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利尿剂对兴奋剂排泄和代谢的影响——Ⅴ. 二甲弗林

The influence of diuretics on the excretion and metabolism of doping agents--V. Dimefline.

作者信息

Delbeke F T, Debackere M

机构信息

Laboratorium voor Farmacologie en Toxicologie der Huisdieren, Faculteit Diergeneeskunde, Rijksuniversiteit Gent, Belgium.

出版信息

J Pharm Biomed Anal. 1991;9(1):23-8. doi: 10.1016/0731-7085(91)80232-x.

Abstract

A sensitive method for the quantitative determination of the respiratory stimulant dimefline in 5 ml urine using capillary gas chromatography with nitrogen specific detection is presented. After the oral administration of a therapeutical amount of 16 mg dimefline to five subjects only 0.26 +/- 0.16% of the dose is excreted as the conjugated drug in 24 h. The maximum excretion rate occurred 3 h after dosing, the peak concentration being 154 +/- 60 ng ml-1. The influence of diuretics taken 2 h after the administration of dimefline was studied in three subjects. From these results it appeared that the use of acetazolamide and hydrochlorthiazide in order to circumvent a positive dimefline doping case is questionable. Due to the potent diuretic effect of furosemide, the intake of this diuretic could result in a suppression of the dimefline concentration below the detection limit of 10 ng ml-1.

摘要

本文介绍了一种采用带氮特异性检测的毛细管气相色谱法定量测定5ml尿液中呼吸兴奋剂二甲弗林的灵敏方法。对5名受试者口服治疗剂量16mg的二甲弗林后,仅0.26±0.16%的剂量在24小时内以结合药物形式排泄。给药后3小时出现最大排泄率,峰值浓度为154±60ng/ml。在3名受试者中研究了二甲弗林给药2小时后服用利尿剂的影响。从这些结果来看,为规避二甲弗林阳性兴奋剂检测案例而使用乙酰唑胺和氢氯噻嗪的做法值得怀疑。由于呋塞米的强效利尿作用,服用这种利尿剂可能会导致二甲弗林浓度低于10ng/ml的检测限。

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