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[头孢曲松的抗菌活性]

[Antibacterial activity of ceftriaxone].

作者信息

Bergogne-Berezin E

出版信息

Rev Med Interne. 1985 Mar;6(2):178-86. doi: 10.1016/s0248-8663(85)80062-x.

Abstract

In this study the author reports the main in vitro characteristics of ceftriaxone, a new aminothiazolyl methoxy-iminocephalosporin. The relationship between its structure and the antibacterial activity compared with cefotaxime reveals an expected longer antibacterial efficacy due to a long elimination half-life (8 h). It has been shown that ceftriaxone is highly stable against most either plasmid or chromosome-mediated beta-lactamases. Several studies demonstrated that the spectrum of ceftriaxone included Gram-positive cocci as well as most Gram-negative bacilli even beta-lactamase producers; a variable in vitro activity against Gram-negative aerobic bacteria (Pseudomonas sp., Acinetobacter sp.) has been proved, with a frequent synergistic bactericidal activity when combined with aminoglycosides, or with other beta-lactam antibiotics (carbenicillin, piperacillin). Multiple PBPs targets have been identified, including PBP1b, 2 and 3, leading to filamentation of E. coli, Ps. aeruginosa and Haemophilus cells. As a result, ceftriaxone displays a high intrinsic in vitro activity against troublesome strains and might be considered as a promising new cephalosporin for treatment of severe infections.

摘要

在本研究中,作者报告了一种新型氨噻唑基甲氧基亚氨基头孢菌素——头孢曲松的主要体外特性。与头孢噻肟相比,其结构与抗菌活性之间的关系显示,由于消除半衰期较长(8小时),预期其抗菌效果更持久。已表明头孢曲松对大多数质粒或染色体介导的β-内酰胺酶具有高度稳定性。多项研究表明,头孢曲松的抗菌谱包括革兰氏阳性球菌以及大多数革兰氏阴性杆菌,甚至包括产β-内酰胺酶的菌株;已证实其对革兰氏阴性需氧菌(假单胞菌属、不动杆菌属)的体外活性存在差异,与氨基糖苷类药物或其他β-内酰胺类抗生素(羧苄西林、哌拉西林)联合使用时,常具有协同杀菌活性。已确定多个青霉素结合蛋白(PBP)靶点,包括PBP1b、2和3,导致大肠杆菌、铜绿假单胞菌和嗜血杆菌细胞形成丝状体。因此,头孢曲松对棘手菌株显示出较高的固有体外活性,可被视为治疗严重感染的一种有前景的新型头孢菌素。

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[Antibacterial activity of ceftriaxone].[头孢曲松的抗菌活性]
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