他唑巴坦是一种对特定的耐抑制剂A类β-内酰胺酶有效的抑制剂。
Tazobactam is a potent inactivator of selected inhibitor-resistant class A beta-lactamases.
作者信息
Bonomo R A, Rudin S A, Shlaes D M
机构信息
Research Service, Department of Veterans Affairs Medical Center, Cleveland, OH, USA.
出版信息
FEMS Microbiol Lett. 1997 Mar 1;148(1):59-62. doi: 10.1111/j.1574-6968.1997.tb10267.x.
The beta-lactam beta-lactamase inhibitor combinations (ampicillin/clavulanate, ampicillin/sulbactam, ticarcillin/clavulanate and piperacillin/tazobactam) were tested against selected inhibitor-resistant class A beta-lactamases of the TEM and OHIO-1 varieties. Minimum inhibitor concentrations (MIC) revealed that the Escherichia coli DH5 alpha transconjugate strains that possessed the OHIO-1 beta-lactamase, Met69Ile mutant of the OHIO-1 beta-lactamase, TEM-30 (Arg244Ser) and TEM-31 (Arg244Cys) beta-lactamase were most susceptible to piperacillin and piperacillin/tazobactam. Kinetic experiments with each beta-lactamase demonstrated that tazobactam was 10-25-fold more potent than clavulanate or sulbactam against TEM-30 and TEM-31 beta-lactamase. Tazobactam was also as effective as clavulanate against the Met69Ile mutant of the OHIO-1 beta-lactamase. Among the clinically available beta-lactams and beta-lactamase inhibitors, piperacillin/tazobactam appears to be the most potent combination against selected inhibitor-resistant strains of TEM and OHIO-1 beta-lactamase.
对β-内酰胺类/β-内酰胺酶抑制剂组合（氨苄西林/克拉维酸、氨苄西林/舒巴坦、替卡西林/克拉维酸和哌拉西林/他唑巴坦）针对TEM和OHIO-1型选定的对抑制剂耐药的A类β-内酰胺酶进行了测试。最低抑制剂浓度（MIC）显示，携带OHIO-1β-内酰胺酶、OHIO-1β-内酰胺酶的Met69Ile突变体、TEM-30（Arg244Ser）和TEM-31（Arg244Cys）β-内酰胺酶的大肠杆菌DH5α转导接合子菌株对哌拉西林和哌拉西林/他唑巴坦最敏感。对每种β-内酰胺酶进行的动力学实验表明，他唑巴坦对TEM-30和TEM-31β-内酰胺酶的效力比克拉维酸或舒巴坦高10至25倍。他唑巴坦对OHIO-1β-内酰胺酶的Met69Ile突变体的效果也与克拉维酸相当。在临床上可用的β-内酰胺类和β-内酰胺酶抑制剂中，哌拉西林/他唑巴坦似乎是针对选定的对TEM和OHIO-1β-内酰胺酶耐药菌株最有效的组合。
Zotero 插件