qingmeisu课件.pptVIP

β-内酰胺类抗生素β-Lactam antibiotics Jingling Zhang and Kehua Jiao Medical school of Nankai University β-Lactam antibiotics 目的 掌握青霉素和头孢霉素的抗菌作用。抗菌谱、适应症、不良反应及其防治。青霉素G，各种半合成青霉素以及各种头孢霉素的特点。了解两类药物的发展概况。 β-Lactam antibiotics 内容 青霉素G的理化性质，抗菌谱，抗菌作用原理和作用特点。体内过程和用药方法。细菌耐药性，过敏反应及其防治。临床用途。 普鲁卡因青霉素G及苄星青霉素产生长效的原因及其临床评价。以6-氨基青霉烷酸为母核人工加上侧链形成半合成青霉素。新青霉素具有耐青霉素酶特性。用于耐药性金葡菌感染。 β-Lactam antibiotics 广谱青霉素氨苄青霉素和羧苄青霉素以及抗绿脓杆菌作用强的广谱青霉素的抗菌作用特点及临床用途。 头孢霉素类为以7-氨基头孢烷酸为主核加上不同侧链的半合成抗菌素。化构和抗菌作用原理与青霉素相似，抗菌谱较广。常用的有头孢菌素第一代，第二代，第三代等。各药的特性和临床应用。 β-Lactam antibiotics Definition Classification Mechanism of action Resistance of microorganisms Penicillin β-Lactam antibiotics Cephalosporins Other β-lactam antibiotics β-lactamase inhibitors β-Lactam antibiotics Definition They are useful and frequently prescribed antibiotics that share a common structure and mechanism of action –inhibition of synthesis of the bacterial peptidoglycan cell wall. β-Lactam antibiotics Classification Penicillin Cephalosporins Other β-lactam antibiotics β-lactamase inhibitors β-Lactam antibiotics Mechanism of action Inhibit bacterial growth by interfering with a specific step in bacterial cell wall synthesis. The cell wall is a rigid outer layer that completely surrounds the cytoplasmic membrane. β-Lactam antibiotics Penicillin-biding proteins (PBPs) catalyze the transpeptidase reaction that removes the terminal alanine to form a crosslink with a nearby peptide, which gives cell wall its structural rigidity. β-Lactam antibiotics Type of PBPs (glycopeptide synthetase): 1A 9000 1B 9000 2 66000 3 60000 4, 5 and 6, 49000, 42000, 40000 β-Lactam antibiotics Penicillins are structural analogs of the natural D-Ala-D-Ala substrate. They are covalently bound by PBPs at the active site. After Penicillin has attached to the PBP, the transpeptidation reaction is inhibited, mucopeptide synthesis is blocked, and the cell dies. β-Lactam antibiotics The exact mechanism responsib