PMID: 7336958May 1, 1981Paper

Metabolism of femoxetine

Acta Pharmacologica Et Toxicologica
H Larsson, J Lund

Abstract

The metabolism of femoxetine, a serotonin uptake inhibitor, has been investigated in rats, dogs, monkeys, and human subjects using two 14C-femoxetine compounds with labelling in different positions. The metabolic pathways were oxidation (and glucuronidation) and demethylation, both reactions most probably taking place in the liver. Nearly all femoxetine was metabolised, and the same metabolites were found in urine from all four species. Only a small percentage of the radioactivity excreted in the urine was not identified. Rat and dog excreted more N-oxide than monkey and man, while most of the radioactivity (60-100%) in these two species was excreted as two hydroxy metabolites. The metabolic pattern in monkey and man was very similar. About 50% was excreted in these two species as one metabolite, formed by demethylation of a methoxy group. A demethylation of a N-CH3 group formed an active metabolite, norfemoxetine. The excretion of this metabolite in urine from man varied from 0 to 18% of the dose between individuals. Most of the radioactivity was excreted with the faeces in rat and dog, while monkey and man excreted most of the radioactivity in urine. This difference in excretion route might be explained by the difference in t...Continue Reading

References

Mar 1, 1979·Acta Pharmacologica Et Toxicologica·J LundH Larsson
Jan 1, 1977·Clinical Toxicology·A Stolman, P A Pranitis
May 1, 1975·European Journal of Pharmacology·J B LassenS O Olsson
Nov 1, 1969·Clinical Pharmacology and Therapeutics·F SjöqvistC Thorstrand

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Citations

Jan 1, 1985·European Journal of Clinical Pharmacology·C Strömberg, M J Mattila
Jan 1, 1986·European Journal of Clinical Pharmacology·J SchmidtH Mengel

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