文档介绍:e to Pharmacology
Chapter 5
β-Lactam antibiotics
Contents
1. Classification
2. Mechanism of action
3. Penicillins
4. Cephalosporins
Penicillins
Cephalosporins
Other β-Lactam drugs
β-Lactamase inhibitors
Cephamycins
Monolactums
of action
Inhibiton of bacterial cell wall synthesis
Target: PBPs(penicillin-binding proteins)
Cell-wall autolytic enzyme
Basic structure: 6-APA
Classification
Natural penicillins
Semisynthetic penicillins
Natural penicillins-Penicillin G
Spectrum of activity
Gram-positive i
i , i, i
Gram-negative i
i, i
Gram-positive bacilli
Bacillus perfringens, bacillus diphtheriae
Spirochete
treponema pallidum, leptospira
Clinical use
First choice for the following infections
Infection caused by i, i, i etc
Infection caused by spirochetes
Infection caused by gram-positive bacilli
ics
Absorption T1/2=
Distribution
Excretion probenecid
90% tubular secretion
10% glomerular filtration
Adverse reaction
Allergic mon:
skin rashes,oral lesion,fever,interstitial nephritis, hemolytic anemia,other hematologic disturbances, vasculitis
Severe: anaphylactic shock
Reason:degraded products of penicillin