头孢菌素类抗菌药物开发历程及探究近况.doc

头孢菌素类抗菌药物开发历程及探究近况摘 要 头孢菌素类抗菌药物因具有抗菌作用强、临床疗效高、耐青霉素酶、毒性低、过敏反应较青霉素少等优点，经过半个多世纪的发展，已有近70个品种广泛应用于临床。目前通常将头孢菌素类药物分为四代，每代药物都有其各自特点和不同的临床适应证。不过，随着头孢菌素类药物的广泛应用，细菌耐药问题也如影随形。因此，通过对头孢菌素类药物的母核7-氨基头孢烷酸的改造，寻找对耐药菌有效、作用更强的新型头孢菌素类药物成为医药工作者近年来关注的热点。ceftbiprole medocaril和ceftaroline fosamil是最近开发的两个注射用头孢菌素类药物新品种，体内、外研究表明，两药对G+、G-菌及耐甲氧西林金黄色葡萄球菌均具有较好的活性，部分国家已开始上市销售。 关键词头孢菌素类药物 抗菌药物 中图分类号：R978.11 文献标识码：A 文章编号：1006-1533(2011)05-0218-04 Development history and current research status of cephalosporins MENG Xian-min1*，DONG Ping1，JIANG Min1，ZHANG Yong-xin2** (1. Shanghai Public Health Clinical Center Affiliated to Fudan University，Shanghai，201508；2. Huashan Hospital Affiliated to Fudan University，Shanghai，200040) ABSTRACTDue to their advantages such as strong antibacterial activities，good clinical efficacy，activities against penicillinase production bacteria，low toxicities，and fewer allergic reaction compared with penicillin，there are nearly seventy cephalosporins widely used in clinical works during the past half century. Cephalosporins are usually divided into four generations and each generation has its own characteristics and different clinical indications. Bacteria resistance always accompanyies with the continual development of cephalosporin. Therefore，development of new cephalosporins through modifying the cephalosporin nucleus 7-ACA becomes the research focus of medical researchers in recent years. Ceftbiprole medocaril and ceftaroline fosamil are two new parenteral cephalosporins with good activities against gram positive bacteria including MRSA，and gram negative bacteria. Now phase 3 clinical trials of the two cephalosporins have completed，these new cephalosporins will provide us with new options for the treatment of infectious diseases caused by MRSA and mixed bacteria. KEY WORDScephalosporins；antibacterials 头孢菌素类药物（cephalosporins）是一大类半合成β-内酰胺类广谱抗菌药物的总称。在2010年美国微生物学会举办的“第50届美国多学科抗微生物药物与化疗会议（ICAAC）”上发表的ICAAC 50年（1961-2010）回顾录中，将头孢烯类、氧头孢烯类、碳头孢烯类和7α-甲氧头孢烯类等药物也归