5 β-Lactam antibiotics药理学英文版.pptVIP

Welcome to Pharmacology Contents 1. Classification 2. Mechanism of action 3. Penicillins 4. Cephalosporins 1.Classification Penicillins Cephalosporins Other β-Lactam drugs β-Lactamase inhibitors Cephamycins Monolactums  2.Mechanism of action Inhibiton of bacterial cell wall synthesis Target: PBPs(penicillin-binding proteins) Cell-wall autolytic enzyme 3.Penicillins Basic structure: 6-APA Classification Natural penicillins Semisynthetic penicillins Natural penicillins-Penicillin G Spectrum of activity Gram-positive cocci pneumococci , staphylococci, Streptococci Gram-negative cocci Meningococci, gonococci Gram-positive bacilli Bacillus perfringens, bacillus diphtheriae Spirochete treponema pallidum, leptospira Clinical use First choice for the following infections Infection caused by streptococci, pneumococci, meningococci etc Infection caused by spirochetes Infection caused by gram-positive bacilli Pharmacokinetics Absorption T1/2=0.5h Distribution Excretion probenecid 90% tubular secretion 10% glomerular filtration Adverse reaction Allergic reaction Common: skin rashes,oral lesion,fever,interstitial nephritis, hemolytic anemia,other hematologic disturbances, vasculitis Severe: anaphylactic shock Reason:degraded products of penicillin Adverse reactions Prophylaxis of allergic reaction Ask allergic history carefully Skin test Adrenaline Other untoward effect gastrointestinal upset—nausea,vomiting and diarrhea Semi-synthesized penicillins Acid-resistant penicillins Penicillinase-resistant penicillins Broad-spectrum penicillins Antipseudomonal penicillins 4.Cephalosporins Chemistry: 7-ACA Classification: four generations First-generation cephalosporins Second- generation cephalosporins Third-generation cephalosporins Fourth- generation cephalosporins Cephalosporins Common characters: Activity on gram-positive bacteria: fourthfirstsecondthird Activity on gram-negative bacteria: firstsecondthirdfourth Stability to β-Lactamase : f