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Demegestone
Chemical compound From Wikipedia, the free encyclopedia
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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.[3][4][5][6][7] It is taken by mouth.[2][1]
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Demegestone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[6][2][8] It has no androgenic activity.[2]
Demegestone was first described in 1966 and was introduced for medical use in France in 1974.[3][4] It has only been marketed in France, and has since been discontinued in this country.[5][4]
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Medical uses
Demegestone has been used to treat luteal insufficiency.[7] It has also been studied in combination with estrogens, such as moxestrol, as an oral contraceptive and treatment for infertility.[1][9][10]
Side effects
Pharmacology
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Perspective
Pharmacodynamics
Demegestone is a progestogen, and hence is an agonist of the progesterone receptor (PR).[6][8][2] It is a highly potent progestogen, showing 50 times the potency of progesterone in the Clauberg test.[2] The ovulation-inbhiting dosage of demegestone is 2.5 mg/day, while the endometrial transformation dosage is 100 mg per cycle.[11] The medication is devoid of androgenic activity,[2] and instead has some antiandrogenic activity.[12] Demegestone has low affinity for the glucocorticoid receptor.[13] In a particular bioassay, both demegestone and progesterone showed antiglucocorticoid rather than glucocorticoid activity.[14] 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).[2]
Pharmacokinetics
Demegestone has good bioavailability.[2] The initial volume of distribution of demegestone is 31 L.[2] 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.[2] The major metabolite of demegestone is a 21-hydroxy derivative.[2] The metabolic clearance rate of demegestone is 20 L/h.[2] Its biological half-lives are 2.39 and 0.24 hours with intravenous injection.[2] Demegestone and/or its metabolites are excreted, at least in part, in urine.[2]
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Chemistry
Demegestone, also known as 17α-methyl-δ9-19-norprogesterone or as 17α-methyl-19-norpregna-4,9-diene-3,20-dione, is a synthetic norpregnane steroid and a derivative of progesterone.[3][4][6] It is specifically a combined derivative of 17α-methylprogesterone and 19-norprogesterone, or of 17α-methyl-19-norprogesterone.[3][4][6] Related derivatives of 17α-methyl-19-norprogesterone include promegestone and trimegestone.[3][6]
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History
Demegestone was first described in the literature in 1964 and was introduced for medical use in 1974 in France.[3][4] It was developed by Roussel Uclaf.[4]
Society and culture
Generic names
Demegestone is the generic name of the drug and its INN.[3] It is also known by its developmental code name R-2453 or RU-2453.[3]
Brand names
Demegestone was marketed under the brand name Lutionex.[3][4]
Availability
Demegestone is no longer marketed and hence is no longer available in any country.[5] It was previously available in France.[5][4]
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References
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