Pharmacokinetics and distribution of the new antihypertensive agent pinacidil in rat, dog and man

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Abstract
The antihypertensive agent pinacidil was rapidly, and almost completely, absorbed following oral administration of 0.5 mg/kg of the [14C]pinacidil monohydrate to rats and dogs. The half-life was about 1 and 2 h in the 2 species, respectively. A bioavailability of 80% of unchanged pinacidil in the rat suggests a 1st-pass effect in this species. After oral and i.v. administration of [14C]pinacidil about 85% of the radioactivity was recovered in the urine and 15% in the feces in rats and dogs; 80-90% was excreted during the first 24 h. Autoradiographic studies in the rat showed similar distributions after oral and i.v. administration. An oral dose of 5 or 10 mg pinacidil monohydrate was rapidly absorbed in healthy volunteers and had a pharmacokinetic profile very similar to that found in rats and dogs. Concomitant food ingestion did not change the biovailability of the drug.