4_antifungal

4_antifungal - Mechanism of action of penicillin drugs Amidase enables synthetic penicillin R Binding PBPs and inactivating them Transpeptidases

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1 Mechanism of action of penicillin drugs Binding PBPs and inactivating them Transpeptidases; blocking cell wall synthesis Inhibitors of autolytic enzymes, resulting in cell lysis and death R Amidase enables synthetic penicillin R amidase Penicillin subgroups Penicillins (penicillin G) Antistaphylococcal penicillins (naficillins) Extended spectrum (ampicillins) Gram - bacteria PBP β -lactamase peptidoglycans porins Periplasmic space phospholipids
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2 Structure function relationship of semisynthetic penicillins Bioavailability Resistance spectrum Oral β -lactamase R G R-group Penicillin V yes no Methicillin no yes Oxacillin yes yes Cloxacillin yes yes Dicloxacillin yes yes Naficillin no yes Ampicillin yes no Penicillin G no no Pharmacokinetic factors penicillins are widely distributed and therapeutic concentrations are readily achieved CSF levels are variable however when meninges are inflamed high concentrations are attained eliminated rapidly by glomerular filtration Therapeutic use of penicillins (examples) - pneumococus pneumonia resistant strains frequently isolated. -meningococcal infections- resistant strains reported in Britain and Spain - ampicillin is effective against H. influenza (25-to 30% resistance) -most strains of N. gonorrhoea, E. coli P. mirablis and Salmonella (increasing percentage of these species is now resistant) How do we fight resistance? An inhibitor of beta lactamases
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3 Other beta lactam analogs penicillins cephalosporins monobactams carbapenem Cephalosporins Mechanisms of resistance against cephalosporins inability to reach site of action alterations in PBPs Discussion of Vancomycin is found in Brody chapter 45
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This note was uploaded on 02/22/2011 for the course PHAR 301 taught by Professor Hales during the Spring '11 term at McGill.

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4_antifungal - Mechanism of action of penicillin drugs Amidase enables synthetic penicillin R Binding PBPs and inactivating them Transpeptidases

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