Concept

Promegestone

Summary
Promegestone, sold under the brand name Surgestone, is a progestin medication which is used in menopausal hormone therapy and in the treatment of gynecological disorders. It is taken by mouth. Side effects of promegestone include menstrual irregularities among others. Promegestone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak antiandrogenic, glucocorticoid, and antimineralocorticoid activity and no other important hormonal activity. The medication is largely a prodrug of trimegestone. Promegestone was first described in 1973 and was introduced for medical use in France in 1983. It has only been marketed in a few countries, including France, Portugal, Tunisia, and Argentina. In addition to its use as a medication, promegestone has been widely used in scientific research as a radioligand of the progesterone receptor. Promegestone is used in menopausal hormone therapy and in the treatment of gynecological conditions caused by luteal insufficiency, including premenopausal disorders, dysmenorrhea and other menstrual disorders, and premenstrual syndrome. It has also been used to treat benign breast disorders such as mastalgia (breast pain). Promegestone tablets have a contraceptive effect and are used as a form of progestogen-only birth control, although it is not specifically licensed as such. Progestin#Side effects Side effects of promegestone include menstrual irregularities among others. It has no androgenic side effects. Promegestone is a progestogen, or an agonist of the progesterone receptor. It has about 200% of the affinity of progesterone for the PR. The endometrial transformation dosage of promegestone is 10 mg per cycle and its ovulation-inhibiting dosage is 0.5 mg/day. Promegestone has weak glucocorticoid activity in addition to its progestogenic activity. Conversely, it has no androgenic, estrogenic, mineralocorticoid, or other hormonal activity. It appears to possess antiandrogenic activity.
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