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利尿剂对兴奋剂排泄和代谢的影响。III. 乙非他明。

The influence of diuretics on the excretion and metabolism of doping agents. III. Etilamfetamine.

作者信息

Delbeke F T, Debackere M

出版信息

Arzneimittelforschung. 1986 Sep;36(9):1413-6.

PMID:3790195
Abstract

The urinary excretion of etilamfetamine (ethylamphetamine) and its major metabolite amphetamine in humans was followed over a period of several days after the oral administration of two formulations. The excretion of both substances was affected by urinary pH. Excretion peaks were observed 3-4 h after the ingestion of etilamfetamine in a capsule and the proportion of etilamfetamine excreted during 72 h was 22.2 to 54.4%. Excepting a shift in the peak excretion time to 4-5 h, no meaningful pharmacokinetic differences were found when Apetinil-Depot, a retard formulation, was administered. The intake of acetozolamide shortly after etilamfetamine resulted in a decrease of the etilamfetamine excretion during one day and a suppression below the detection limit for periods varying from 2-7 h post-dosing. Although the etilamfetamine excretion was suppressed from 2 to at least 10 h post-dosing, the action of the diuretic clofenamide on the etilamfetamine excretion is generally not so obvious as that of acetazolamide. The administration of furosemide only reduced the etilamfetamine concentrations by a factor of 4 to 5 during a 2-h period.

摘要

在口服两种制剂后的几天时间里,对人体中乙非他明(乙基苯丙胺)及其主要代谢物苯丙胺的尿排泄情况进行了跟踪研究。两种物质的排泄均受尿液pH值影响。在摄入胶囊装乙非他明后3 - 4小时观察到排泄峰值,72小时内排泄的乙非他明比例为22.2%至54.4%。当服用缓释制剂阿佩替尼长效注射剂时,除排泄峰值时间推迟至4 - 5小时外,未发现有意义的药代动力学差异。在乙非他明服用后不久摄入乙酰唑胺,导致乙非他明在一天内排泄量减少,且在给药后2 - 7小时内低于检测限。尽管乙非他明排泄在给药后2至至少10小时受到抑制,但利尿剂氯苯甲酰胺对乙非他明排泄的作用通常不如乙酰唑胺明显。服用呋塞米仅在2小时内使乙非他明浓度降低了4至5倍。

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