Gestodene
Progestin medication / From Wikipedia, the free encyclopedia
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Gestodene, sold under the brand names Femodene and Minulet among others, is a progestin medication which is used in birth control pills for women.[5][6] It is also used in menopausal hormone therapy.[7] The medication is available almost exclusively in combination with an estrogen.[8] It is taken by mouth.[6][9]
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Trade names | Femodene, Femodette, Gynera, Harmonet, Meliane, Minesse, Minulet, others |
Other names | GSD; SHB-331; δ15-Norgestrel; 15-Dehydronorgestrel; 17-hydroxy-18a-homo-19-nor-17α-pregna-4,15-dien-20-yn-3-one; 17α-Ethynyl-18-methyl-19-nor-δ15-testosterone; 17α-Ethynyl-18-methylestra-4,15-dien-17β-ol-3-one; 13β-Ethyl-18,19-dinor-17α-pregna-4,15-dien-20-yn-17β-ol-3-one |
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Routes of administration | By mouth |
Drug class | Progestogen; Progestin |
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Bioavailability | 96% (87–111%)[1][2][3] |
Protein binding | 98% (64% to SHBGTooltip sex hormone-binding globulin, 34% to albumin, 2% free)[4] |
Metabolism | Liver (reduction, hydroxylation)[4] |
Elimination half-life | 12–15 hours[2][4] |
Excretion | Urine |
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ECHA InfoCard | 100.056.478 |
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Formula | C21H26O2 |
Molar mass | 310.437 g·mol−1 |
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Melting point | 197.9 °C (388.2 °F) |
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Side effects of the combination of an estrogen and gestodene include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, and others.[citation needed] Gestodene is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[10][11] It has weak androgenic activity, weak antimineralocorticoid activity, and weak glucocorticoid activity.[10][11]
Gestodene was discovered in 1975 and was introduced for medical use, specifically in birth control pills, in 1987.[4][12] It was subsequently introduced for use in menopausal hormone therapy as well.[7][8] Gestodene is sometimes referred to as a "third-generation" progestin.[13] It is marketed in birth control pills widely throughout the world, whereas it is available for use in menopausal hormone therapy only a few countries.[8][7] Gestodene is not approved in the United States.[14][15]