Demonstration of stereoselective disposition of warfarin enantiomers by whole-body autoradiography

The oral anticoagulant warfarin and its 14C-labelled derivative are commercially available in racemic forms. Two methods for the chromatographic resolution of the radiolabel were used to investigate the distribution of radioactivity of radioactivity of individual enantiomers in the rat by whole-body...

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Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 1990-04, Vol.15 (2), p.103-107
Main Authors: SZINAI, I, SIMONYI, M, FITOS, I, TEGYEY, Z, MAGYAR, A
Format: Article
Language:English
Subjects:
Animals
Autoradiography
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Carbon Radioisotopes
Humans
Male
Medical sciences
Pharmacology. Drug treatments
Rats
Rats, Inbred Strains
Stereoisomerism
Time Factors
Tissue Distribution
Warfarin - pharmacokinetics
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Summary:The oral anticoagulant warfarin and its 14C-labelled derivative are commercially available in racemic forms. Two methods for the chromatographic resolution of the radiolabel were used to investigate the distribution of radioactivity of radioactivity of individual enantiomers in the rat by whole-body autoradiography. Computer-assisted quantification of autoradiograms indicated the average disappearance of levo-warfarin and its metabolites to be substantially slower than that of dextro-warfarin and its metabolites from the following organs: liver, pancreas, kidney, lung, blood, intestines.
ISSN:0378-7966
2107-0180
DOI:10.1007/BF03190193