Machnik M, Hegger I, Kietzmann M, Thevis M, Guddat S, Schänzer W
Institute of Biochemistry, German Sport University, Cologne, Germany.
J Vet Pharmacol Ther. 2007 Feb;30(1):86-90. doi: 10.1111/j.1365-2885.2007.00820.x.
The Federation Equestre Internationale has permitted the use of altrenogest in mares for the control of oestrus. However, altrenogest is also suspicious to misuse in competition horses for its potential anabolic effects and suppression of typical male behaviour, and thus is a controlled drug. To investigate the pharmacokinetics of altrenogest in horses we conducted an elimination study. Five oral doses of 44 mug/kg altrenogest were administered to 10 horses at a dose interval of 24 h. Following administration blood and urine samples were collected at appropriate intervals. Altrenogest concentrations were measured by liquid chromatography-tandem mass spectrometry. The plasma levels of altrenogest reached maximal concentrations of 23-75 ng/mL. Baseline values were achieved within 3 days after the final administration. Urine peak concentrations of total altrenogest ranged from 823 to 3895 ng/mL. Twelve days after the final administration concentrations were below the limit of detection (ca 2 ng/mL).
国际马术联合会已允许在母马中使用烯丙孕素以控制发情。然而，烯丙孕素因其潜在的合成代谢作用和对典型雄性行为的抑制作用，也存在被用于竞赛马匹的滥用嫌疑，因此它是一种管制药物。为了研究烯丙孕素在马体内的药代动力学，我们进行了一项消除研究。以24小时的给药间隔，给10匹马口服5次剂量为44微克/千克的烯丙孕素。给药后，在适当的间隔时间采集血液和尿液样本。通过液相色谱-串联质谱法测定烯丙孕素浓度。烯丙孕素的血浆水平达到了23 - 75纳克/毫升的最大浓度。在最后一次给药后的3天内达到基线值。总烯丙孕素的尿峰浓度范围为823至3895纳克/毫升。最后一次给药12天后，浓度低于检测限（约2纳克/毫升）。
