Pharmacokinetic and pharmacodynamic modelling of trimazosin and its major metabolite.
The pharmacokinetic and pharmacodynamic profiles of intravenous trimazosin, a postsynaptic alpha 1 antagonist, were analyzed empirically by integrated modelling techniques. The mean terminal elimination half-life for trimazosin was 186 +/- 80 min and the mean elimination half-life of its alkyl hydroxylated metabolite (CP 23445) was 93 +/- 29 min. The placebo-corrected fall in systolic blood pressure after 5 min standing was most appropriately characterized in all subjects by a model that incorporated "effect" compartments for both parent drug and its metabolite.
D000328:Adult; D001711:Biotransformation; D001794:Blood Pressure / Q000187:drug effects; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008954:Models, Biological; D010879:Piperazines / Q000378:metabolism* / Q000494:pharmacology
D010879:Piperazines; C005185:trimazosin; C040290:1-hydroxytrimazosin