Pharmacokinetic and pharmacodynamic modelling of trimazosin and its major metabolite

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Abstract
The pharmacokinetic and pharmacodynamic profiles of intravenous trimazosin, a postsynaptic α 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 (CP23445) 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.