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Prazosin, pharmacokinetics and concentration effect.

D N Bateman, D C Hobbs, T M Twomey

    European Journal of Clinical Pharmacology
    |September 1, 1979
    PubMed
    Summary
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    This study investigated prazosin pharmacokinetics and blood pressure effects in healthy males. Prazosin showed moderate oral bioavailability, with intravenous administration yielding more pronounced hypotensive effects, especially when standing.

    Area of Science:

    • Pharmacology
    • Clinical Pharmacy
    • Cardiovascular Therapeutics

    Background:

    • Prazosin is an alpha-1 blocker used to treat hypertension.
    • Understanding its pharmacokinetic and pharmacodynamic profile is crucial for effective dosing.

    Purpose of the Study:

    • To determine the pharmacokinetics and blood pressure effects of prazosin after intravenous and oral administration.
    • To assess oral bioavailability and correlate plasma concentrations with hypotensive effects.

    Main Methods:

    • A single 1 mg dose of prazosin was administered intravenously and orally to 6 healthy male volunteers.
    • Plasma prazosin concentrations and blood pressure were monitored over time.
    • Terminal half-life, oral bioavailability, and blood pressure changes were calculated.

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    Main Results:

    • The mean terminal half-life of prazosin was 2.9 hours for both intravenous and oral routes.
    • Oral bioavailability was determined to be 56.9%.
    • Intravenous prazosin administration resulted in more pronounced blood pressure reduction compared to oral dosing, particularly in the erect position. A significant correlation was observed between decreased blood pressure and plasma drug concentration following intravenous administration.

    Conclusions:

    • Prazosin exhibits moderate oral bioavailability and a consistent elimination half-life across administration routes.
    • Intravenous administration offers a more potent hypotensive effect, highlighting the importance of route in clinical application.
    • Plasma concentration monitoring is valuable for predicting prazosin's blood pressure effects after IV administration.