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Enantiomers of warfarin and vitamin K1 metabolism.
Author(s) -
Choonara IA,
Haynes BP,
Cholerton S,
Breckenridge AM,
Park BK
Publication year - 1986
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1986.tb02966.x
Subject(s) - warfarin , vitamin k epoxide reductase , metabolite , vitamin , chemistry , pharmacology , enantiomer , pharmacokinetics , anticoagulant , metabolism , prothrombin time , medicine , biochemistry , cyp2c9 , cytochrome p450 , stereochemistry , atrial fibrillation
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.