Danazol has progestin-like actions on the human endometrium
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Danazol treatment significantly reduced endometrial estrogen and progestin receptor concentrations and 17 beta-hydroxysteroid dehydrogenase activity, mimicking progestin effects and suppressing luteal steroid levels.
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Abstract
The administration of danazol, 200 mg three times daily, from the 3rd to the 23rd day of the cycle to normally menstruating women exhibited the following actions on the human endometrium: significantly reduced cytosol oestrogen and progestin receptor concentrations, and declined 17 beta-hydroxysteroid dehydrogenase activity. Very similar results were obtained during medroxyprogesterone acetate (100 mg daily) treatment for the same period of time. Danazol administration did not decrease circulating gonadotrophin levels but clearly suppressed luteal serum oestradiol and progesterone concentrations. Danazol was found to bind in vitro to endometrial progestin receptor with an affinity approximately 3% of that of progesterone. These findings are compatible with the notion that a local progestin-like rather than a systemic action of danazol is the way by which its therapeutic effect is exerted. This may be potentiated by the suppression of circulating oestradiol levels.
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Cited by (31)
- Androgens Upregulate Endometrial Epithelial Progesterone Receptor Expression: Potential Implications for Endometriosis 2017
- Synthetic Steroid Hormones Regulated Cell Proliferation Through MicroRNA-34a-5p in Human Ovarian Endometrioma 2016
- Reduced expression of alphavbeta3 integrin in the endometrium of unexplained infertility patients with recurrent IVF-ET failures: improvement by danazol treatment 2003
- Today's treatments: medical, surgical and in partnership 1999
- Modern medical management of endometriosis 1997
- Effects of danazol and progesterone on sex hormone-binding globulin mRNA expression in human endometrial cancer cell line Ishikawa 1997
- Postmenopausal endometrial hyperplasia: role of danazol therapy 1994
- Action of danazol on the conversion of estrone sulfate to estradiol and on the sulfatase activity in the MCF-7, T-47D and MDA-MB-231 human mammary cancer cells 1993
- Changing concepts of medical treatment of endometriosis 1993
- Endometrial patterns during therapy with danazol or gestrinone for endometriosis: structural and ultrastructural study 1992
- Medical treatment of mild endometriosis associated with infertility 1991
- Endometrial effects of danazol in perimenopausal abnormal bleeding 1991
- Endometrial patterns during danazol and cyproterone acetate treatment for endometriosis: structural and ultrastructural study 1991
- Effects of danazol, gonadotropin-releasing hormone agonist, and a combination of danazol and gonadotropin-releasing hormone agonist on experimental endometriosis 1990
- Steroidal drugs in endometriosis 1989
- Preliminary report on the use of danazol in the treatment of endometrial adenomatous hyperplasia 1988
- Inhibitory effects of danazol and medroxyprogesterone acetate on [3H]thymidine incorporation in human endometrial cancer cells 1988
- Genital bleeding during the administration of danazol 1988
- Placebo-controlled comparison of danazol and high-dose medroxyprogesterone acetate in the treatment of endometriosis after conservative surgery 1987
- Growth inhibition by danazol in a human endometrial cancer cell line with estrogen-independent progesterone receptors 1987
- Effects of danazol on incidence of progesterone and oestrogen receptors in benign breast disease 1987
- Placebo-controlled comparison of danazol and high-dose medroxyprogesterone acetate in the treatment of endometriosis 1987
- Danazol binds to progesterone receptors and inhibits the growth of human endometrial cancer cells in vitro 1986
- Short-term effects of danazol and medroxyprogesterone acetate on cytosol and nuclear estrogen and progestin receptors, 17 beta-hydroxysteroid dehydrogenase activity, histopathology, and ultrastructure of human endometrial adenocarcinoma 1985
- Steroidal regulation of endometriosis tissue: lack of induction of 17 beta-hydroxysteroid dehydrogenase activity by progesterone, medroxyprogesterone acetate, or danazol 1985
- Serum estradiol and danazol. I. Endometriosis response, side effects, administration interval, concurrent spironolactone and dexamethasone 1985
- Cytosol estrogen and progestin receptor concentrations and 17 beta-hydroxysteroid dehydrogenase activities in the endometrium and endometriotic tissue. Effects of hormonal treatment 1984
- Short-term effects of danazol on endometrial histology 1984
- Serum estradiol and danazol. I. Endometriosis response, side effects, administration interval, concurrent spironolactone and dexamethasone 1984
- Progestin-like effects of danazol on rabbit uterus 1983
- Estrogen and progestin receptors in endometriosis lesions: comparison with endometrial tissue 1981
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