Institute for Medical Research and Education, Essen, Germany.
Maturitas. 2009 Dec;65 Suppl 1:S3-11. doi: 10.1016/j.maturitas.2009.10.011. Epub 2009 Dec 6.
Dydrogesterone has a molecular structure closely related to that of natural progesterone, but it has enhanced oral availability compared with progesterone. The hormonal profile and the progestational potency of dydrogesterone has been determined in vitro, in vivo and in humans, in combination with estrogens or without. It showed varying affinity for progesterone-binding proteins in uterine tissue in vitro, depending on the species. It exerted a clear progestational response in the rabbit in vivo, although the potency was influenced somewhat by the route of administration. When used in hormone replacement therapy, 10mg dydrogesterone given sequentially provides adequate protection against endometrial hyperplasia in postmenopausal women using 2mg estradiol. Similarly, a dydrogesterone dose of 5mg also protects the endometrium when continuously combined with 1mg estradiol. Dydrogesterone also has beneficial effects in women with amenorrhea/oligomenorrhea, dysfunctional uterine bleeding and irregular cycles. In conclusion, having a similar profile to progesterone but with better oral availability, dydrogesterone has been used successfully to treat disorders related to absolute or relative progesterone deficiency.
地屈孕酮的分子结构与天然孕酮非常相似，但与孕酮相比，其口服生物利用度更高。地屈孕酮的激素谱和孕激素效价已在体外、体内和人体中得到确定，可与雌激素联合使用或不联合使用。它在体外对子宫组织中的孕激素结合蛋白表现出不同的亲和力，具体取决于物种。它在体内对兔有明显的孕激素反应，尽管效力在一定程度上受到给药途径的影响。在激素替代治疗中，10mg 地屈孕酮序贯给药，与 2mg 雌二醇联合使用可充分预防绝经后妇女的子宫内膜增生。同样，当与 1mg 雌二醇连续联合使用时，5mg 的地屈孕酮剂量也可保护子宫内膜。地屈孕酮对闭经/稀发排卵、功能失调性子宫出血和不规则周期的妇女也有有益的作用。总之，地屈孕酮具有与孕酮相似的作用模式，但口服生物利用度更好，已成功用于治疗与绝对或相对孕激素缺乏相关的疾病。
