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首页> 外文期刊>Journal of pharmacokinetics and biopharmaceutics >A double-blind study of the sedative effects of the thalidomide enantiomers in humans.
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A double-blind study of the sedative effects of the thalidomide enantiomers in humans.

机译：沙利度胺对映体对人的镇静作用的双盲研究。

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This study investigated the sedative effects of the enantiomers of thalidomide in humans. Since the enantiomers undergo chiral inversion in vivo this entailed application of suitable statistical methodology to distinguish the effects of each enantiomer in the presence of the other one. Six healthy male volunteers received single oral doses of (+)-(R)-thalidomide, (-)-(S)-thalidomide or racemic thalidomide in a double-blind study, and the results of this study were compared with those of a similar study where three subjects received (+)-(R)-thalidomide, (-)-(S)-thalidomide or placebo in a double-blind fashion. Blood samples for analysis of (+)-(R)-thalidomide and (-)-(S)-thalidomide were obtained. Prior to sampling it was noted whether the subject was awake or asleep, and his feelings of tiredness and heaviness were estimated using Borg scales. After blood sampling continuous reaction time was measured by a 10-min series of auditory signals. The concentration-effect relationships were analyzed by logistic regression techniques and Cox regression for the reaction time data. The (+)-(R)-thalidomide concentrations, but not the (-)-(S)-thalidomide concentrations, exhibited significant positive influences on all sedative effects studied (sleep, tiredness, and reaction times). In some of the analyses of reaction times the (-)-(S)-thalidomide concentrations had a significant effect in the opposite direction. The time course and intensity of sedative effect is thus influenced by which enantiomer is administered and by the kinetics of in vivo chiral inversion.
机译：这项研究调查了沙利度胺对映体对人的镇静作用。由于对映异构体在体内进行手性反转，因此需要应用适当的统计方法来区分每种对映异构体在另一种存在下的作用。在一项双盲研究中，六名健康的男性志愿者接受了单次口服（+）-（R）-沙利度胺，（-）-（S）-沙利度胺或消旋沙利度胺的口服剂量，并将该研究结果与一项类似的研究，其中三名受试者以双盲方式接受（+）-（R）-沙利度胺，（-）-（S）-沙利度胺或安慰剂。获得用于分析（+）-（R）-沙利度胺和（-）-（S）-沙利度胺的血样。在取样之前，应注意受试者是清醒还是睡着，并使用伯格量表评估他的疲倦和沉重感。采血后，通过一系列10分钟的听觉信号来测量连续反应时间。通过逻辑回归技术和Cox回归分析反应时间数据的浓度-效应关系。 （+）-（R）-沙利度胺的浓度，而不是（-）-（S）-沙利度胺的浓度，对研究的所有镇静作用（睡眠，疲倦和反应时间）均表现出显着的积极影响。在一些反应时间分析中，（-）-（S）-沙利度胺浓度在相反方向上具有显着影响。因此，镇静作用的时间过程和强度受所用对映异构体的给药方式以及体内手性转化动力学的影响。

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