Summary
The metabolic fate of fluvoxamine maleate in man was investigated. The metabolites were isolated from the pooled urines of healthy volunteers who had ingested either 5 mg radioactive, or 100 mg non-radioactive fluvoxamine maleate as a single dose. The main isolation methods were solvent extraction, column and thin-layer chromatography.
Eleven metabolites were isolated; eight of these were carboxylic acids. Identification of nine metabolites was accomplished by mass spectrometry supported by information from the UV spectra and the ionogenic properties. The main route of metabolic degradation of fluvoxamine begins with oxidative elimination of the methoxyl group, another route with removal of the primary amino group.
In view of the nature of the degradation pattern none of the metabolites is likely to possess psychotropic activity. For the two primary metabolites this has, in effect, been demonstrated.
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References
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Overmars, H., Scherpenisse, P.M. & Post, L.C. Fluvoxamine maleate: metabolism in man. European Journal of Drug Metabolism and Pharmacokinetics 8, 269–280 (1983). https://doi.org/10.1007/BF03188757
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DOI: https://doi.org/10.1007/BF03188757