Biotransformation of tolmesoxide in animals and man.
1. The excretion and metabolism of tolmesoxide ((4,5-dimethoxy-2-methylphenyl)-methylsulphoxide) has been studied in rat, dog and man. In all species, absorption of oral doses of [14C]tolmesoxide was virtually complete and 78--99% of the 14C was excreted in the urine. 2. In bile-duct cannulated rats, excretion in bile and urine was 49% and 53% dose respectively. Metabolites of tolmesoxide in bile undergo enterohepatic circulation with final elimination by the kidneys. 3. Quantification and identification of metabolites in urine (0-24 h) were obtained by two-dimensional t.l.c. Tolmesoxide was extensively metabolized in all animal species. 4. The major routes of metabolism in rat, dog and man were oxidation to sulphones and O-demethylation followed by sulphate or glucuronide conjugation. Little or none of the urinary 14C was present as sulphide derivatives.
D000328:Adult; D000818:Animals; D001646:Bile / Q000378:metabolism; D001711:Biotransformation; D055598:Chemical Phenomena; D002621:Chemistry; D002855:Chromatography, Thin Layer; D004285:Dogs; D005243:Feces / Q000032:analysis; D005260:Female; D005965:Glucuronates / Q000378:metabolism; D006801:Humans; D008297:Male; D010084:Oxidation-Reduction; D051381:Rats; D013431:Sulfates / Q000378:metabolism; D013454:Sulfoxides / Q000378:metabolism* / Q000652:urine; D014050:Toluene / Q000031:analogs & derivatives* / Q000378:metabolism / Q000652:urine
D005965:Glucuronates; D013431:Sulfates; D013454:Sulfoxides; D014050:Toluene; C016152:tolmesoxide