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Absorption, metabolism and excretion of14C-sultopride in the rat

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Summary

Rats received (14C)-Sultopride (St) in doses of 20 mgAg by ip. and oral route. After ip.-administration, urinary elimination was 62% of administered dose in 72 hours, fecal excretion, 25% in 96 hours. Conversely, at 120 hours after oral administration, renal elimination was 46% and fecal elimination 34%. From these data 75% absorption of St in rat intestine may be deduced. From total excreted radioactivity (feces plus urine; ip. route) 35% is due to unchanged St. Seven metabolites were isolated from the urine. By comparison of isolated compounds with chemically synthesized putative metabolites using spectrophotometric and radiometric TLC scanning procedures 5 metabolites were identified: O-desmethylated St (DMSt; 20% of total radioactivity excreted), sulfon-desethylated St (SDESt; 13%), 5-pyrrolidine-oxo St (OSt; 3%), the product of hydrolysis of the central amide bond (MESS; 4%) and the secondary metabolite O-desmethyl-oxo St (ODMST; less than 1%). Two metabolites both minor (1% or less), remained unidentified. In guinea-pigs, metabolism of St leadsalmost exclusively to OSt while in mice, to DMSt.

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  1. C. und O. Vogt-Institut für Hirnforschung der Universität Düsseldorf, Moorenstrasse 5, D-4000, Düsseldorf 1, FRG

    Karl Dross, Peter Sillmann & Jonny Küster

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  1. Karl Dross
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  2. Peter Sillmann
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  3. Jonny Küster
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Dross, K., Sillmann, P. & Küster, J. Absorption, metabolism and excretion of14C-sultopride in the rat. European Journal of Drug Metabolism and Pharmacokinetics 9, 1–9 (1984). https://doi.org/10.1007/BF03189600

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  • DOI: https://doi.org/10.1007/BF03189600

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