Interaction of phenylbutazone with racemic phenprocoumon and its enantiomers in rats

Journal of Pharmacokinetics and Biopharmaceutics
W Schmidt, E Jähnchen

Abstract

The interaction of phenylbutazone with the enantiomers and racemic [3H]phenprocoumon was studied in male inbred Wistar-Lewis rats following a single i.v. dose of the three forms of phenprocoumon and chronic oral treatment with phenylbutazone (average plasma concentration of about 60 microgram/ml). Phenylbutazone augmented the anticoagulant effect of R(+), S(-), and R, S(+/-) phenprocoumon to a similar extent. The free fraction of drug in the plasma of the enantiomers and racemic phenprocoumon increased in the presence of phenylbutazone. However, the rate of elimination of total drug from plasma and liver and the distribution between liver and plasma of all three forms of phenprocoumon remained nearly unaffected by phenylbutazone. Thus there is no evidence for a stereoselective drug interaction between phenprocoumon and phenylbutazone. For racemic [oH]phenprocoumon it was possible to follow the kinetics of free drug in plasma and liver along with the time course of anticoagulant activity. In these studies, free drug concentrations in plasma and liver increased during treatment with phenylbutazone, but the elimination rate constant of free racemic phenprocoumon in plasma and liver remained essentially unchanged. Phenylbutazone ma...Continue Reading

References

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Citations

Jan 1, 1989·European Journal of Clinical Pharmacology·D TrenkE Jähnchen
Jan 1, 1981·Pharmacology & Therapeutics·L Aarons
Apr 1, 1981·British Journal of Clinical Pharmacology·E JähnchenD Trenk
Jun 1, 1988·The Journal of Pharmacy and Pharmacology·D TrenkS Oie
Feb 1, 1988·Journal of Pharmacokinetics and Biopharmaceutics·D TrenkS Oie
Apr 1, 1980·Journal of Pharmacokinetics and Biopharmaceutics·D Trenk, E Jähnchen
Dec 1, 1980·The Journal of Pharmacy and Pharmacology·D TrenkE Jähnchen

Related Concepts

Metazoa
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Rats, Laboratory

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