Oral administration of dehydroepiandrosterone to healthy men:: Alteration of the urinary androgen profile and consequences for the detection of abuse in sport by gas chromatography mass spectrometry
Oral administration of dehydroepiandrosterone to healthy men:: Alteration of the urinary androgen profile and consequences for the detection of abuse in sport by gas chromatography mass spectrometry
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DOI：
10.1016/s0039-128x(97)00138-4
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发表时间：
1998-02-01
期刊：
影响因子：
2.7
通讯作者：
Lafarge, JP
中科院分区：
文献类型：
--
作者：
Dehennin, L;Ferry, M;Lafarge, JP
脱氢表雄酮（DHEA）替代疗法作为对DHEA和DHEA硫酸盐产生的高年龄相关性下降的补偿是一个深入研究的问题，因为许多有益的作用已经被证明。或被建议和期望。因此，运动员滥用DHEA已被国际奥委会考虑，最近禁止了该物质。由于口服补充DHEA很容易获得，我们决定研究沿着50 mg单次替代剂量给药途径对尿雄激素特征的影响。通过气相色谱-质谱法与选择离子监测的定量分析表明，该药物很容易被吸收，24小时后剂量恢复率为50 - 75%，并与DHEA，雄酮和etiocholanolone的glucuro-和磺基共轭物作为最丰富的代谢产物。与血液中发现的报告数据一致，外源性DHEA向主要生物活性雄激素睾酮的转化率较低，但通过给予氘标记的DHEA和随后的氘标记睾酮的鉴定和定量证明是真实的。建议DHEA葡萄糖醛酸苷的浓度阈值为300 μ g/L，用于筛查运动中的DHEA滥用，但单次替代剂量只能在8小时内检测到。如此短的检测期是相当大的首过肝脏代谢的结果，也是循环和尿DHEA和DHEA硫酸盐浓度的高个体间变异性的结果。(C)1998年，Elsevier Science Inc.
Dehydroepiandrosterone (DHEA) replacement therapy as compensation for high age-related decline of DHEA and DHEA sulfate production is a matter of intense investigation, since many beneficial effects have been proven. or are suggested and expected. Therefore, DHEA abuse by athletes has been considered by the International Olympic Committee, which banned the substance recently. As DHEA for oral supplementation is easily available, we decided to investigate the effect on the urinary androgen profile of administration along this route of a single substitution dose of 50 mg. Quantitative analysis by gas chromatography-mass spectrometry with selected ion monitoring demonstrated that the drug was readily absorbed with 50 to 75% recovery of dosing after 24 h, and with glucuro- and sulfoconjugates of DHEA, androsterone, and etiocholanolone as the most abundant metabolites. In agreement with reported data found in blood, conversion of exogenous DHEA to the principal biologically active androgen, testosterone, was low but proven to be real by the administration of deuterium-labeled DHEA and the subsequent identification and quantification of deuterium-labeled testosterone. A concentration threshold of 300 mu g/L of DHEA glucuronide is proposed for the screening of DHEA abuse in sport, but a single replacement dose can only be detected during 8 h. Such a short detection period is the consequence of considerable first-pass hepatic metabolism and also of the high interindividual variability of circulating and urinary DHEA and DHEA sulfate concentrations. (C) 1998 by Elsevier Science Inc.