Distribution of oxametacine and its anti-inflammatory metabolites in inflamed tissues of rats.
The anti-inflammatory drug oxametacine (1-p-chlorobenzoyl-5-methoxy-2-methyl-3-indolylacetohydroxamic acid) is extensively metabolized both in laboratory animals and in man. In rats, dosed orally with 5 mg/kg [14C]-oxametacine, there is a 2.2-2.7 fold increase in radioactivity in the inflamed tissues, in the hind-paws of animals with adjuvant arthritis and in the granulomas of cotton-pellet implanted rats. The total tissue radioactivity (following two-fold extraction with methanol; recoveries being 95 +/- 3%) was distributed into the following metabolites: 34-7% oxametacine, 26-37% indomethacin, 16-46% demethylindomethacinamide, and 26-10% indomethacinamide over 2-8 h following drug administration.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism*; D001711:Biotransformation; D006099:Granuloma / Q000378:metabolism; D006614:Hindlimb / Q000378:metabolism; D007213:Indomethacin / Q000031:analogs & derivatives* / Q000378:metabolism; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D000893:Anti-Inflammatory Agents; C019028:oxamethacin; D007213:Indomethacin