Premium
Interruption of the enterohepatic circulation of phenprocoumon by cholestyramine
Author(s) -
Meinertz Thomas,
Gilfrich Hans-Joachim,
Groth Ulrich,
Jonen Hans Georg,
Jähnchen Eberhard
Publication year - 1977
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1977216731
Subject(s) - cholestyramine , phenprocoumon , enterohepatic circulation , chemistry , pharmacokinetics , pharmacodynamics , pharmacology , medicine , biochemistry , bile acid , warfarin , cholesterol , atrial fibrillation
The effect of cholestyramine (12 gm/day divided into 3 doses) on the pharmacokinetics and pharmacodynamics of a single intravenous dose (30 mg) of phenprocoumon was studied in 6 normal subjects. Cholestyramine treatment led to an increase in the rate of elimination of phenprocoumon in all. Total clearance increased 1.5‐ to 2‐fold. The total anticoagulant effect per dose was considerably reduced during treatment with cholestyramine. Binding studies in vitro showed that phenprocoumon is strongly bound to cholestyramine and that at a given cholestyramine concentration the percentage of phenprocoumon bound remained constant over a large concentration range of phenprocoumon. The results suggest that phenprocoumon undergoes extensive enterohepatic recycling in man which can be effectively interrupted by cholestyramine.