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. 1986;21(Suppl 2):149S–153S. doi: 10.1111/j.1365-2125.1986.tb02864.x

Pharmacokinetics of conventional and slow-release verapamil

F Follath, H R Ha, Evelyne Schütz, F Bühler
PMCID: PMC1400738  PMID: 3756058

Abstract

1 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 (> 95%) and a relatively short half-life (t½β is 3-5 h). After repeated dosing, the rate of hepatic drug clearance seems to decrease.

2 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.

3 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.

Keywords: verapamil, slow release formulation, pharmacokinetics

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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