Summary
The metabolic fate of a new diuretic, tienilic acid, was investigated in Wistar rats, Swiss mice, Beagle dogs, and large white pigs using the14C-labelled compound. Tienilic add and its metabolites were determined in bile, urine, and plasma following intravenous and oral administration. In general, only a small amount of unmetabolized drug is excreted. Biotransformation consists of two major metabolic routes; one is reduction and the other is oxidative hydrolysis of the molecule at the level of the carbonyl group. These two routes co-exist in all species studied, but the reduction route is prominent in the dog. Mass spectrometry was used to elucidate the structure of two metabolites and confirm it for the third.
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Tienilic acid = generic name, marketed under the name of DIFLUREX (French Trademark) by the ANPHAR Laboratory, 91380 Chilly-Mazarin (France).
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Levron, J.C., Le Fur, J.M., Adnot, P. et al. Pharmacokinetic study of 2,3-dichloro 4- (2-thienyl keto14C) phenoxyacetic acid (tienilic acid) in animals. European Journal of Drug Metabolism and Pharmacokinetics 2, 107–120 (1977). https://doi.org/10.1007/BF03189295
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DOI: https://doi.org/10.1007/BF03189295