Megestrol asetat |
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| Nama dagang | Tracetate, dll |
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| 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 |
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| License data |
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Rute
pemberian | Oral |
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| Kelas obat | Progestogen; Progestin; Ester progestogen; Antigonadotropin; Antiandrogen steroid |
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| Kode ATC | |
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| Status hukum |
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| Bioavailabilitas | 100%[2] |
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| Pengikatan protein | 82% menuju albumin,[3] tidak memiliki afinitas terhadap SHBG atau CBG[2][4] |
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| Metabolisme | Hati (hidroksilasi, reduksi, biokonjugasi)[5] |
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| Waktu paruh eliminasi | Rata-rata: 34 jam[6]
Kisaran: 13–105 jam[6] |
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| Ekskresi | Urine: 57–78%[5]
Feses: 8–30%[5] |
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[(8R,9S,10R,13S,14S,17R)-17-asetil-6,10,13-trimetil-3-okso-2,8,9,11,12,14,15,16-oktahidro-1H-siklopenta[a]fenantren-17-il] asetat
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| CompTox Dashboard (EPA) | |
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| ECHA InfoCard | 100.008.969  |
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| Rumus | C24H32O4 |
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| Massa molar | 384,52 g·mol−1 |
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| Model 3D (JSmol) | |
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CC1=C[C@@H]2[C@H](CC[C@]3([C@H]2CC[C@@]3(C(=O)C)OC(=O)C)C)[C@@]4(C1=CC(=O)CC4)C
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InChI=1S/C24H32O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h12-13,18-20H,6-11H2,1-5H3/t18-,19+,20+,22-,23+,24+/m1/s1 Key:RQZAXGRLVPAYTJ-GQFGMJRRSA-N
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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 March 2014. Diakses tanggal 30 December 2023.
- 1 2 3 4 5 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.
- ↑
- ↑ Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH (December 2003). "Classification and pharmacology of progestins". Maturitas. 46 (Suppl 1): S7 – S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.
- 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.
- 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 (March 1989). "Megestrol acetate: clinical experience". Cancer Treatment Reviews. 16 (1): 49–63. doi:10.1016/0305-7372(89)90004-2. PMID 2471590.
- 1 2
- 1 2
- ↑
- ↑
- ↑
- ↑
- ↑
- ↑ Gordon JD (2007). Obstetrics, Gynecology & Infertility: Handbook for Clinicians. Scrub Hill Press, Inc. hlm. 228–. ISBN 978-0-9645467-7-6.
- ↑
- ↑
- ↑
- ↑
- ↑
- ↑
- ↑
- ↑
- ↑ "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.
- Argilés JM, Anguera A, Stemmler B (June 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.
- 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.
- Chang AY (April 1998). "Megestrol acetate as a biomodulator". Seminars in Oncology. 25 (2 Suppl 6): 58–61. PMID 9625385.
- Farrar DJ (March 1999). "Megestrol acetate: promises and pitfalls". AIDS Patient Care and STDs. 13 (3): 149–152. doi:10.1089/apc.1999.13.149. PMID 10375262.
- 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.
- Greenberg M, Lawler D, Zawistowski S, Jöchle W (June 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.
- Karcic E, Philpot C, Morley JE (May 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.
- 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.
- 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.
- 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.
- Mateen F, Jatoi A (October 2006). "Megestrol acetate for the palliation of anorexia in advanced, incurable cancer patients". Clinical Nutrition. 25 (5): 711–715. doi:10.1016/j.clnu.2006.05.009. PMID 16867306.
- Pascual López A, Roqué i Figuls M, Urrútia Cuchi G, Berenstein EG, Almenar Pasies B, Balcells Alegre M, Herdman M (April 2004). "Systematic review of megestrol acetate in the treatment of anorexia-cachexia syndrome". Journal of Pain and Symptom Management. 27 (4): 360–369. doi:10.1016/j.jpainsymman.2003.09.007. PMID 15050664.
- Romatowski J (March 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.
- Ruiz Garcia V, López-Briz E, Carbonell Sanchis R, Gonzalvez Perales JL, Bort-Marti S (March 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.
- Ruiz-García V, Juan O, Pérez Hoyos S, Peiró R, Ramón N, Rosero MA, García MA (July 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.
- 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.
- 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.
- Smith CS, Logomarsino JV (March 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.
- Stockheim JA, Daaboul JJ, Yogev R, Scully SP, Binns HJ, Chadwick EG (March 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.
- 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.
- Tchekmedyian NS (June 1993). "Treatment of anorexia with megestrol acetate". Nutrition in Clinical Practice. 8 (3): 115–118. doi:10.1177/0115426593008003115. PMID 8289758.
- 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.
- Vyzula R (April 1997). "[Current views on use of megestrol acetate in oncology practice]". Vnitrni Lekarstvi (dalam bahasa Ceko). 43 (4): 250–255. PMID 9601846.
- Wazny LD, Nadurak S, Orsulak C, Giles-Smith L, Tangri N (May 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.
- 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.
- Yeh SS, Schuster MW (2006). "Megestrol acetate in cachexia and anorexia". International Journal of Nanomedicine. 1 (4): 411–416. doi:10.2147/nano.2006.1.4.411. PMC 2676640. PMID 17722275.
