氨曲南和亚胺培南对β－内酰胺酶稳定性和抑酶效应的研究  

Study of stability and inhibitory activity of aztreonam and imipenem to β-lactamases

作　　者：黎世能[1] 王浴生[1] 雷军[1] 

机构地区：[1]华西医科大学临床药理研究所,成都中医学院附院临床药理研究室

出　　处：《中国药理学通报》1994年第2期133-136,共4页Chinese Pharmacological Bulletin

摘　　要：用紫外分光光度法．以其它青霉素类、头孢菌素类抗生素为对照．研究氨曲南（Ａｚｔｒｅｏｎａｍ．ＡＺ）和亚胺培南（Ｉｍｉｐｅｎｅｍ．ＩＭＰ）对１１种标准β－内酰胺酶的稳定性及抑酶作用。结果表明．ＡＺ．ＩＭＰ与第三代头孢菌素头孢噻甲羧肟．头孢氨噻类似，对１１种标准β－内酰胺酶均高度稳定。除酶Ｋ１对头孢氨噻相对水解率达２５％外．其余均不超过１５％．其余的青霉素类及第一、二代头孢菌素类，除头孢西丁酶稳定性较好外．均对β－内酰胺酶不稳定．大多数相对水解率１００％以上。抑酶结果表明．ＡＺ或ＩＭＰ对β－内酰胺酶抑制，除与β－内酰胺酶类型有关外．还与ＡＺ或ＩＭＰ本身浓度密切关联。Stability and inhibitory activity of aztreonam(AZ) and imipenem(IMP) to 11 stamdard β-lactamases were studied, using peniCillins and cephalosporins as control. The activities of the β-lactamases using cephaloridine(CER) as substrate and the relative hydrolysis rates(RHR) of β-lactams by the β-lactamases was determined spectrophotometrically.The results showed that like ceftazidime and ceftaxime of the 3rd generation cephalosporins,AZ and IMP were very stable to 11 standerd β-lacta mases.RHRs were less than 15%,except the RHR Of ceftaxime by K1 enzyme,Which was 25%.The other β-lactams were susceptible to the β-lactamases and RHRs of most drugs were more than 100% except cefoxitin,which was stable to the β-lactamases.The studies of inhibitory effect revealed that AZ and IMP possessed variable inhibitory action against the hydrolysis of β-lactamases on CER.The inhibitory activity to β-lactamases was related not only to the types of β-lactamases, but also to the con centration of the inhibitors.

关 键 词：氨曲南 亚胺培南 Β-内酰胺酶 

分 类 号：R978.1[医药卫生—药品]