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甲氧苄啶-磺胺甲恶唑对敏感和耐多药结核分枝杆菌的细胞内和细胞外活性。

Intra- and extracellular activities of trimethoprim-sulfamethoxazole against susceptible and multidrug-resistant Mycobacterium tuberculosis.

作者信息

Davies Forsman L, Schön T, Simonsson U S H, Bruchfeld J, Larsson M, Juréen P, Sturegård E, Giske C G, Ängeby K

机构信息

Unit of Infectious Diseases, Department of Medicine Solna, Karolinska Institutet, Stockholm, Sweden Department of Infectious Diseases, Karolinska University Hospital Solna, Stockholm, Sweden

Department of Medical Microbiology, Linköping University Hospital, Linköping, Sweden Department of Medicine and Optometry, Linnaeus University, Kalmar, Sweden.

出版信息

Antimicrob Agents Chemother. 2014 Dec;58(12):7557-9. doi: 10.1128/AAC.02995-14. Epub 2014 Sep 22.

Abstract

We investigated the activity of trimethoprim-sulfamethoxazole (SXT) against Mycobacterium tuberculosis, the pathogen that causes tuberculosis (TB). The MIC distribution of SXT was 0.125/2.4 to 2/38 mg/liter for the 100 isolates tested, including multi- and extensively drug-resistant isolates (MDR/XDR-TB), whereas the intracellular MIC90 of sulfamethoxazole (SMX) for the pansusceptible strain H37Rv was 76 mg/liter. In an exploratory analysis using a ratio of the unbound area under the concentration-time curve from 0 to 24 h over MIC (fAUC0-24/MIC) using ≥ 25 as a potential target, the cumulative fraction response was ≥ 90% at doses of ≥ 2,400 mg of SMX. SXT is a potential treatment option for MDR/XDR-TB.

摘要

我们研究了甲氧苄啶-磺胺甲恶唑(SXT)对引起结核病(TB)的病原体结核分枝杆菌的活性。对于所测试的100株分离菌,包括耐多药和广泛耐药分离株(MDR/XDR-TB),SXT的MIC分布为0.125/2.4至2/38毫克/升,而对全敏感菌株H37Rv,磺胺甲恶唑(SMX)的细胞内MIC90为76毫克/升。在一项探索性分析中,使用0至24小时浓度-时间曲线下未结合面积与MIC的比值(fAUC0-24/MIC),以≥25作为潜在靶点,在SMX剂量≥2400毫克时,累积分数反应≥90%。SXT是MDR/XDR-TB的一种潜在治疗选择。

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