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Pharmacokinetics and Distribution of the New Antihypertensive Agent Pinacidil in Rat, Dog and Man

Pharmacokinetics and Distribution of the New Antihypertensive Agent Pinacidil in Rat, Dog and Man

E Eilertsen, J W Hart, M P Magnussen, H Sørensen, E Arrigoni-Martelli

Xenobiotica. 1982 Mar;12(3):177-85.

PMID: 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP85371648	Pinacidil monohydrate		85371-64-8	Price

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