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| Data klinis | |
|---|---|
| Nama dagang | Tracetate, dll |
| Nama lain | MGA; BDH-1298; NSC-71423; SC-10363; 17α-Asetoksi-6-dehidro-6-metilprogesteron; 17α-Asetoksi-6-metilpregna-4,6-diena-3,20-diona |
| License data | |
| Rute pemberian | Oral |
| Kelas obat | Progestogen; Progestin; Ester progestogen; Antigonadotropin; Antiandrogen steroid |
| Kode ATC | |
| Status hukum | |
| Status hukum | |
| Data farmakokinetika | |
| Bioavailabilitas | 100%[2] |
| Pengikatan protein | 82% menuju albumin,[3] tidak memiliki afinitas terhadap SHBG atau CBG[2][4] |
| Metabolisme | Hati (hidroksilasi, reduksi, biokonjugasi)[5] |
| Waktu paruh eliminasi | Rata-rata: 34 jam[6] Kisaran: 13–105 jam[6] |
| Ekskresi | Urine: 57–78%[5] Feses: 8–30%[5] |
| Pengenal | |
| |
| Nomor CAS | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.008.969  |
| Data sifat kimia dan fisik | |
| Rumus | C24H32O4 |
| Massa molar | 384,52 g·mol−1 |
| Model 3D (JSmol) | |
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Megestrol asetat (disingkat MGA) adalah obat progestin yang terutama digunakan sebagai stimulan nafsu makan untuk mengobati sindrom wasting seperti kakeksia.[2][6][7][1] Obat ini juga digunakan untuk mengobati kanker payudara dan kanker endometrium, dan telah digunakan dalam pengaturan kelahiran.[6][7][8][9] Megestrol asetat umumnya diformulasikan secara tunggal, meskipun telah dikombinasikan dengan estrogen dalam formulasi kontrasepsi.[10] Obat ini biasanya diminum.[2]
Efek samping megestrol asetat meliputi peningkatan nafsu makan, penambahan berat badan, perdarahan vagina, mual, edema, kadar hormon seks rendah, disfungsi seksual, osteoporosis, komplikasi kardiovaskular, efek glukokortikoid, dan lain-lain.[7] Megestrol asetat adalah progestin atau progestogen sintetis, dan karenanya merupakan agonis reseptor progesteron, target biologis progestogen seperti progesteron. Ia memiliki aktivitas androgenik parsial yang lemah, aktivitas glukokortikoid yang lemah, dan tidak memiliki aktivitas hormonal penting lainnya.[2] Karena aktivitas progestogeniknya, megestrol asetat memiliki efek antigonadotropik.[7] Mekanisme kerja efek perangsang nafsu makan dari megestrol asetat tidak diketahui.[11][12][13]
Megestrol asetat ditemukan pada tahun 1959 dan diperkenalkan untuk penggunaan medis, khususnya dalam pil kontrasepsi oral gabungan, pada tahun 1963.[8][9][14] Obat ini dapat dianggap sebagai progestin "generasi pertama".[15] Obat ini ditarik di beberapa negara pada tahun 1970 karena kekhawatiran tentang toksisitas kelenjar susu yang diamati pada anjing, tetapi ternyata hal ini tidak berlaku untuk manusia.[16][17][18][19][20] Megestrol asetat disetujui untuk pengobatan kanker endometrium pada tahun 1971 dan sindrom wasting pada tahun 1993.[7][21] Obat ini dipasarkan secara luas di seluruh dunia.[22][23] Obat ini tersedia sebagai obat generik.[24]
Referensi
- 1 2 "Megace ES- megesterol acetate suspension". DailyMed. 18 Maret 2014. Diakses tanggal 30 Desember 2023.
