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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.

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Meredith, P.A., Kelman, A.W., Elliott, H.L. et al. Pharmacokinetic and pharmacodynamic modelling of trimazosin and its major metabolite. Journal of Pharmacokinetics and Biopharmaceutics 11, 323–335 (1983). https://doi.org/10.1007/BF01058953

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  • DOI: https://doi.org/10.1007/BF01058953

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