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哌拉西林的体外活性,一种具有异常广谱活性的新型半合成青霉素。

In vitro activity of piperacillin, a new semisynthetic penicillin with an unusually broad spectrum of activity.

作者信息

Verbist L

出版信息

Antimicrob Agents Chemother. 1978 Mar;13(3):349-57. doi: 10.1128/AAC.13.3.349.

Abstract

The in vitro activity of piperacillin (T-1220), a new semisynthetic derivative of aminobenzylpenicillin, was investigated. The majority of streptococci and pneumococci were inhibited by 0.12 micrograms/ml; the staphylococci and enterococci were inhibited by 2 micrograms/ml. Piperacillin was slightly more active against Neisseria and Haemophilus influenzae than was ampicillin. Piperacillin was active against all members of the Enterobacteriaceae including the Klebsiella, 58% of which were inhibited by 8 micrograms/ml. The activity of piperacillin was at least equivalent, but generally superior, to that of ampicillin or carbenicillin on species susceptible to these drugs. Most striking was its activity on Pseudomonas aeruginosa: 50% were inhibited by 2 micrograms/ml, and 83% were inhibited by 4 micrograms/ml. The minimum bactericidal concentrations were very close to the minimum inhibitory concentrations, and in most species only a slight inoculum effect was observed on the minimum bacterial values except for certain P. aeruginosa strains. A complete parallel resistance exists between piperacillin and ampicillin or carbenicillin. However, the clinical importance of this is largely mitigated by the intrinsically higher activity of piperacillin.

摘要

对氨基苄青霉素的一种新型半合成衍生物哌拉西林(T - 1220)的体外活性进行了研究。大多数链球菌和肺炎球菌被0.12微克/毫升的浓度所抑制;葡萄球菌和肠球菌被2微克/毫升的浓度所抑制。哌拉西林对奈瑟菌属和流感嗜血杆菌的活性略高于氨苄西林。哌拉西林对包括克雷伯菌属在内的所有肠杆菌科细菌均有活性,其中58%被8微克/毫升的浓度所抑制。在对这些药物敏感的菌种上,哌拉西林的活性至少与氨苄西林或羧苄西林相当,但通常更优。最显著的是其对铜绿假单胞菌的活性:2微克/毫升的浓度可抑制50%,4微克/毫升的浓度可抑制83%。最低杀菌浓度与最低抑菌浓度非常接近,并且在大多数菌种中,除了某些铜绿假单胞菌菌株外,在最低抑菌浓度值上仅观察到轻微的接种量效应。哌拉西林与氨苄西林或羧苄西林之间存在完全平行的耐药性。然而,哌拉西林本身较高的活性在很大程度上减轻了这一情况的临床重要性。

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