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g=parenteral, v=oral active against G+ susceptible to B lacatamases |
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penicillin resistant, narrow spectrum protected against B lactamases Used only against pen-G resistan staphylocci not effective against G- |
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broad-spectrum (aminopenicillins) additional activity against G- susceptible to B lactamases |
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carboxypenicillin pseudomonas aeurginosa other G- infections susceptible to B lactamase large doses cause sodium overload |
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ureidopenicillin pseudomonas aeurginosa other G- infections susceptible to B lactamase |
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most common drug allergy due to breakdown into peniccoyl which binds proteins cross reactive to beta lactams hypersensitivity can be fatal |
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high against G+ alternative if mild penicillin allergy prophylaxis in surgery |
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more active against G- resistance to B lactamases less active than 1st gen to G+ poor CNS penetration |
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good CNS penetration and good against G- meningitis and gonorrhea |
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broad spectrum, good CNS, useful in empirical treatment |
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cleared by kidney poor absorption of many of them hypersensitivity, diarrhea, potentially nephrotoxic |
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B lactam w/ broad spectrum binds PBP1 and PBP 2 primarily kidney elimination cilastatin prevents renal inactivation nausea, diarhhea, seizures |
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Monobactam binds PB3 to inhibit cell wall synth. active toward G- only IV due to poor absorption excreted by kidneys resistant to B lactamases safe in patients with penicillin allergy |
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tricyclic glycopeptied prevents polymerization of cell wall precursors only works in G+ excreted by kidneys treats MRSA, severe CDAD Ok for penicillin allergies ototoxic, red man syndrom, thrombophlebiits |
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phosphoenol pyruvate analogue for G- UTI inhibits production of murein monomers enters bacteria via glycerophosphate monomer |
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works on G+ cyclic polypeptide inhibits bactoprenol dephosphorylation bactoprenol trans murein monomers into periplasmic space used topically with other agents nephrotoxic in high concentrations |
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interfere with protein synthesis streptomycin, gentamicin, amikacin, neomycin (SANG) HIGHLY POLAR--not well distributed attract LPS bactericidal against G- passive diffusion through porins then active transport into cytosol (O2 dependent) binds 30S and causes RNA misreading blockade of translocation LONG post antibiotic effect |
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aminoglycoside 2nd line for tuberculosis |
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combine with B lactam to fight G+ cocci and also effective in combo againsst G- organisms |
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aminoglycoside least susceptible into inactivation |
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aminoglycoside topical therapy |
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aminoglycosides (adverse reactions) |
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ototoxicity if long exposure nephrotoxicity neuromuscular blockade |
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transported by active transport binds 30S, inhibits binding of tRNAs to A site of mRNA ribosomal complex resistance due to production of interfering proteins or efflux transporters orally effective, forms chelates, distributed widely in CNS, bone teeth, placent, breast milk |
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tetracycline (uses and adverse rxns) |
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G+ and G- organisms tigecycline--new and effective rickettsia, chlamydia, lyme disaese, anthrax, mycoplasma pneumonia acne and periodontal disease treat peptic ulcer with metronidazole combo prophylaxis of malaria
ADVERSE: GI irritation, bone and teeth deposition (don't give to kids), renal toxicity, superinfection (CDAD), hepatotoxicity, photosensitivity |
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Macrolides (erythromycin) |
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bacteriostatic bind reversibly to P site on 50S, inhibiting translocation Resistance--efflux or methylation of 50S subunit via erm ghepatic metabolism via cyp3A4--interacts with other drugs Legionnaire's, whooping cough, diptherica, chlamydia ADVERSE: GI irritation chestatic hepatitis, prolonged Q-T |
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Lincosamide binds at 50S to block peptide bond formation G+ aerobes Group A strep, gas gangrene, abdominal and pelvic bacteroides fragilis diarrhea and CAD--adverse |
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binds peptidyl transferase to prevent attachment of incoming tRNA to A site MRSA, G- anaerobes widely distributed and liver metabolism resistance--acetyltransferase only for life threatening situations ADVERSE--grey baby, bone marrow suppression, aplastic anemia |
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oxazolidinone binds at unique site of 23S rRNA of 50S subunite--blocks fomration of initiation complex use--MDR G+--VRE and MRSA ADVERSE--myelosuppression (anemia, leucopenia, thrombocytopenia) interacts w/ MAOIs and SSRIs |
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quinupristin-dalfopristin |
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synergistic combo bind to peptidyl transferase of 23S rRNA to block initiation dalfopristin--inhibits peptidyl transferase Quinupristin binds at macrolide ssite mainly for G+ ADVERSE--hyperbilirubinemia and myalgia/arthralgia |
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(ciprofloxacin) inhibit one of two topoisomerase II enzymes prophylaxis of anthrax urogenital tions ADVERSE--tendon rupture, confusion, prolonged Q-T interval CDAD inc. plasma levels of warfarin and theophylline reduced absorption with cations |
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anaerobic bacteria and protozoa prodrug--PFOR or nitroreductase in anaerobes produces cytotoxic intermediates that destray DNA! use for CDAD Use with tetracycline to fight H. pylori ADVERSE--headache, GI disturbances, weird colored urine, metallic taste CYP3A4 substrate |
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sulfonamide inhibits dihydropteroate synthase (folic acid synthesis)--prevents DNA replication board spectrum G+/G- E coli UTI ADVERSE Kernictus, hypersensitivity, hemolytic anemia, renal damage |
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inhibitor of dihydrofolate reductase use against G- and G+ UTIs bone marrow suppression |
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synergistic TMP/SMX broad spectrum of G+/G- ADVERSE: myelosuppression UTIs, pneumocystis jirovici pneumonia otitis media infections |
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cycli lipopetide Ca++ dependent insertion into membrane only active against G+ skin infections by MRSA or VRSA ADVERSE-myopathy |
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polymyxin E binds plasma membrane and disrupts bilayer two forms--sulfate (dermal, oculare, GI) and methate (parenteral) MDR G- ADVERSE--neuro/nephro toxic |
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inhibits mycolic acid synthesis passively diffuses into mycobacteria activated by KatG resistance--change in KatG gene inactivated by liver acetylatin treats TB peripheral neuropathy due to loss of B6 Hepatotoxicity--potentially fatal necrosis |
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Rifamycin binds to B subunit of RNA polymerase resistance--muation of rpoB treats TB, leprosy, H influenzae, S aureus, Legionalla, Neisseria meningitidis ADVERSE--hepatotoxic (jaundice and hepatitis) discoloration of body fluids induces many CYP forms |
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Inhibits mycolic acid syntehsis via arabinosyl transferase III resistance--embAB gene use to treat TB in combo ADVERSE--optic neuritis |
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prodrug--converted to pyrazinoic acid by mycobacterial pyrazinamidase treat TB ADVERSE--hepatotoxic, hyperuricemia(gout) |
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