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Clinical data | |
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Trade names | Dimetriose, Dimetrose, Nemestran, others |
Other names | Ethylnorgestrienone; A-46745; R2323; R-2323; RU-2323; 17α-Ethynyl-18-methyl-δ9,11-19-nortestosterone; 17α-Ethynyl-18-methylestra-4,9,11-trien-17β-ol-3-one; 13β-Ethyl-18,19-dinor-17α-pregna-4,9,11-trien-20-yn-17β-ol-3-one |
AHFS/Drugs.com | International Drug Names |
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Routes of administration | By mouth, vaginal[1] |
Drug class | Progestogen; Progestin; Antiprogestogen; Androgen; Anabolic steroid; Steroidogenesis inhibitor; Antiestrogen |
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Pharmacokinetic data | |
Protein binding | To albumin[1] |
Metabolism | Liver (hydroxylation)[1] |
Elimination half-life | 27.3 hours[1] |
Excretion | Urine and bile[1] |
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ECHA InfoCard | 100.210.606 |
Chemical and physical data | |
Formula | C21H24O2 |
Molar mass | 308.421 g·mol−1 |
3D model (JSmol) | |
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Gestrinone, sold under the brand names Dimetrose and Nemestran among others, is a medication which is used in the treatment of endometriosis.[3][4] It has also been used to treat other conditions such as uterine fibroids and heavy menstrual bleeding and has been investigated as a method of birth control.[5][6][1] Gestrinone is used alone and is not formulated in combination with other medications.[7] It is taken by mouth or in through the vagina.[1][8]
Side effects of gestrinone include menstrual abnormalities, estrogen deficiency, and symptoms of masculinization like acne, seborrhea, breast shrinkage, increased hair growth, and scalp hair loss, among others.[1][8][9][10] Gestrinone has a complex mechanism of action, and is characterized as a mixed progestogen and antiprogestogen, a weak androgen and anabolic steroid, a weak antigonadotropin, a weak steroidogenesis inhibitor, and a functional antiestrogen.[11][1][12][13]
Gestrinone was introduced for medical use in 1986.[14] It has been used extensively in Europe but appears to remains marketed only in a few countries throughout the world.[10][15][7] The medication is not available in the United States.[16] Due to its anabolic effects, the use of gestrinone in competition has been banned by the International Olympic Committee.[17]
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