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Clinical Trial
. 1982 May;13(5):699-703.
doi: 10.1111/j.1365-2125.1982.tb01439.x.

A pharmacodynamic and pharmacokinetic assessment of a new alpha-adrenoceptor antagonist, doxazosin (UK33274) in normotensive subjects

H L Elliott, P A Meredith, D J Sumner, K McLean, J L Reid
Clinical Trial

A pharmacodynamic and pharmacokinetic assessment of a new alpha-adrenoceptor antagonist, doxazosin (UK33274) in normotensive subjects

H L Elliott et al. Br J Clin Pharmacol. 1982 May.

Abstract

1 Doxazosin is a quinazoline derivative, related to prazosin, recently developed for the treatment of hypertension. 2 The intravenous administration of doxazosin (12 micrograms/kg) to six healthy normotensive subjects resulted in significant fall in erect blood pressure, with a corresponding increase in heart rate, but there were no significant changes in supine blood pressure or heart rate. 3 The changes in blood pressure and heart rate were maximal at 6 h after intravenous dosing. With prazosin the maximum effects occurred within the first hours. 4 Pressor response studies with phenylephrine confirmed that doxazosin is a relatively selective postsynaptic alpha-adrenoceptor antagonist. 5 The mean elimination half-life of doxazosin was 11 h. This compared with a T1/2 of 2.5 h for prazosin.

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