antibacterial agents – Flashcards
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| target criteria |
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| unique to prokaryotic celss essential for growth / metabolism nontoxic to humans |
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| antibacterial target |
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| cell wall synthesis, protein synthesis, nucleic acid synthesis, cell membrane function |
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| penicillins moa |
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| block crossbridge formation (transpeptidation) during sythesis of the cell wall results in osmotic lysis bacteriacodal |
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| penicillins spectrum |
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| Gm + cocci few Gm - |
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| penicillins toxicity |
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| serious allergic response anaphylatic rxn (1/500) |
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| penicillin resistance mechanisms |
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| common produce penicillinase alter structure of the target |
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| natural penicillins use |
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| Gm +, anaerobes, Neisseria and Hemophilus |
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| penicillinase resistant penicillins use |
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| penicillinase-producing staph. aureus and Staph. epidermidis |
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| aminopenicillin use |
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| Gm +, anaerobes, Neisseria, Hemophilus Gm - cocci, enterobacteriaceae, absorbed orally |
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| carboxypenicillins use |
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| anti-pseudomonal Gm - aerobic rods |
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| ureidopenicillins use |
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| anti-pseudomonal Gm - aerobic rods |
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| first generation cephalosporins |
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| Gm + |
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| second generation cephalosporins |
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| + Gm- maintained most Gm + |
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| third gen. cephalosporions |
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| + Gm - bacilli - Gm + |
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| fourth gen cephalosporions |
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| most Gm - Gm + cocci |
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| cephalosporion resistance |
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| same as penicillins |
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| cephalosporions adverse rxs/toxicity |
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| hypersensitivity, rash, diarrhea, vaginal thrush, pseudomembranous colitis |
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| carbapenems spectrum |
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| broadest of all b-lactams |
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| carbapenems use |
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| cephalosporion-resistant enterobacteriaceae polymicrobial infections anaerobes |
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| glycopeptides moa |
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| binds to d-alanyl-d-alanine terminus of the pentapeptide side chain blocks transgylcosylationa nd transpeptidation |
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| glycopeptides use |
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| Gm + cocci not Gm - Drug of last resort |
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| vanco resistance from _ genes and _ mutation |
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| 3, 6 |
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| bacitracin moa |
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| blocks dephosphorylation of peptidogylcan-precursor carrier results in failure to regenerate carrier causing failure to move precursor out of cell |
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| bacitracin use and spectrum |
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| topical Gm + |
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| inhibitors of protein synthesis |
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| block initiation (30 or 70) block elongation prevent peptide completion |
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| aminoglycosides moa |
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| inhibit initiation by blocking 30S initiation complex formation |
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| aminoglycosides spectrum |
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| Gm - bacteria |
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| oxazolidinones moa |
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| binds to 50S and blocks assembly of 70S ribosome |
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| oxazolidinones spectrum |
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| Gm + cocci |
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| tetracycline types |
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| tetracycline - short acting doxycycline - long acting minocycline - long acting glycylcyclines - active against cycline resistant strains |
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| tetracycline moa |
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| reversibly binds to 30S subunit to sterically block aminoacyl-tRNA binding at A site |
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| tetracycline spectrum |
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| broadest of all antibiotics Gm +,- intracelullar wallless |
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| tetracycline toxicity |
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| GI upset and diarrhea |
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| tetracycline contraindications |
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| harms bone development in fetus stains teeth brown in children less than 8 years old |
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| chloramphenicol structure |
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| small, hydrophobic excellent tissue penetration bone, CSF, tissues with poor blood supply |
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| chloramphenical moa |
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| blocks peptide bond formation on 70S ribosome |
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| chloramphenicol spectrum |
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| second line therapy (potentially serious toxicity problems) bacterial meningitis intracellular anaerobes |
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| chloramphenicol toxicity |
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| common - dose dependent bone marrow suppression rare - aplastic anemia (fatal) |
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| macrolides moa |
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| stimulates dissociation of peptidyl-tRNA by blocking peptide exit tunnel can start protein synthesis, but ends synthesis before a functioning protein can be formed |
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| macrolides spectrum |
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| Gm + cocci mycoplamsmas - wall-less chlamydia |
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| macrolide types |
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| erythromycin - more GI upset azithromycin - more active against Gm - enterics clarithromycin - more active against Gm + |
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| lincosamide moa |
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| same as macrolides |
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| lincosmaides spectrum |
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| Gm - enterics anaerobes Pneumocystis jirovecii |
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| lincosamides toxicity |
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| complications from loss of normal flora in GI |
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| ketolides moa |
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| binds to same site as macrolides but with higher affinity |
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| ketolides spectrum |
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| active against most erythromycin resistant strains |
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| streptogramins moa |
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| dalfopristin - type a - block peptide transfer quinupristin - type b - increase dissociation of peptidyl-tRNA |
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| streptogramins spectrum |
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| Gm + some Gm - vanco resistant stuff bone and joint MRSA infections |
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| inhibitors of nucleic acid synthesis |
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| block DNA replicaiton block RNA transcription Block purine synthesis |
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| Quinolones moa |
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| inhibits bacterial topoimoerases and promotes DNA cleavage blocks DNA gyrase causes supercoiling (- twists) |
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| quinolones spectrum |
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| Gm - staph and strep intracellular and wall less anaerobes |
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| rifamycin moa |
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| inhibits b-subunit of DNA dependent RNA polymerase blocks elongation |
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| rifamycins spectrum |
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| Gm + bacteria meningitis treatment and prevention mycobacteria |
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| sulfonomide classes |
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| short and medium acting long acting gi tract limited topical |
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| sulfonomides moa |
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| high affinity for bacterial enzyme that makes tetrahydrofolic acid |
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| sulfonomides resistance |
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| widespread - used in combinations |
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| trimethoprim moa |
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| analog of DHFA inhibits DNA precursor formation |
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| tirmethoprim use |
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| with sulfonomides Gm + cocci Gm - rods |
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| trimethoprim resistance |
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| common - used in combos |
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| sulfa/tmp spectrum |
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| Gm - bacteria UTI's |
