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  • Title: Pharmacokinetics and distribution of the new antihypertensive agent pinacidil in rat, dog and man.
    Author: Eilertsen E, Hart JW, Magnussen MP, Sørensen H, Arrigoni-Martelli E.
    Journal: Xenobiotica; 1982 Mar; 12(3):177-85. PubMed ID: 7113254.
    Abstract:
    1. 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 two species, respectively. A bioavailability of 80% of unchanged pinacidil in the rat suggests a first-pass effect in this species. 2. After oral and intravenous administration of [14C]pinacidil about 85% of the radioactivity was recovered in the urine and 15% in the faeces in rats and dogs; 80-90% was excreted during the first 24 h. Autoradiographic studies in the rat showed similar distributions after oral and intravenous administration. 3. 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 bioavailability of the drug.
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