{{cite web}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - 1 2 3 4 5 Kuhl H (Agustus 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 journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Chu YH, Li Q, Zhao ZF (April 1986). "Pharmacokinetics of megestrol acetate in women receiving IM injection of estradiol-megestrol long-acting injectable contraceptive". The Chinese Journal of Clinical Pharmacology. Diarsipkan dari asli tanggal 25 Mei 2021. Diakses tanggal 14 Agustus 2019. A radioimmunoassay (RIA), radioligand assay and equilibrium dialysis for determination of plasma and salivary megestrol acetate (MA) concentration, sex hormone binding globulin (SHBG) capacity in plasma and percentage albumin bound MA were studied in healthy women receiving single im injection of estradiol-megestrol long-acting injectable contraceptive. The results showed that after injection the concentration of plasma MA increased rapidly. The meantime of peak plasma MA level was 3rd day, there was a linear relationship between log of plasma MA concentration and time (day) after administration in all subjects, elimination phase half-life t1/2β = 14.35 ± 9.1 days. The plasma sex hormone-binding globulin capacity significantly increased at 7th, 14th day and decreased at 21st, 29th day after injection. The percentage albumin bound MA was 82.4%. There was no specific sex hormone-binding globulin bound MA. There was a positive correlation between the MA concentrations in saliva and those in plasma.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH (Desember 2003). "Classification and pharmacology of progestins". Maturitas. 46 (Suppl 1): S7–S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - 1 2 3 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.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - 1 2 3 4 Barakat RR, Markman M, Randall M (2009). Principles and Practice of Gynecologic Oncology. Lippincott Williams & Wilkins. hlm. 447–. ISBN 978-0-7817-7845-9.
- 1 2 3 4 5 Schacter L, Rozencweig M, Canetta R, Kelley S, Nicaise C, Smaldone L (Maret 1989). "Megestrol acetate: clinical experience". Cancer Treatment Reviews. 16 (1): 49–63. doi:10.1016/0305-7372(89)90004-2. PMID 2471590.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - 1 2 Marks L (2010). Sexual Chemistry: A History of the Contraceptive Pill. Yale University Press. hlm. 77–78. ISBN 978-0-300-16791-7.
- 1 2 Mears E (Mei 1963). "A new type of oral contraceptive". British Medical Journal. 1 (5341): 1318–1320. doi:10.1136/bmj.1.5341.1318. PMC 2123904. PMID 13934321.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Morton IK, Hall JM (1999). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer. hlm. 173. ISBN 978-0-7514-0499-9. Diakses tanggal 2 Juni 2012.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Berger AM, Shuster JL, Von Roenn JH (6 Oktober 2006). Principles And Practice of Palliative Care And Supportive Oncology. Lippincott Williams & Wilkins. hlm. 128. ISBN 978-0-7817-9595-1. Diakses tanggal 27 Mei 2012.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Jörres A (19 Februari 2010). Management of Acute Kidney Problems. Springer. hlm. 210. ISBN 978-3-540-69413-7. Diakses tanggal 27 Mei 2012.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Ettinger DS (11 November 2008). Supportive Care in Cancer Therapy. Springer. hlm. 61. ISBN 978-1-58829-941-3. Diakses tanggal 27 Mei 2012.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Benign Prostatic Hypertrophy. Springer Science & Business Media. 6 Desember 2012. hlm. 277–. ISBN 978-1-4612-5476-8.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Gordon JD (2007). Obstetrics, Gynecology & Infertility: Handbook for Clinicians. Scrub Hill Press, Inc. hlm. 228–. ISBN 978-0-9645467-7-6.
- ↑ Consolidated List of Products Whose Consumption And/or Sale Have Been Banned, Withdrawn, Severely Restricted Or Not Approved by Governments. United Nations Publications. 1983. hlm. 137–. ISBN 978-92-1-130230-1.
- ↑ Nelson LW, Weikel JH, Reno FE (Oktober 1973). "Mammary nodules in dogs during four years' treatment with megestrol acetate or chlormadinone acetate". Journal of the National Cancer Institute. 51 (4): 1303–1311. doi:10.1093/jnci/51.4.1303. PMID 4126857.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ FDA Consumer. U.S. Department of Health, Education, and Welfare, Public Health Service, Food and Drug Administration. Februari 1976. Several foreign countries, including Germany, Canada, and Great Britain, have banned the sale of birth control pills containing megestrol acetate after a study done at FDA's request indicated it caused breast cancer in dogs. Megestrol acetate has never been marketed in the United States as an oral contraceptive. FDA routinely requires long-term animal studies before any drug can be marketed for human use. Following animal studies with megestrol acetate, FDA in the late sixties and early seventies allowed limited studies of the drug in women. In 1972, after noticing a significant number of test dogs developing breast nodules (none of them malignant), FDA ordered that megestrol acetate be discontinued in human oral contraceptive studies.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ United States. Congress. Senate. Committee on Labor and Public Welfare (1976). Hearings, Reports and Prints of the Senate Committee on Labor and Public Welfare. U.S. Government Printing Office. Megestrol was never marketed in the United States for contraceptive use because in 1972, FDA took prompt action to discontinue investigational studies on megestrol after dogs exposed to the drug for four years In a chronic toxicity study developed benign breast tumors.
