Summary
Pinacidil is a new vasodilating agent. Previous studies have shown that the effect on blood pressure is related to the serum concentration. This study compared a sustained release tablet with a controlled release capsule formulation developed to extend the duration of the antihypertensive effect. 12 patients with severe essential hypertension requiring basic therapy with a diuretic, a β-adrenoceptor blocker and pinacidil participated in this randomised crossover study. All patients had received pinacidil at a constant dosage for more than 6 months. When the same dose was given, the capsule formulation gave a lower peak serum concentration of pinacidil and pinacidil N-oxide compared with the tablet formulation. The maximum serum concentration (Cmax) was more extended, with a Cmax/2 of 9.5 hours after the capsule compared with 6 hours after the tablet. Neither formulation lowered blood pressure in any patient for 12 hours. Thus, if blood pressure reduction is considered essential during the whole dose interval, twice-daily administration of the capsule formulation is not sufficient.
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Carlsen, J.E., Køber, L. & Rehling, M. Pharmacokinetic and Pharmacodynamic Evaluation of Two Different Oral Formulations of Pinacidil, a Potassium Channel Opener. Drug Invest. 3, 336–340 (1991). https://doi.org/10.1007/BF03259749
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DOI: https://doi.org/10.1007/BF03259749