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新型注射用碳青霉烯类药物S-4661对妇科病原体的体内外抗菌活性

In vitro and in vivo antibacterial activities of a new injectable carbapenem, S-4661, against gynaecological pathogens.

作者信息

Mikamo H, Izumi K, Hua Y X, Hayasaki Y, Sato Y, Tamaya T

机构信息

Department of Obstetrics and Gynaecology, School of Medicine, Gifu University, Tsukasa-machi, Gifu City, Gifu 500-8705, Japan.

出版信息

J Antimicrob Chemother. 2000 Sep;46(3):471-4. doi: 10.1093/jac/46.3.471.

Abstract

Carbapenems are often used to treat infections in obstetrics and gynaecology because of their activity against anaerobes. S-4661, a new injectable carbapenem antibiotic, has favourable pharmacokinetic properties and is not hydrolysed by dehydropeptidase I. We investigated the in vitro and in vivo antibacterial activities of S-4661 against strains of Streptococcus agalactiae, Escherichia coli, Peptostreptococcus magnus, Bacteroides fragilis and Prevotella bivia, which are major pathogens in the fields of obstetrics and gynaecology. The MIC(50) and MIC(90) of S-4661 for these strains were 0.25 and 1 mg/L, respectively. The in vivo efficacy of S-4661 was evaluated in a rat model of intrauterine infection, namely pyometra caused by E. coli and B. fragilis. The accumulation of neutrophils in the uterus in the S-4661-treated group was less marked and the number of bacteria significantly lower than those in the untreated group. These results suggest that S-4661 may be useful for treating polymicrobial infections in the fields of obstetrics and gynaecology.

摘要

碳青霉烯类药物因其对厌氧菌的活性,常用于治疗妇产科感染。新型注射用碳青霉烯类抗生素S-4661具有良好的药代动力学特性,且不会被脱氢肽酶I水解。我们研究了S-4661对无乳链球菌、大肠杆菌、大消化链球菌、脆弱拟杆菌和二路普雷沃菌的体外和体内抗菌活性,这些菌株是妇产科领域的主要病原体。S-4661对这些菌株的MIC(50)和MIC(90)分别为0.25和1mg/L。在大鼠子宫内感染模型(即由大肠杆菌和脆弱拟杆菌引起的子宫积脓)中评估了S-4661的体内疗效。S-4661治疗组子宫内中性粒细胞的积聚不如未治疗组明显,且细菌数量显著低于未治疗组。这些结果表明,S-4661可能有助于治疗妇产科的混合感染。

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