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哌拉西林(T - 1220),一种新型半合成青霉素:与羧苄西林、替卡西林、氨苄西林、头孢噻吩、头孢孟多和头孢西丁的体外抗菌活性比较

Piperacillin (T-1220), a new semisynthetic penicillin: in vitro antimicrobial activity comparison with carbenicillin, ticarcillin, ampicillin, cephalothin, cefamandole and cefoxitin.

作者信息

Jones R N, Thornsberry C, Barry A L, Fuchs P C, Gavan T L, Gerlach E H

出版信息

J Antibiot (Tokyo). 1977 Dec;30(12):1107-14. doi: 10.7164/antibiotics.30.1107.

Abstract

Piperacillin (T-1220) is a new semisynthetic penicillin with an unusually broad spectrum of antimicrobial activity. In vitro comparisons of this drug with 6 other beta-lactam antimicrobics (ticarcillin, carbenicillin, ampicillin, cephalothin, cefamandole and cefoxitin) were conducted. These included minimal inhibitory concentrations (MIC) against 394 bacterial isolates, the minimal lethal concentrations (MLC) against 79 of those, as well as the effect of inoculum size on the MIC and MLC of the drugs. Piperacillin had significantly greater activity than did the other penicillins against Pseudomonas species and Klebsiella pneumoniae. Against P. aeruginosa piperacillin was 8- and 16-fold more active than ticarcillin and carbenicillin, respectively. The MLC of piperacillin rarely differed from the MIC by more than one log2 dilutions except against P. aeruginosa in which the MLC was 4-fold greater or more than the MIC of 45% of isolates tested. Ticarcillin, carbenicillin and cefoxitin showed minimal inoculum size effects. Cefamandole results showed the greatest inoculum size variation with 55% and 37% of isolates showing an 8-fold increase in MIC and MLC respectively by increasing inoculum from 10(5) to 10(7) CFU/ml. Piperacillin was intermediately effected having 25% of strains greater than 8-fold increase in MIC.

摘要

哌拉西林(T - 1220)是一种新型半合成青霉素,具有异常广泛的抗菌活性谱。对该药物与其他6种β-内酰胺类抗菌药物(替卡西林、羧苄西林、氨苄西林、头孢噻吩、头孢孟多和头孢西丁)进行了体外比较。这些比较包括对394株细菌分离株的最低抑菌浓度(MIC)、对其中79株的最低致死浓度(MLC),以及接种量对药物MIC和MLC的影响。哌拉西林对假单胞菌属和肺炎克雷伯菌的活性明显高于其他青霉素。对铜绿假单胞菌,哌拉西林的活性分别比替卡西林和羧苄西林高8倍和16倍。除对铜绿假单胞菌外,哌拉西林的MLC与MIC的差异很少超过1个对数2稀释度,在对铜绿假单胞菌的测试中,45%的分离株MLC比MIC大4倍或更多。替卡西林、羧苄西林和头孢西丁显示出最小的接种量效应。头孢孟多的结果显示接种量变化最大,当接种量从10⁵增至10⁷CFU/ml时,分别有55%和37%的分离株MIC和MLC增加8倍。哌拉西林受到的影响处于中间水平,25%的菌株MIC增加超过8倍。

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