- ↑ Runnebaum BC, Rabe T, Kiesel L (6 Desember 2012). Female Contraception: Update and Trends. Springer Science & Business Media. hlm. 134–. ISBN 978-3-642-73790-9.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Eibl G, Edderkaoui M (22 April 2015). Risk Factors for Pancreatic Cancer: Underlying Mechanisms and Potential Targets. Frontiers Media SA. hlm. 96–. ISBN 978-2-88919-468-1.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ Index Nominum 2000: International Drug Directory. Taylor & Francis US. 2000. hlm. 641. ISBN 978-3-88763-075-1. Diakses tanggal 2 Juni 2012.
{{cite book}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - ↑ "Megestrol".
- ↑ "Generic Megace Availability".
Bacaan lanjutan
- "Megestrol acetate NCD oral suspension -- Par Pharmaceutical: megestrol acetate nanocrystal dispersion oral suspension, PAR 100.2, PAR-100.2". Drugs in R&D. 8 (4): 251–254. 2007. doi:10.2165/00126839-200708040-00005. PMID 17596111. S2CID 195341085.
- Aisner J, Tchekmedyian NS, Tait N, Parnes H, Novak M (April 1988). "Studies of high-dose megestrol acetate: potential applications in cachexia". Seminars in Oncology. 15 (2 Suppl 1): 68–75. PMID 3285486.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Argilés JM, Anguera A, Stemmler B (Juni 2013). "A new look at an old drug for the treatment of cancer cachexia: megestrol acetate". Clinical Nutrition. 32 (3): 319–324. doi:10.1016/j.clnu.2013.01.004. PMID 23395103.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Berstein LM (1998). "[Megestrol acetate as hormone therapy in oncology]". Voprosy Onkologii (dalam bahasa Rusia). 44 (2): 142–148. PMID 9615815.
- Bonte J (2000). "Third generation aromatase inhibitors in metastatic breast cancer patients failing tamoxifen. Randomized comparisons with megestrol acetate: a critical review". European Journal of Gynaecological Oncology. 21 (6): 555–559. PMID 11214609.
- 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.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Chang AY (April 1998). "Megestrol acetate as a biomodulator". Seminars in Oncology. 25 (2 Suppl 6): 58–61. PMID 9625385.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Farrar DJ (Maret 1999). "Megestrol acetate: promises and pitfalls". AIDS Patient Care and STDs. 13 (3): 149–152. doi:10.1089/apc.1999.13.149. PMID 10375262.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Femia RA, Goyette RE (2005). "The science of megestrol acetate delivery: potential to improve outcomes in cachexia". BioDrugs. 19 (3): 179–187. doi:10.2165/00063030-200519030-00004. PMID 15984902. S2CID 11602342.
- Fox CB, Treadway AK, Blaszczyk AT, Sleeper RB (April 2009). "Megestrol acetate and mirtazapine for the treatment of unplanned weight loss in the elderly". Pharmacotherapy. 29 (4): 383–397. doi:10.1592/phco.29.4.383. PMID 19323618. S2CID 6695434.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Greenberg M, Lawler D, Zawistowski S, Jöchle W (Juni 2013). "Low-dose megestrol acetate revisited: a viable adjunct to surgical sterilization in free roaming cats?". Veterinary Journal. 196 (3): 304–308. doi:10.1016/j.tvjl.2013.01.038. PMID 23499239.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Karcic E, Philpot C, Morley JE (Mei 2002). "Treating malnutrition with megestrol acetate: literature review and review of our experience". The Journal of Nutrition, Health & Aging. 6 (3): 191–200. PMID 12152625.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Leśniak W, Bała M, Jaeschke R, Krzakowski M (November 2008). "Effects of megestrol acetate in patients with cancer anorexia-cachexia syndrome--a systematic review and meta-analysis". Polskie Archiwum Medycyny Wewnetrznej. 118 (11): 636–644. doi:10.20452/pamw.510. PMID 19140567. S2CID 1338200.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Mann M, Koller E, Murgo A, Malozowski S, Bacsanyi J, Leinung M (1997). "Glucocorticoidlike activity of megestrol. A summary of Food and Drug Administration experience and a review of the literature". Archives of Internal Medicine. 157 (15): 1651–1656. doi:10.1001/archinte.1997.00440360053005. PMID 9250225.
