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Bethanidine dose, plasma levels, and antihypertensive effects.

C N Corder

    Journal of Clinical Pharmacology
    |May 1, 1978
    PubMed
    Summary

    This study found that bethanidine effectively lowers blood pressure in hypertensive patients, with plasma levels correlating to dosage. Recommendations are provided for its safe and effective use in antihypertensive therapy.

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    Area of Science:

    • Pharmacology
    • Cardiovascular Medicine
    • Clinical Therapeutics

    Background:

    • Hypertension remains a significant global health concern requiring effective pharmacologic management.
    • Bethanidine is an antihypertensive agent whose dose-response relationship and pharmacokinetic profile require further elucidation.

    Purpose of the Study:

    • To evaluate the relationship between bethanidine dosage, plasma concentrations, and its hypotensive effects in hypertensive patients.
    • To assess the pharmacokinetic profile of bethanidine, including its elimination half-time.
    • To provide recommendations for initiating and maintaining antihypertensive therapy with bethanidine.

    Main Methods:

    • A study involving twelve hypertensive patients receiving concurrent diuretic therapy with benzthiazide.
    • Administration of bethanidine three times daily for a duration of two to twelve months.
    • Measurement of standing diastolic blood pressure, plasma bethanidine levels, and observation of withdrawal effects.

    Main Results:

    • Significant reduction in mean standing diastolic pressure from 112 to 91 mm Hg observed in 11 patients.
    • Mean total daily bethanidine dose was 79 mg, with plasma levels correlating to the dose (mean 0.65 µM).
    • A weaker correlation was noted between bethanidine dose and antihypertensive effect; withdrawal effects resolved within 12 hours, while plasma elimination half-time was 39 hours.

    Conclusions:

    • Bethanidine demonstrates efficacy in reducing blood pressure in hypertensive patients, particularly when used concurrently with diuretics.
    • Plasma bethanidine concentrations correlate with administered dosage, aiding in therapeutic monitoring.
    • Established pharmacokinetic data and observed clinical effects inform practical recommendations for bethanidine therapy initiation and maintenance.

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