Antiinflammatory activity and other pharmacological properties of 11 beta, 21-dihydroxy-2'-methyl-5' beta H-pregna-1,4 dieno[17,16-d] oxazole 3,20-dione-21-acetate (Deflazacort).

The pharmacology of 11 alpha, 21-dihydroxy-2'-methyl-5' beta H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione-21-acetate (deflazacort) was studied by oral and parenteral administration in acute, short- and long-term experiments in rats. Deflazacort has antiinflammatory activity in various laboratory models, such as carrageenin and nystatin oedema, cotton pellet granuloma, adjuvant arthritis and on liver glycogen storage. The antiinflammatory potency of deflazacort is greater than that of prednisolone, but lower than that of dexamethasone. Absorption from the gut and duration of action appear to be highly satisfactory, as deduced from pharmacological and biochemical measurements. Glucose tolerance curves seem less affected by deflazacort than by prednisolone, while cardiovascular and central nervous system findings do not show unexpected responses.