The in vivo glucocorticoid and antiglucocorticoid actions of medroxyprogesterone acetate.
The in vivo glucocorticoid actions of medroxyprogesterone acetate [6 alpha-methyl-17-acetoxy-pregn-4-ene-3,20-dione (MPA)] were assessed in intact prepubertal female Wistar rats using five simultaneous assays: plasma glucose, plasma corticosterone, hepatic glycogen content, hepatic tyrosine aminotransferase activity, and croton oil-induced ear inflammation. Antiglucocorticoid acitivity was measured through interference by MPA with the glucocorticoid effect of a standard 5-microgram dose of dexamethasone in these same assays. The glucocorticoid activity of MPA was evident from suppression of corticosterone and ear inflammation and stimulation of tyrosine aminotransferase activity. The antiglucocorticoid activity of MPA was detected through inhibition of basal and dexamethasone-stimulated hepatic glycogen and partial reversal of the suppression of ear inflammation by dexamethasone. The progestational steroid MPA was thus found to have assay-specific glucocorticoid and antiglucocorticoid actions and may have a potential use in the treatment of some states of glucocorticoid excess.
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism*; D003345:Corticosterone / Q000097:blood*; D003436:Croton Oil / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D005260:Female; D005938:Glucocorticoids / Q000037:antagonists & inhibitors*; D006003:Glycogen / Q000378:metabolism; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008525:Medroxyprogesterone / Q000494:pharmacology*; D010031:Otitis / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D014444:Tyrosine Transaminase / Q000378:metabolism
D001786:Blood Glucose; D005938:Glucocorticoids; D003907:Dexamethasone; D003436:Croton Oil; D006003:Glycogen; D014444:Tyrosine Transaminase; D008525:Medroxyprogesterone; D003345:Corticosterone