[Pharmacokinetics and biotransformation of oxametacine in healthy volunteers (author's transl)].
The bisphasic time-concentration course of the total plasma activity can be ascribed to 2 metabolites--oxametacine-glucuronide and desmethylindometacinamid(DMA)-glucuronide. The rate of biotransformation for oxametacine (1-p-chlorbenzoyl-2-methyl-5-methoxy-3-indolylacethydroxamic acid) is high. In contrast to laboratory animals the metabolic degradation of the mother substance to indometacine is negligible. Oxametacine is therefore not a pro-drug for indometacine in man. The main routes of biotransformation in man are: demethylation, conjugation, with active glucuronic acid, reduction to the acid amide and debenzoylation. For the 75 mg single dose urinary recoveries of the main metabolites, DMA-glucuronide and desbenzoyldesmethylmetacinamide (DBDMA)-glucuronide are 22.9% and 9.2%, respectively. The total recovery was found to be 97.55% of the dose, this being made up of 48.49% renal and 49.06% fecal excretion.
D000328:Adult; D001711:Biotransformation; D002855:Chromatography, Thin Layer / Q000379:methods; D005260:Female; D006801:Humans; D006868:Hydrolysis; D007213:Indomethacin / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism; D007700:Kinetics; D008297:Male
C019028:oxamethacin; D007213:Indomethacin
Pharmakokinetik und Biotransformation von Oxametacin bei gesunden Probanden.