of protein synthesis static drugs no known resistance mechanism |
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| oxazolidinones members |
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| linezolid |
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| streptogramins (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| spect: vacomycin-resistant enterococcus faecium bind 50S block protein synthesis at two steps in elongation, inhibit protein synthesis static drug no known resistance mechanism |
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| streptogramin members |
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| dalfopristin + quinupristin = synercid |
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| mupirocin (family/member) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| S. aureus, toxic, only used topically binds isoleucyl-tRNA synthase enzyme, blocks formation of Ile-tRNA, inhibits protein synthesis cidal drugs no known resistance mechanism |
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| quinolones/fluoroquinolones (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| broad range (most G- and lots of G+), poor against streptococci and staphylococci binds to DNA gyrase (G-) or topoisomerase (G+) in complex with DNA, promotes DNA cleavage and interferes with supercoiling cidal drugs resisted by alteration of target DNA enzymes, changes in uptake via porins, efflux pumps |
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| quinolones/fluoroquinolones members |
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| ciprofloxacin moxifloxacin levofloxacin |
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| nitromidazoles (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| anaerobes, microaerophiles, some parasites bacterial enzyme reduces drug's nitro group, active compound damages DNA cidal drugs no known resistance mechanism |
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| nitromidazole members |
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| metronidazole |
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| rifamycin (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| mainly in combo therapy for TB, post-exposure prophylaxis for bacterial meningitis binds beta-subunit of bacterial DNA-dependent RNA polymerase, inhibits transcription cidal drugs resisted by alteration in the RNA polymerase |
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| rifamycin members |
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| refampin rifabutin rifaximin |
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| sulfonamides (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| broad spectrum inhibit para-aminobenzoid acid conversion to DGP acid, stops nucleic acid synthesis, inhibits folic acid metabolism/synthesis static alone, cidal with TMP resistance develops quickly if used alone |
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| sulfonamide members |
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| sulfamethoxazole (SMX) sulfones (dapsone) |
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| trimethoprim (family) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| broad spectrum inhibits DHP reductase, blocks folic acid synthesis static alone, cidal with SMX no known resistance mechanism |
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| trimethoprim members |
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| TMP |
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| nitrofurantoin (family/member) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| mostly for UTIs, usually recurrent requires reduction inside bacteria, inhibits several metabolic processes cidal drugs no known resistance mechanism |
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| PZA = pyrazinamide (family/member) (spectrum, mechanism, static/cidal, resistance mechanisms) |
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| very narrow: mycobacterium tuberculosis cleaved by bacterial enzyme (pyrazinamidase) to active form: pyrazinoic acid cidal to actively growing, mostly static resistance develops quickly if used alone, mutation in gene encoding bacterial enzyme |
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| inhibition of cell wall synthesis |
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| beta-lactams glycopeptides bacitracin isoniazid ethambutol |
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| disrupt cell membrane |
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| poylmyxins daptomycin |
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| 30S protein synthesis inhibitors |
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| aminoglycosides tetracyclines |
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| 50S protein synthesis inhibitors |
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| chloramphenicol macrolides lincosamides oxazolidinones streptogramins |
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| non-ribosomal protein synthesis inhibitors |
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| mupirocin |
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| DNA integrity damaging |
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| quinolones/fluoroquinolones metronidzole |
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| transcription inhibitors |
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| rifamycins |
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| folic acid inhibitors |
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| sulfonamides trimethoprims |
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| penicillins |
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| penicillin G and V |
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| cephalosporings |
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| semi-synthetic Beta-lactam |
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| carbapenems |
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| imipenem, meropenem, ertapenem |
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| monobactams |
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| aztreonam |
