Antibiotics v413

Antibiotics v413 - Class Antibiotic 1st gen Penicillins PCN...

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Class Antibiotic Mechanism Uses Side effects Bioavailability Metabolism Comments 1st gen Penicillins PCN G, PCN V 2nd gen Penicillins 3rd gen Penicillins amoxicillin, ampicillin AKA = aminopenicillins 4th gen Penicillins MSSA, enterobacteriaceae broader activity against gram (-) cefepime Monobactams aztreonam renal excretion Carbapenems Parenteral Vancomycin Notes: Resistance - VRE enterococci: plasmid mediated, enzyme synth D-ala-D-lactic acid --> vancomycin no longer recognizing target Aminoglycosides streptomycin Tetracyclines β -lactam Antibiotic (bacteriocidal): β -lactam ring structural analong of D-ala-D-ala substrate of enzymes (penicillin binding proteins = PBPs) used in cell wall synth. β - lactams are suicide inhibitors of PBPs. PBP- 1 = transpeptidase (inhib-->lysis), PBP-2 = shape (inhib-->round cells), PBP-3 = septum formation (inhib-->long cells); not bacteriocidal in slow growing or dormant bac (eg. endocarditis, osteomyelitis) & bac. that deownregulate autolysin activity. susceptible gram (+), others - Treponema pallidum. First line for: GAS, syphilis, viridans strep endocarditis allergic rxns (cross reactivity from β -lactam ring byproducts), neutropenia, Methicillin - allergic interstitial nephritis, Nafcillin & Oxacillin - hepatitis, CarboxyPCNs - large salt load IV, IM, or Oral, effective: >4x MIC for 60-80% of day, only amoxicillin absorbs w/ food, PCNs distributed to most tissues (NOT CNS, prostate, eye), can cross inflamed meninges, high CSF levels induce seizures short half-life, excreted unchanged in kidney (glomerular filtration & tubular secretion), Probenecid extend half- life (dec tubular sec), Nafcillin/Oxacillin & UreidoPCNs - hepatic excretion natural PCNs, rapid metab, benzathine PCN can be inj IM methicillin, nafcillin, dicloxacillin, oxacillin resist penicillinase of MSSA, less active against gram (+) w/o β -lactamases, NO activity against gram (-) MRSA - methicillin resistant = resistant to all 2nd gen PCNs treat some gram (-) w/o β -lactamases, some activity against gram (+) w/o β -lactamases UreidoPCN:mezlocillin, piperacillin, carboxyPCN: carbenicillin,ticarcillin broad spectrum: gram (-) - Pseudomonas, still inactivated by some β -lactamases, UreidoPCN can be used for gram (+) & enterococci Ureidopenicillins not used for S. aureus 1st gen cephalosporins cephalexin, cefazolin, cephapirin, cephalothin allergy, antabuse rxn (adverse rxn w/ alcohol) & inhibits action of Vit K w/ MTT side chains of cefotetan, cefonicid, moxalactam, cefoperazone Oral or Parenteral, effective: >4x MIC for 60- 80% of day, good tissue penetration (except non- inflam meninges) excreted by kidneys (glomerular filtration & tubular secretion), Cephalothin - deacylated by liver to less active form (don't use in meningitis), Ceftriaxone, Cefotetan, Cefoperazone - some excretion in bile each successive generation is more active against gram (-) and more resistant to β - lactamases, lose activity to gram (+) 2nd gen cephalosporins cefuroxime, cefotetan,
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This note was uploaded on 09/14/2011 for the course PHARM mb taught by Professor Staff during the Spring '11 term at UCSD.

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Antibiotics v413 - Class Antibiotic 1st gen Penicillins PCN...

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