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Megestrol acetate
Pharmaceutical drug / From Wikipedia, the free encyclopedia
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Megestrol acetate (MGA), sold under the brand name Megace among others, is a progestin medication which is used mainly as an appetite stimulant to treat wasting syndromes such as cachexia.[2][6][7][1] It is also used to treat breast cancer and endometrial cancer, and has been used in birth control.[6][7][8][9] Megestrol acetate is generally formulated alone, although it has been combined with estrogens in birth control formulations.[10] It is usually taken by mouth.[2]
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Trade names | Megace, others |
Other names | MGA; BDH-1298; NSC-71423; SC-10363; 17α-Acetoxy-6-dehydro-6-methylprogesterone; 17α-Acetoxy-6-methylpregna-4,6-diene-3,20-dione |
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Routes of administration | By mouth |
Drug class | Progestogen; Progestin; Progestogen ester; Antigonadotropin; Steroidal antiandrogen |
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Bioavailability | 100%[2] |
Protein binding | 82% to albumin,[3] no affinity for SHBGTooltip sex hormone-binding globulin or CBGTooltip corticosteroid-binding globulin[2][4] |
Metabolism | Liver (hydroxylation, reduction, conjugation)[5] |
Elimination half-life | Mean: 34 hours[6] Range: 13–105 hours[6] |
Excretion | Urine: 57–78%[5] Feces: 8–30%[5] |
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ECHA InfoCard | 100.008.969 ![]() |
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Formula | C24H32O4 |
Molar mass | 384.516 g·mol−1 |
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Side effects of megestrol acetate include increased appetite, weight gain, vaginal bleeding, nausea, edema, low sex hormone levels, sexual dysfunction, osteoporosis, cardiovascular complications, glucocorticoid effects, and others.[7] Megestrol acetate is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[2] It has weak partial androgenic activity, weak glucocorticoid activity, and no other important hormonal activity.[2] Due to its progestogenic activity, megestrol acetate has antigonadotropic effects.[7] The mechanism of action of the appetite stimulant effects of megestrol acetate is unknown.[11][12][13]
Megestrol acetate was discovered in 1959 and was introduced for medical use, specifically in birth control pills, in 1963.[8][9][14] It may be considered a "first-generation" progestin.[15] The medication was withdrawn in some countries in 1970 due to concerns about mammary toxicity observed in dogs, but this turned out not to apply to humans.[16][17][18][19][20] Megestrol acetate was approved for the treatment of endometrial cancer in 1971 and wasting syndromes in 1993.[7][21] It is marketed widely throughout the world.[22][23] It is available as a generic medication.[24]