Levy G, O'Reilly R A, Wingard L B
J Pharm Sci. 1978 Jun;67(6):867-8. doi: 10.1002/jps.2600670640.
The elimination kinetics and anticoagulant effect produced by single 1.5-mg/kg doses of (R)-(+(-, (S)-(--)-, and racemic warfarin were determined in 10 healthy men. The results obtained in experiments with the individual enantiomers were used to predict the elimination kinetics and anticoagulant effect of racemic warfarin, assuming that there is no interaction between the two enantiomers. These predictions were compared to experimental results, and no significant differences were observed. This finding suggests that there are no pronounced pharmacokinetic or pharmacodynamic interactions between single large doses of (R)-(+)- and (S)-(--)-warfarin in humans.
在10名健康男性中测定了单剂量1.5毫克/千克的(R)-(+)-、(S)-(-)-和消旋华法林的消除动力学及抗凝效果。在使用单一对映体的实验中获得的结果被用于预测消旋华法林的消除动力学及抗凝效果,假设两种对映体之间不存在相互作用。将这些预测结果与实验结果进行比较,未观察到显著差异。这一发现表明,在人类中,单一大剂量的(R)-(+)-和(S)-(-)-华法林之间不存在明显的药代动力学或药效学相互作用。