New progestogens: a review of their effects in perimenopausal and postmenopausal women.

摘要: The progestins have different pharmacological properties depending upon the parent molecule, usually testosterone or progesterone, from which they are derived. Very small structural changes in molecule may induce considerable differences activity of derivative. In postmenopausal women with an intact uterus, used combination estrogen as hormone-replacement therapy (HRT). development new generations improved selectivity profiles has been a great challenge. Steroidal and nonsteroidal progesterone-receptor (PR) agonists synthesised well, although latter still very early stage development. Several progestins, last 2 decades, be considered fourth-generation progestins. These include dienogest, drospirenone, Nestorone (Population Council, New York, NY, USA), nomegestrol acetate trimegestone. designed to no androgenic estrogenic actions closer physiological hormone progesterone. Drospirenone differs classic it is derived spirolactone. It essentially antimineralocorticoid steroid effect but partial antiandrogenic effect. antiovulatory potency varies. Trimegestone most potent date, followed by two older 3-keto-desogestrel levonorgestrel. molecules trimegestone, drospirenone dienogest also activity. Following publication results Women's Health Initiative study, role HRT became controversial. Unfortunately, this concern directed towards class, striking exist among Natural progesterone some its derivatives, such 19-norprogesterone molecules, not and, therefore, negative on lipid profile. effects breast tissue remain controversial well. However, progestin duration application, cell differentiation apoptosis predominate over proliferation. unclear if currently available able bind specifically PR isoforms PR-A PR-B whether clinical relevance proliferation unclear. Although likely that neutral risk coronary heart disease cancer younger women, hypothesis must confirmed large randomised, well controlled trials.