Global InformationMegestrol acetate information
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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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| Pharmacokinetic data | |
| Bioavailability | 100%[2] |
| Protein binding | 82% to albumin,[3] no affinity for SHBG or CBG[2][4] |
| Metabolism | Liver (hydroxylation, reduction, conjugation)[6] |
| Elimination half-life | Mean: 34 hours[5] Range: 13–105 hours[5] |
| Excretion | Urine: 57–78%[6] Feces: 8–30%[6] |
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| ECHA InfoCard | 100.008.969 |
| Chemical and physical data | |
| Formula | C24H32O4 |
| Molar mass | 384.516 g·mol−1 |
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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][5][7][1] It is also used to treat breast cancer and endometrial cancer, and has been used in birth control.[5][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]
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in birth control pills, in 1963.[8][9][14] It may be considered a "first-generation" progestin.[15] The medication was withdrawn in some countries in 1970 due to concerns about mammary toxicity observed in dogs, but this turned out not to apply to humans.[16][17][18][19][20] Megestrol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]
- ^ a b "Megace ES- megesterol acetate suspension". DailyMed. 18 March 2014. Retrieved 30 December 2023.
- ^ a b c d e f Kuhl H (August 2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
- ^ Cite error: The named reference
ChuLi1986bwas invoked but never defined (see the help page). - ^ Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, et al. (December 2003). "Classification and pharmacology of progestins". Maturitas. 46 (Suppl 1): S7–S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.
- ^ a b c d Barakat RR, Markman M, Randall M (2009). Principles and Practice of Gynecologic Oncology. Lippincott Williams & Wilkins. pp. 447–. ISBN 978-0-7817-7845-9.
- ^ a b c Canetta R, Florentine S, Hunter H, Lenaz L (September 1983). "Megestrol acetate". Cancer Treatment Reviews. 10 (3): 141–157. doi:10.1016/0305-7372(83)90029-4. PMID 6352021.
- ^ a b c d e Schacter L, Rozencweig M, Canetta R, Kelley S, Nicaise C, Smaldone L (March 1989). "Megestrol acetate: clinical experience". Cancer Treatment Reviews. 16 (1): 49–63. doi:10.1016/0305-7372(89)90004-2. PMID 2471590.
- ^ a b Cite error: The named reference
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Springer2012was invoked but never defined (see the help page). - ^ Gordon JD (2007). Obstetrics, Gynecology & Infertility: Handbook for Clinicians. Scrub Hill Press, Inc. pp. 228–. ISBN 978-0-9645467-7-6.
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Drugs.comwas invoked but never defined (see the help page). - ^ "Generic Megace Availability".