Pharmacokinetics of conventional and slow-release verapamil

British Journal of Clinical Pharmacology
F FollathF Bühler

Abstract

Verapamil is a racemic mixture of two optical isomers, the (-)-form being the more active component. Recent studies indicate a rapid hepatic transformation of (-)-verapamil, which results in different concentration-effect relationships after oral and intravenous administration. In practice the important pharmacokinetic properties of verapamil are low bioavailability (20%), predominant elimination by metabolism (greater than 95%) and a relatively short half-life (t1/2, beta is 3-5 h). After repeated dosing, the rate of hepatic drug clearance seems to decrease. Slow release (SR) formulations of verapamil may offer certain therapeutic advantages during long-term treatment. A comparison of conventional (C) and SR tablets in a 1-week treatment of eight cardiac patients showed a relative bioavailability (AUCSR/AUCC) of 90 +/- 30%. More stable serum drug levels were maintained by 12-hourly administration of SR verapamil. A further study using a new 240 mg SR preparation in patients with arterial hypertension showed that even a single daily dose can be sufficient for adequate blood pressure control over 24 h.

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Citations

Jan 1, 1989·European Journal of Clinical Pharmacology·C M JespersenJ F Hansen
Jan 29, 2003·International Journal of Pharmaceutics·Müge Kiliçarslan, Tamer Baykara
Jul 10, 2002·Clinical Pharmacokinetics·Reza MehvarMajid Vakily
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Mar 10, 1994·The New England Journal of Medicine·T F LüscherM Wenk
Sep 1, 2021·Clinical and Translational Science·Michael E ManiskasJustin F Fraser

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