华法林对映体与维生素K1代谢
Enantiomers of warfarin and vitamin K1 metabolism.
作者信息
Choonara I A, Haynes B P, Cholerton S, Breckenridge A M, Park B K
出版信息
Br J Clin Pharmacol. 1986 Dec;22(6):729-32. doi: 10.1111/j.1365-2125.1986.tb02966.x.
Abstract
The effect of the individual enantiomers of warfarin at steady state (1 mg daily) was investigated in five healthy volunteers. Both enantiomers produced a significant increase in prothrombin time, but the increase with S warfarin (1.8 +/- 0.8 s, mean +/- s.d.) was greater than with R warfarin (1.0 +/- 0.3 s), despite lower steady state plasma concentrations of S warfarin, due to its more rapid clearance. Following the administration of vitamin K1, the maximum plasma concentration and area under the plasma concentration time curve values for the metabolite vitamin K1 2,3-epoxide were greater after S warfarin than after R warfarin. The greater anticoagulant potency of S warfarin is reflected by a greater degree of inhibition of vitamin K1 epoxide reductase.
摘要
在五名健康志愿者中研究了华法林对映体在稳态（每日1毫克）时的作用。两种对映体均使凝血酶原时间显著延长，但S-华法林（1.8±0.8秒，平均值±标准差）导致的延长幅度大于R-华法林（1.0±0.3秒），尽管S-华法林的稳态血浆浓度较低，这是由于其清除速度更快。给予维生素K1后，S-华法林代谢产物维生素K1 2,3-环氧化物的最大血浆浓度和血浆浓度-时间曲线下面积值高于R-华法林。S-华法林更强的抗凝效力表现为对维生素K1环氧化物还原酶的抑制程度更高。
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本文引用的文献
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