User:Mr. Ibrahem/Megestrol

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Mr. Ibrahem/Megestrol
Clinical data
Trade namesMegace, others
Other namesMegestrol acetate, MGA; BDH-1298; NSC-71423; SC-10363; 17α-Acetoxy-6-dehydro-6-methylprogesterone; 17α-Acetoxy-6-methylpregna-4,6-diene-3,20-dione
AHFS/Drugs.comMonograph
Routes of
administration		By mouth (tablets, suspension)
Drug classProgestogen; Progestin
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability100%[1]
Protein binding82% to albumin,[2] no affinity for SHBGTooltip sex hormone-binding globulin or CBGTooltip corticosteroid-binding globulin[1][3]
MetabolismLiver (hydroxylation, reduction, conjugation)[5]
Elimination half-lifeMean: 34 hours[4]
Range: 13–105 hours[4]
ExcretionUrine: 57–78%[5]
Feces: 8–30%[5]
Identifiers
  • [(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
Chemical and physical data
FormulaC24H32O4
Molar mass384.516 g·mol−1
3D model (JSmol)
  • 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
  • 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

Megestrol (MGA), sold under the brand name Megace among others, is a medication mainly used as an appetite stimulant to treat wasting syndromes such as cachexia.[6] It is also used to treat breast cancer and endometrial cancer, and has been used in birth control.[6][7] MGA is generally formulated alone, though has been combined with estrogens in birth control.[6][7] It is usually taken by mouth.[6]

Common side effects include weight gain, vaginal bleeding, nausea, high blood pressure, high blood sugar, and rash.[6] Other side effects may include blood clots.[6] Use during pregnancy or breastfeeding may harm the baby.[6] It is a manufactured progestin.[6] How it brings about weight gain is unclear.[6]

Megestrol was patented in 1959 and introduced for medical use, specifically in birth control pills, in 1963.[7][8] It is available as a generic medication.[6] In the United Kingdom 30 tablets of 160 mg costs the NHS about £20 as of 2021.[9] This amount in the United States costs about 23 USD.[10] It is sold in many countries globally.[11]

References[edit]

  1. ^ a b Kuhl H (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. Archived (PDF) from the original on 2016-08-22. Retrieved 2021-10-31.
  2. ^ 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. Archived from the original on 2021-05-25. Retrieved 2021-10-31. 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 SHBG 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 SHBG bound MA. There was a positive correlation between the MA concentrations in saliva and those in plasma.
  3. ^ Schindler AE, Campagnoli C, Druckmann R, 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.
  4. ^ a b Richard R. Barakat; Maurie Markman; Marcus Randall (2009). Principles and Practice of Gynecologic Oncology. Lippincott Williams & Wilkins. pp. 447–. ISBN 978-0-7817-7845-9. Archived from the original on 2021-06-06. Retrieved 2021-10-31.
  5. ^ a b c Canetta R, Florentine S, Hunter H, Lenaz L (September 1983). "Megestrol acetate". Cancer Treat. Rev. 10 (3): 141–57. doi:10.1016/0305-7372(83)90029-4. PMID 6352021.
  6. ^ a b c d e f g h i j k l "Megestrol Monograph for Professionals". Drugs.com. Archived from the original on 25 February 2021. Retrieved 15 November 2021.
  7. ^ a b c Lara Marks (2010). Sexual Chemistry: A History of the Contraceptive Pill. Yale University Press. pp. 77–78. ISBN 978-0-300-16791-7. Archived from the original on 2021-06-18. Retrieved 2021-10-31.
  8. ^ Benign Prostatic Hypertrophy. Springer Science & Business Media. 6 December 2012. pp. 277–. ISBN 978-1-4612-5476-8.
  9. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 996. ISBN 978-0857114105.
  10. ^ "Megestrol Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 16 November 2021.
  11. ^ Index Nominum 2000: International Drug Directory. Taylor & Francis US. 2000. p. 641. ISBN 978-3-88763-075-1. Archived from the original on 26 May 2013. Retrieved 2 June 2012.
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