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头孢噻肟和去乙酰头孢噻肟在人脑脓肿中的渗透情况。

Penetration of cefotaxime and desacetylcefotaxime into brain abscesses in humans.

作者信息

Sjölin J, Eriksson N, Arneborn P, Cars O

机构信息

Department of Infectious Diseases, University Hospital, Uppsala, Sweden.

出版信息

Antimicrob Agents Chemother. 1991 Dec;35(12):2606-10. doi: 10.1128/AAC.35.12.2606.

Abstract

Since clinical trials comparing the efficacies of different antibiotic regimens for treatment of brain abscesses are difficult to perform, the choice of antibiotics must rely on the antibacterial spectrum and the ability of the drug to penetrate into the abscess fluid. The aim of this investigation was to study the ability of cefotaxime and its active metabolite desacetylcefotaxime to penetrate into brain abscesses. Eight patients were given 3 g of cefotaxime intravenously every 8 h. Abscess fluid samples, obtained at surgery at various times after dosing, and blood samples were analyzed for their concentrations of cefotaxime and desacetylcefotaxime by using a newly developed microbiological assay. The brain abscess concentrations of cefotaxime and desacetylcefotaxime were 1.9 +/- 1.7 and 4.0 +/- 2.2 mg/liter, respectively. Simultaneous concentrations in plasma were 2.0 +/- 1.0 and 3.9 +/- 1.8 mg/liter, respectively. With increasing time following cefotaxime dosing there was a significant increase in the abscess:plasma concentration ratio of desacetylcefotaxime. Since both cefotaxime and desacetylcefotaxime penetrate well into the brain abscess, reaching concentrations above the MIC for probable bacteria except gram-negative anaerobes, it is concluded that cefotaxime in combination with metronidazole may be used as an alternative in the treatment of brain abscesses.

摘要

由于比较不同抗生素治疗脑脓肿疗效的临床试验难以开展,抗生素的选择必须依赖于抗菌谱以及药物渗透至脓肿液的能力。本研究的目的是研究头孢噻肟及其活性代谢产物去乙酰头孢噻肟渗透至脑脓肿的能力。8例患者每8小时静脉注射3g头孢噻肟。利用新开发的微生物测定法分析给药后不同时间手术获取的脓肿液样本和血样中头孢噻肟和去乙酰头孢噻肟的浓度。头孢噻肟和去乙酰头孢噻肟在脑脓肿中的浓度分别为1.9±1.7mg/L和4.0±2.2mg/L。同时血浆中的浓度分别为2.0±1.0mg/L和3.9±1.8mg/L。随着头孢噻肟给药时间的延长,去乙酰头孢噻肟的脓肿:血浆浓度比显著升高。由于头孢噻肟和去乙酰头孢噻肟均能很好地渗透至脑脓肿,除革兰氏阴性厌氧菌外,达到的浓度高于可能存在细菌的最低抑菌浓度,因此得出结论,头孢噻肟联合甲硝唑可作为治疗脑脓肿的替代方案。

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