新一代β－内酰胺抗生素对阴沟杆菌β－内酰胺酶的诱导分析  

INDUCTION OF β-LACTAMASE BY NEW-GENERATION β-LACT AM ANTIBIOTICS IN ENTEROBACTER CLOACAE

作　　者：黎世能[1] 王浴生[1] 雷军[1] 

机构地区：[1]华西医科大学药理教研室,成都中医学院附院临床药理研究室

出　　处：《中国抗生素杂志》1994年第5期367-371,共5页Chinese Journal of Antibiotics

摘　　要：研究４种新一代－β内酰胺抗生素，氨曲南（ＡＺ）、亚胺培南（ＩＭＩ）、头孢噻肟（ＣＴＸ）和哌拉西林（ＰＩＰＣ）对耐ＡＺ阴沟杆菌及其敏感株的β－内酰胺酶诱导发现，ＩＭＩ为强诱酶剂，ＣＴＸ次之，ＡＺ和ＰＩＰＣ较弱；药物对细菌诱酶能力还与细菌外膜通透性，是否发生组成型突变有关。进一步分析诱导产生的β－内酰胺酶的水解底物轮廓，对酶抑制剂敏感性及等电点，发现诱导酶与组成酶、基础酶性质相似，均属Ｒｉｃｈｒｎｏｎｄ－Ｓｙｋｅｓ分类中１型酶。时间杀菌曲线表明，１／４ＭＩＣ的ＡＺ与１／４ＭＩＣ的ＩＭＩ联用于对两药均敏感的阴沟杆菌，产生相互拮抗。The induction of β-lactamase by 4 new-generation β-lac-tam antibiotics was studied in 2 strains of Aztreonam-resistant Enterob-acter cloacae and their correspondant wild type strains.Results showed that ainong the tested β-lactam antibiotics,Imipenem had the hig-hest inducing activity,Cefotaxime lower,Aztreonam and Piperacillin the lowest,and the degree of induction was reiated to permeability of outer membrane and constitutive mutation of the bacteria. Analysis of the in-ducible β-lactamase in hydrolysis substrate profile,susceptibility to β-1-actamase inhibitors and isoelectric point showed that its characteristic was almost the same with the β-lactamses from the correspondent const-itutive mutant and wild type strain,belonging to Richmand & Sykes typeIβ-lactamase. The time-killing curves showed that antagonism occured bctween Imipenem in MIC/4 concentration and Aztreonam, which sugge-sts that β-lactamase was induced.

关 键 词：β 内酰胺酶 阴沟杆菌 氨曲南 亚胺培南 

分 类 号：R978.11[医药卫生—药品] R915[医药卫生—药学]