Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: Aurogen South Africa (Pty) Ltd, Woodhill Office Park, Building 1, 53 Phillip Engelbrecht Avenue, Meyersdal, Ext. 12, 1448, Johannesburg, South Africa
A.7.1 Vasodilators, hypotensive medicines
Doxazosin exerts a vasodilator effect via selective and competitive blockade of post-junctional alpha-1-adrenoceptors. Doxazosin has been shown to block the 1A subtype of the alpha-1-adrenoceptor which accounts for over 70% of the subtypes in the prostate.
Doxazosin is well absorbed after oral administration, with peak blood levels occurring at about 2 hours. The plasma elimination is biphasic with the terminal elimination half-life being 19 to 22 hours, hence providing the basis for once daily dosing. Doxazosin is extensively metabolised with less than 5% excreted unchanged.
Maximum reduction in blood pressure normally occurs about 6 hours after dosing.
Most (98%) of plasma doxazosin is protein bound. In vitro data in human plasma indicates that doxazosin has no effect on protein binding of the medicines tested (digoxin, phenytoin, warfarin or indomethacin)
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