Kokko E, Jänne O, Kauppila A, Rönnberg L, Vihko R
Acta Endocrinol (Copenh). 1982 Apr;99(4):588-93. doi: 10.1530/acta.0.0990588.
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.
对正常月经周期的女性，在月经周期第3天至第23天每天3次给予200mg达那唑，该药对人子宫内膜有以下作用：显著降低胞质雌激素和孕激素受体浓度，并使17β-羟类固醇脱氢酶活性下降。在相同时间段给予醋酸甲羟孕酮（每日100mg）治疗时也获得了非常相似的结果。给予达那唑并未降低循环促性腺激素水平，但明显抑制黄体期血清雌二醇和孕酮浓度。发现达那唑在体外与子宫内膜孕激素受体结合，其亲和力约为孕酮的3%。这些发现与以下观点相符，即达那唑发挥治疗作用的方式是通过局部孕激素样作用而非全身作用，循环雌二醇水平的抑制可能会增强这种作用。