- Mantovani G, Macciò A, Lai P, Massa E, Ghiani M, Santona MC (April 1998). "Cytokine activity in cancer-related anorexia/cachexia: role of megestrol acetate and medroxyprogesterone acetate". Seminars in Oncology. 25 (2 Suppl 6): 45–52. PMID 9625383.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Mantovani G, Macciò A, Lai P, Massa E, Ghiani M, Santona MC (1998). "Cytokine involvement in cancer anorexia/cachexia: role of megestrol acetate and medroxyprogesterone acetate on cytokine downregulation and improvement of clinical symptoms". Critical Reviews in Oncogenesis. 9 (2): 99–106. doi:10.1615/critrevoncog.v9.i2.10. PMID 9973244.
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{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Romatowski J (Maret 1989). "Use of megestrol acetate in cats". Journal of the American Veterinary Medical Association. 194 (5): 700–702. doi:10.2460/javma.1989.194.05.700. PMID 2647696.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Ruiz Garcia V, López-Briz E, Carbonell Sanchis R, Gonzalvez Perales JL, Bort-Marti S (Maret 2013). "Megestrol acetate for treatment of anorexia-cachexia syndrome". The Cochrane Database of Systematic Reviews. 2013 (3) CD004310. doi:10.1002/14651858.CD004310.pub3. PMC 6418472. PMID 23543530.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Ruiz-García V, Juan O, Pérez Hoyos S, Peiró R, Ramón N, Rosero MA, García MA (Juli 2002). "[Megestrol acetate: a systematic review usefulness about the weight gain in neoplastic patients with cachexia]". Medicina Clinica (dalam bahasa Spanyol). 119 (5): 166–170. doi:10.1016/S0025-7753(02)73352-6. PMID 12200017.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Schacter L, Rozencweig M, Canetta R, Kelley S, Nicaise C, Smaldone L (Maret 1989). "Megestrol acetate: clinical experience". Cancer Treatment Reviews. 16 (1): 49–63. doi:10.1016/0305-7372(89)90004-2. PMID 2471590.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Sedlacek SM (April 1988). "An overview of megestrol acetate for the treatment of advanced breast cancer". Seminars in Oncology. 15 (2 Suppl 1): 3–13. PMID 3285483.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Smith CS, Logomarsino JV (Maret 2016). "Using megestrol acetate to ameliorate protein-energy wasting in chronic kidney disease". Journal of Renal Care. 42 (1): 53–59. doi:10.1111/jorc.12138. PMID 26537025.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Stockheim JA, Daaboul JJ, Yogev R, Scully SP, Binns HJ, Chadwick EG (Maret 1999). "Adrenal suppression in children with the human immunodeficiency virus treated with megestrol acetate". The Journal of Pediatrics. 134 (3): 368–370. doi:10.1016/s0022-3476(99)70467-1. PMID 10064680.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Strang P (1997). "The effect of megestrol acetate on anorexia, weight loss and cachexia in cancer and AIDS patients (review)". Anticancer Research. 17 (1B): 657–662. PMID 9066597.
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{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Thomas DR (2004). "Incidence of venous thromboembolism in megestrol acetate users". Journal of the American Medical Directors Association. 5 (1): 65–6, author reply 66–7. doi:10.1097/01.JAM.0000105070.61741.9D. PMID 14726802.
- Venner P (1992). "Megestrol acetate in the treatment of metastatic carcinoma of the prostate". Oncology. 49 Suppl 2 (2): 22–27. doi:10.1159/000227123. PMID 1461622.
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{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Wazny LD, Nadurak S, Orsulak C, Giles-Smith L, Tangri N (Mei 2016). "The Efficacy and Safety of Megestrol Acetate in Protein-Energy Wasting due to Chronic Kidney Disease: A Systematic Review". Journal of Renal Nutrition. 26 (3): 168–176. doi:10.1053/j.jrn.2015.11.002. PMID 26776251.
{{cite journal}}: Pemeliharaan CS1: Tanggal diterjemahkan otomatis (link) - Wentling GK, Sevin BU, Geiger XJ, Bridges MD (2005). "Benign metastasizing leiomyoma responsive to megestrol: case report and review of the literature". International Journal of Gynecological Cancer. 15 (6): 1213–1217. doi:10.1111/j.1525-1438.2005.00190.x. PMID 16343217.
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