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A pharmacodynamic and pharmacokinetic assessment of a new alpha‐ adrenoceptor antagonist, doxazosin (UK33274) in normotensive subjects.
Author(s) -
Elliott HL,
Meredith PA,
Sumner DJ,
McLean K,
Reid JL
Publication year - 1982
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1982.tb01439.x
Subject(s) - doxazosin , prazosin , blood pressure , phenylephrine , heart rate , medicine , antagonist , supine position , nicardipine , mean blood pressure , anesthesia , receptor
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.