Norgestimate, sold under the brand names Ortho Tri-Cyclen and Previfem among others, is a progestin medication which is used in birth control pills for women and in menopausal hormone therapy.[1][3][4][5] The medication is available in combination with an estrogen and is not available alone.[6] It is taken by mouth.[1]
Side effects of the combination of an estrogen and norgestimate include menstrual irregularities, headaches, nausea, abdominal pain, breast tenderness, mood changes, and others.[3][4] Norgestimate is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[1] It has very weak androgenic activity and no other important hormonal activity.[1] The medication is a prodrug of norelgestromin and to a lesser extent of levonorgestrel in the body.[1]
Norgestimate was patented in 1965 and introduced for medical use, specifically in birth control pills, in 1986.[7][8] It was introduced for use in menopausal hormone therapy in the United States in 1999.[9] Norgestimate is sometimes referred to as a "third-generation" progestin.[10] It is marketed in birth control pills widely throughout the world, whereas it is available for use in menopausal hormone therapy only in the United States and Brazil.[6] Norgestimate is available as a generic medication.[11] In 2021, the version with ethinylestradiol was the 76th most commonly prescribed medication in the United States, with more than 8million prescriptions.[12][13]
^ abcdefghijklmnopKuhl H (August 2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration". Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
^Fotherby K (August 1996). "Bioavailability of orally administered sex steroids used in oral contraception and hormone replacement therapy". Contraception. 54 (2): 59–69. doi:10.1016/0010-7824(96)00136-9. PMID 8842581.
^ abcd"Prefest- estradiol/norgestimate kit". DailyMed. 29 February 2016. Retrieved 9 November 2020.
^ abcde"Ortho Tri Cyclen- norgestimate and ethinyl estradiol kit Ortho Cyclen- norgestimate and ethinyl estradiol kit". DailyMed. 16 May 2019. Retrieved 9 November 2020.
^Lemke TL, Williams DA (2008). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 1316–. ISBN 978-0-7817-6879-5.
^ abCite error: The named reference Drugs.com was invoked but never defined (see the help page).
^Cite error: The named reference RunnebaumRabe2012 was invoked but never defined (see the help page).
^Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 479. ISBN 9783527607495.
^Cite error: The named reference FDA2013 was invoked but never defined (see the help page).
^Carp HJ (9 April 2015). Progestogens in Obstetrics and Gynecology. Springer. p. 112. ISBN 978-3-319-14385-9.
Norgestimate, sold under the brand names Ortho Tri-Cyclen and Previfem among others, is a progestin medication which is used in birth control pills for...
and ethinylestradiol G03AA10 Gestodene and ethinylestradiol G03AA11 Norgestimate and ethinylestradiol G03AA12 Drospirenone and ethinylestradiol G03AA13...
similar to other newer 19-nortestosterone progestins like gestodene and norgestimate. It has been estimated that 150 μg/day desogestrel has less than one-sixth...
a prodrug of levonorgestrel. Norgestimate is the C3 oxime of LNG-A. The drug is a minor active metabolite of norgestimate, which is a prodrug of norelgestromin...
injection site. Erenumab was shown not to interact with ethinylestradiol, norgestimate or the migraine drug sumatriptan. It is expected to generally have a...
Norelgestromin is a progestogen. It is one of the active metabolites of norgestimate. Unlike many related progestins, norelgestromin reportedly has negligible...
of 96%. Unlike other third-generation progestins like desogestrel and norgestimate, gestodene is not a prodrug. Peak levels of gestodene occur within 1...
non-fatal venous thromboembolic events compared with women who took a norgestimate-containing oral contraceptive with 35 μg of estrogen. However, a different...
United States, with more than 12 million prescriptions; the version with norgestimate was the 76th most commonly prescribed medication in the US, with more...
mass: 369.50 g/mol, exact mass: 369.2304 u) may refer to: Diprafenone Norgestimate This set index page lists chemical structure articles associated with...
fourth-generation progestins, including desogestrel, dienogest, drospirenone, or norgestimate, as well as birth control pills containing cyproterone acetate or chlormadinone...
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