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磷霉素氨丁三醇盐给药后磷霉素在下尿路中的分布。

Fosfomycin distribution in the lower urinary tract after administration of fosfomycin trometamol salt.

作者信息

Scaglione F, Cicchetti F, Demartini G, Arcidiacono M

机构信息

Department of Pharmacology, University of Milan, Bassini Hospital, Italy.

出版信息

Int J Clin Pharmacol Res. 1994;14(3):107-9.

PMID:7883387
Abstract

Fosfomycin trometamol (FT) is a new fosfomycin salt with pharmacokinetic characteristics allowing hypothesis of its use in the single-dose therapy of lower urinary tract infections. In this study the diffusion of fosfomycin into bladder mucosa and urine after administration of a single oral dose of FT (3 g) was evaluated in patients affected by bladder or prostatic carcinoma having to undergo surgery. The administration of FT was scheduled in order to obtain blood, urine and tissue samples, to be collected during surgical operation at different times post administration. The peak concentrations in serum and bladder mucosa were detected within 3 h and 6 h respectively. Fosfomycin concentrations in bladder mucosa proved to be higher than the MICs of the most common urinary tract pathogens for at least 36 h. In urine, fosfomycin reached concentrations markedly higher than those found in serum and bladder mucosa, antibacterial levels lasting until the 48th hour post dosing. Fosfomycin trometamol, because of its pharmacokinetic and pharmacodynamic properties, appears to be suitable for single-dose therapy of uncomplicated UTIs.

摘要

磷霉素氨丁三醇(FT)是一种新型磷霉素盐,其药代动力学特性使其有可能用于下尿路感染的单剂量治疗。在本研究中,对患有膀胱癌或前列腺癌且需接受手术的患者,评估了单次口服3克FT后磷霉素在膀胱黏膜和尿液中的扩散情况。FT的给药时间经过安排,以便在给药后的不同时间点手术过程中采集血液、尿液和组织样本。血清和膀胱黏膜中的峰值浓度分别在3小时和6小时内检测到。膀胱黏膜中的磷霉素浓度被证明至少在36小时内高于最常见尿路病原体的最低抑菌浓度(MIC)。在尿液中,磷霉素达到的浓度明显高于血清和膀胱黏膜中的浓度,抗菌水平持续到给药后48小时。由于其药代动力学和药效学特性,磷霉素氨丁三醇似乎适用于单纯性尿路感染的单剂量治疗。

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