Demegestone

Demegestone, sold under the brand name Lutionex, is a progestin medication which was previously used to treat luteal insufficiency but is now no longer marketed. It is taken by mouth. Demegestone 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 no androgenic activity. Demegestone was first described in 1966 and was introduced for medical use in France in 1974. It has only been marketed in France, and has since been discontinued in this country. Demegestone has been used to treat luteal insufficiency. It has also been studied in combination with estrogens, such as moxestrol, as an oral contraceptive and treatment for infertility. Progestin#Side effects Demegestone is a progestogen, and hence is an agonist of the progesterone receptor (PR). It is a highly potent progestogen, showing 50 times the potency of progesterone in the Clauberg test. The ovulation-inbhiting dosage of demegestone is 2.5 mg/day, while the endometrial transformation dosage is 100 mg per cycle. The medication is devoid of androgenic activity, and instead has some antiandrogenic activity. Demegestone has low affinity for the glucocorticoid receptor. In a particular bioassay, both demegestone and progesterone showed antiglucocorticoid rather than glucocorticoid activity. The major metabolite of demegestone, a 21-hydroxylated metabolite, is a moderately potent progestogen (4 times the potency of progesterone) and a weak mineralocorticoid (2% of the potency of deoxycorticosterone). Demegestone has good bioavailability. The initial volume of distribution of demegestone is 31 L. Demegestone is metabolized by hydroxylation at the C21, C1, C2, and C11 positions, which is eventually followed by A-ring aromatization after 1,2-dehydration. The major metabolite of demegestone is a 21-hydroxy derivative. The metabolic clearance rate of demegestone is 20 L/h. Its biological half-lives are 2.39 and 0.24 hours with intravenous injection.