PMID: 7336756Nov 1, 1981Paper

Studies on the biotransformation of indoramin in the patas monkey

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
R A Franklin, D M Pierce

Abstract

1. Studies on absorption, excretion and biotransformation of the antihypertensive agent indoramin (3-[2-(4-benzamidopiperidino)ethyl]indole hydrochloride) have been carried out in patas monkeys. 2. Absorption of the drug was extensive, as indicated by less than 8% of the dose appearing in faeces as the unchanged compound. 3. Approx. 35% of an orally administered dose of the 3H-labelled drug was recovered in urine while a similar amount was found in faeces. Urinary excretion of total 3H was mono-exponential with a half-life of 17 h. 4. Biotransformation was extensive, the unchanged drug constituting less than 4.5% of the urinary metabolites. The principal identified metabolites were a sulphate conjugate of 3-[2-(4-benzamidopiperidine)ethyl]indol-6-ol and an acid-labile conjugate of the parent drug. A minor metabolite resulting from N-dealkylation of the drug was identified as 4-benzamidopiperidine. Small amounts of 3-[2-(4-[4-hydroxybenzamido]piperidino)-ethyl]indole were found in a dichloromethane extract of acid-hydrolysed urine. 5. The faeces contained only negligible amounts of conjugated metabolites. The principal components were the indole-6-hydroxylated derivative of the parent drug with smaller amounts of the 5-hydroxyla...Continue Reading

References

Mar 1, 1978·Analytical Biochemistry·B J Morrison, R A Franklin
Jun 1, 1976·British Journal of Clinical Pharmacology·G H DraffanC T Dollery
Jan 1, 1974·Current Medical Research and Opinion·R CarballoJ Suarez
Mar 1, 1981·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R A FranklinT Ward
Aug 19, 1961·Biochimica Et Biophysica Acta·R M ACHESON, A R HANDS

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Citations

Jan 1, 1983·European Journal of Clinical Pharmacology·R A FranklinD Stevenson
Jan 1, 1984·European Journal of Clinical Pharmacology·H M NorburyS J Warrington
Dec 1, 1990·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·D M Pierce

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