Short-term effects of danazol and medroxyprogesterone acetate on cytosol and nuclear estrogen and progestin receptors, 17β-hydroxysteroid dehydrogenase activity, histopathology, and ultrastructure of human endometrial adenocarcinoma

1985 ◽  
Vol 35 (2) ◽  
pp. 157-163 ◽  
Author(s):  
Anti Kauppila ◽  
Hannu Isotalo ◽  
Seppo Kivinen ◽  
Frej Stenbäck ◽  
Reijo Vihko
Keyword(s):  
Dehydrogenase Activity ◽  
Medroxyprogesterone Acetate ◽  
Endometrial Adenocarcinoma ◽  
Hydroxysteroid Dehydrogenase ◽  
Short Term ◽  
Progestin Receptors ◽  
Short Term Effects

Danazol has progestin-like actions on the human endometrium

1982 ◽  
Vol 99 (4) ◽  
pp. 588-593 ◽  
Author(s):  
E. Kokko ◽  
O. Jänne ◽  
A. Kauppila ◽  
L. Rönnberg ◽  
R. Vihko
Keyword(s):  
Dehydrogenase Activity ◽  
Therapeutic Effect ◽  
Medroxyprogesterone Acetate ◽  
Hydroxysteroid Dehydrogenase ◽  
Human Endometrium ◽  
Daily Treatment ◽  
Systemic Action ◽  
Progestin Receptor ◽  
Menstruating Women

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 17β-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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