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磷霉素的 trometamol 盐:微生物学评价。

The trometamol salt of fosfomycin: microbiological evaluation.

作者信息

Greenwood D, Coyle S, Andrew J

出版信息

Eur Urol. 1987;13 Suppl 1:69-75. doi: 10.1159/000472866.

Abstract

The spectrum of activity of fosfomycin and its pharmacological behaviour make it an attractive candidate for the oral treatment of uncomplicated urinary tract infection. Various factors affect the antibacterial activity so that results in different culture media vary widely. The highest activity was displayed in Eugonbroth and such results correlated well with those obtained in pooled human urine. The activity was enhanced in acid conditions such as commonly exist in infected urine. Glucose-6-phosphate potentiated the activity of fosfomycin against Escherichia coli and some other bacteria when tested in Eugonbroth (but less predictably in human urine) and the potentiating effect may be necessary in order to obtain therapeutically meaningful results in susceptibility tests. Experiments in an in vitro model of the treatment of bacterial cystitis (carried out in the absence of glucose-6-phosphate) indicated that both sensitive and 'resistant' strains of E. coli respond to concentrations of fosfomycin achievable by high-dose oral therapy with the trometamol salt. Resistance did not emerge in previously sensitive strains (or in one of the 2 'resistant' strains), providing a high peak level of antibiotic was achieved.

摘要

磷霉素的抗菌谱及其药理特性使其成为口服治疗单纯性尿路感染的理想候选药物。多种因素会影响其抗菌活性,以至于在不同培养基中得到的结果差异很大。在优贡肉汤中显示出最高活性,且该结果与在混合人尿中获得的结果高度相关。在感染尿液中常见的酸性条件下,其活性会增强。在优贡肉汤中进行测试时,6-磷酸葡萄糖可增强磷霉素对大肠杆菌和其他一些细菌的活性(但在人尿中这种增强作用较难预测),为了在药敏试验中获得具有治疗意义的结果,这种增强作用可能是必要的。在细菌性膀胱炎的体外模型中进行的实验(在没有6-磷酸葡萄糖的情况下进行)表明,无论是敏感的还是“耐药的”大肠杆菌菌株,对通过高剂量口服三甲胺盐磷霉素可达到的浓度都有反应。只要达到抗生素的高峰浓度,先前敏感的菌株(或2株“耐药”菌株中的1株)就不会出现耐药性。

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