Kinetics of [3H]trifluoperazine in bile fistula rats.
1. Anaesthetized male rats with a bile fistula received 12-3 micron mol/kg [9-3H]tri-fluoperazine into the tail vein, and the biliary excretion of total radioactivity, unchanged drug and phenolic glucuronides was followed for 8 h. 2. About half of the administered radioactivity apeared in bile within 8 h;80% of the biliary metabolites were unextractable even after beta-glucuronidasearylsulphatase hydrolysis; about 10% were glucuronides of 7-hydroxytrifluoperazine and its N-demethylated analogue; approx. 0-6% of the excreted radioactivity was unchanged drug. 3. A more rapid excretion, but a similar metabolite pattern, was observed when the drug was administered into the portal vein and bile was collected for 2 h. 4. Rats pre-treated with trifluoperazine per os for 3 weeks and then given the radioactive dose into the tail vein excreted increased quantities of the demethylated phenol glucuronide, while the other metabolities remained unchanged.
D000818:Animals; D001646:Bile / Q000378:metabolism*; D001659:Biliary Tract / Q000502:physiology; D001662:Biliary Tract Surgical Procedures; D005402:Fistula; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D011169:Portal Vein; D051381:Rats; D013623:Tail / Q000098:blood supply; D013997:Time Factors; D014018:Tissue Distribution; D014268:Trifluoperazine / Q000008:administration & dosage / Q000378:metabolism*
D014268:Trifluoperazine