第40章-β-内酰胺类抗生素黄仁彬.pptVIP

Chapter 40  β-内酰胺类抗生素 (β-lactam Antibiotics) Key concept 1 β-Lactam antibiotics are frequently prescribed drugs that share a common structure and mechanism of action by inhibition of synthesis of the bacterial peptidoglycan in the cell wall of the microorganism β-内酰胺类抗生素是一类具有相同化学结构的临床常用药物，它们的共同作用机制是抑制细菌细胞壁的肽聚糖合成， Penicillins G and V are commonly used penicillins, which are highly active against susceptible gram-positive cocci. The penicillinase-resistant penicillins such as methicillin are effective against penicillinase-producing staphylococcus aureus; 青霉素G和V是常用的青霉素类抗生素，主要用于敏感的G+球菌。耐青霉素酶类如甲氧西林，主要用于产青霉素酶的金黄色葡萄球菌 Ampicillin and amoxicillin are broad spectrum with activity against gram positive and negative bacteria. Ticarcillin and piperacillin are activity against pseudomonas aeruginosa. 氨苄西林和阿莫西林是广谱抗生素，对G+菌和G-菌均有效。替卡西林和哌拉西林主要用于铜绿假单胞菌 The cephalosporin antibiotics are classified by generation, with the first-generation agents having strong gram-positive and weak gram-negative activity with nephrotoxicity 头孢菌素类抗生素分为四代：第一代头孢菌素对G+菌有强抗菌活性，对G-菌弱，有肾毒性 The second generation drugs showing somewhat better activity against gram-negative bacteria and anaerobes with less nephrotoxicity. 第二代头孢菌素与第一代头孢菌素相比对G-菌和厌氧菌有较强抗菌活性，肾毒性较第一代有所降低 The third generation agents providing more resistance to degradation by β-lactamases, less activity against gram-positive organisms and much more activity against gram negative bacteria, and little nephrotoxicity. 第三代头孢菌素对β-内酰胺酶的稳定性增加，对G+的作用降低，对G-菌的作用增强，对肾基本无毒性 The fourth generation drugs exhibiting a spectrum similar to the third, but with further increased stability to hydrolysis by β-lactamases 第四代头孢菌素与第三代头孢菌素抗菌谱基本相似，不易被β-内酰胺酶水解 β-lactamase inhibitors such as sulbactam, clavulanate and tazobactam are used in combination with β-lactam, in order to increase their activity and extend their antibacterial spectrum against β-lactamase-producing organisms. β-内酰胺酶抑制剂（如舒巴坦、克拉维酸、三唑巴坦）与β-内酰胺类抗生