The persistence and effects of rimexolone in arthritic and normal rabbit knee joints.
The persistence and effects of 3H-labelled and intra-articularly administered 11 beta-hydroxy-16 alpha,17 alpha,21-trimethylpregna-1,4-diene-3,20-dione (rimexolone, [3H]-Org 6216 have been investigated in a model of fibrin-induced mono-articular arthritis in the rabbit. It appears that joint swelling is suppressed in a dose-dependent way when the drug is administered into the arthritic joint. With a dose of 15 mg the joint circumference was restored to the initial value recorded prior to antigen challenge within 14 days. Administration of rimexolone into the non-arthritic joint also suppressed contralateral arthritic joint swelling, but this effect was less pronounced and shorter lasting. Radioactivity from [3H]-rimexolone at doses of 5 or 15 mg disappears slowly from both non-arthritic and arthritic knee joints.
D000818:Animals; D001168:Arthritis / Q000188:drug therapy*; D001169:Arthritis, Experimental / Q000188:drug therapy*; D001835:Body Weight / Q000187:drug effects; D005938:Glucocorticoids / Q000494:pharmacology* / Q000627:therapeutic use; D007700:Kinetics; D007719:Knee Joint / Q000033:anatomy & histology / Q000187:drug effects*; D008297:Male; D011245:Pregnadienes / Q000494:pharmacology* / Q000627:therapeutic use; D011817:Rabbits
D005938:Glucocorticoids; D011245:Pregnadienes; C013769:rimexolone