Disposition of pranolium chloride in dogs, baboons and monkeys

European Journal of Drug Metabolism and Pharmacokinetics
L AllanR F Palmer

Abstract

The general disposition of [14C]-Pranolium Chloride (SC-27761), a potential anti-arrhythmic agent, has been studied in the beagle dog, baboon and rhesus monkey. The compound was moderately absorbed from the gastro-intestinal tract of the three species at 5 mg/kg. There was appreciable inter-animal variation in the amount of absorption, and the absorption was dose-dependent in the monkey. After i.v. dosage the radioactivity was largely cleared via the kidneys. The initial elimination half-lives for Pranolium in the dog and primate were between 0.6 to 3.1 hours after i.v. dosage, but could not be determined after oral dosage. Less than 1% of the dose was localised in monkey fetal tissues, two hours after an i.v. dose was given to pregnant female rhesus monkeys, and the highest concentrations of radiolabel were detected in fetal liver. Pranolium was found to be extensively metabolised and 1-naphthol was identified as a major metabolite. Pranolium was excreted in urine both unchanged and as conjugates, but 1-naphthol was excreted largely as conjugates.

References

Jul 1, 1978·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R MehtaP Millburn
Jan 15, 1977·Biochemical Pharmacology·K Turnheim, F Lauterbach
Oct 6, 1977·Naunyn-Schmiedeberg's Archives of Pharmacology·K Turnheim, F Lauterbach
Aug 1, 1979·Clinical Pharmacology and Therapeutics·T WalleT E Gaffney

Citations

Jan 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·R C Carpenter
Jan 1, 1989·Archives of Oto-rhino-laryngology·H F Mahieu, H K Schutte

Related Concepts

Pranolium iodide, (+-)-isomer
Process of Absorption
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Cardiac Depressants
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Carbon Radioisotopes
Canis familiaris
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Macaca mulatta

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