新型β-内酰胺酶抑制剂——阿维巴坦的研究进展  

The Research Advance of a Novel β-lactamase Inhibitor—Avibactam

作　　者：曾志旋 曹胜华[1] 陈林[1] 

机构地区：[1]四川抗菌素工业研究所,成都610052

出　　处：《国外医药（抗生素分册）》2014年第2期58-62,共5页World Notes on Antibiotics

摘　　要：阿维巴坦(Avibactam)是一个与酶可逆性共价结合新型的β-内酰胺酶抑制剂,目前处于Ⅲ期临床试验。阿维巴坦较已上市的3个β-内酰胺酶抑制剂——克拉维酸、舒巴坦、三唑巴坦——作用更强范围更广,对A类、C类和部分D类β-内酰胺酶抑制作用显著。与头孢他啶、头孢洛林等药物联用时,其能够恢复或增强抗生素的活性,耐受性良好,无严重不良事件报道。本文对阿维巴坦的作用机制、药代动力学、联合用药、毒副作用和合成路线等方面作一综述。Avibactam is a novel β-lactamase inhibitor which is able to bond reversibly and covalently to β-lactamase, and currently it is in phase Ⅲ clinical trials. The efficacy of avibactam is stronger than the three listed β-lactamase inhibitors named clavulanic acid, sulbactam and tazobactam, and the spectrum of it is also broader than them. Avibactam remarkably inhibits the activities of ambler class A, ambler class C β-lactamase and some ambler class D enzymes. What＇s more, drugs like ceftazidime, ceftaroline and etc. combine with avibactam, their efficacy can be restored or enhanced. The combinations are of good tolerance and have no serious adverse events. The mechanism, pharmacokinetics characteristics, drug combination, adverse events, synthesis routte and other aspects of avibactam are summaried in the article.

关 键 词：阿维巴坦 Β-内酰胺酶抑制剂 作用机制 联合用药 

分 类 号：R978.1[医药卫生—药品]