Assessment of the potency of orally administered progestins in women.
The effects of at least three doses of each of five orally administered progestins on estrogen-primed, postmenopausal endometrial biochemistry and morphologic features were analyzed. The progestins tested were norethindrone, medroxyprogesterone acetate (MPA), norgestrel, dydrogesterone, and progesterone. The dose required to elicit responses similar to those seen in premenopausal, secretory endometria was assessed for each of the parameters measured, and the relative potencies were calculated. Potencies, relative to a value of 1 for norethindrone, are L norgestrel 8 (D/L norgestrel 4), MPA 0.1, dydrogesterone 0.02, and progesterone 0.002. The dose of norethindrone required to elicit secretory phase activity was about 0.35 mg/day. These values agree with published data obtained with the use of different methods (delay of menstruation in premenopausal women, endometrial histologic features of estrogen-primed, ovariectomized women).
D000284:Administration, Oral; D000328:Adult; D000367:Age Factors; D004247:DNA / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D004341:Drug Evaluation; D004394:Dydrogesterone / Q000494:pharmacology; D004717:Endometrium / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D004960:Estradiol Dehydrogenases / Q000032:analysis; D005260:Female; D006003:Glycogen / Q000378:metabolism; D006801:Humans; D007521:Isocitrate Dehydrogenase / Q000032:analysis; D008525:Medroxyprogesterone / Q000031:analogs & derivatives / Q000494:pharmacology; D017258:Medroxyprogesterone Acetate; D008593:Menopause; D008597:Menstrual Cycle / Q000187:drug effects; D008875:Middle Aged; D009640:Norethindrone / Q000494:pharmacology; D009644:Norgestrel / Q000494:pharmacology; D011374:Progesterone / Q000494:pharmacology; D045167:Progesterone Congeners / Q000008:administration & dosage / Q000494:pharmacology*; D012016:Reference Values
D045167:Progesterone Congeners; D009644:Norgestrel; D011374:Progesterone; D006003:Glycogen; D004247:DNA; D004394:Dydrogesterone; D017258:Medroxyprogesterone Acetate; D007521:Isocitrate Dehydrogenase; D004960:Estradiol Dehydrogenases; D008525:Medroxyprogesterone; D009640:Norethindrone