Norelgestromin, ornorelgestromine, sold under the brand namesEvra andOrtho Evra among others, is aprogestin medication which is used as a method ofbirth control for women.[5][6][7] The medication is available in combination with anestrogen and is not available alone.[5] It is used as apatch that is applied to the skin.[6][7]
Norelgestromin was introduced for medical use in 2002.[10] It is sometimes referred to as a "third-generation" progestin.[11][12] Norelgestromin is marketed widely throughout the world.[5] It is available as ageneric medication.[13]
Norelgestromin is available only as a transdermal contraceptive patch in combination with ethinyl estradiol.[6] The Ortho Evra patch is a 20 cm2, once-weekly adhesive that contains 6.0 mg norelgestromin and 0.6 mg ethinyl estradiol and delivers 200 μg/day norelgestromin and 35 μg/day ethinyl estradiol.[4][14]
Norelgestromin is aprogestogen.[3][4] It is one of theactive metabolites ofnorgestimate.[8][9] Unlike many related progestins, norelgestromin reportedly has negligibleandrogenic activity.[9] However, it produceslevonorgestrel as an active metabolite to some extent, which does have some androgenic activity.[4][3] Nonetheless, transdermally-administered norelgestromin does not counteract the increase insex hormone-binding globulin levels produced by ethinyl estradiol.[4]
Relative affinities (%) of norelgestromin and metabolites
Upon application of a transdermal patch containing norelgestromin and ethinyl estradiol,plateau levels of both are reached by approximately 48 hours, andsteady-state levels are reached within 2 weeks of application.[4] Absorption following application to the buttock, upper outer arm, abdomen, and upper torso was assessed and, while absorption from the abdomen was slightly lower, it was considered to be therapeutically equivalent for the various areas.[4] Mean levels of norelgestromin at steady-state ranged from 0.305 ng/mL to 1.53 ng/mL, with an average of about 0.725 ng/mL.[4] Theplasma protein binding of norelgestromin is 99%, and it is bound toalbumin but not tosex hormone-binding globulin.[1][2][3]
Norelgestromin is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name, andBANTooltip British Approved Name.[5] The combined ethinyl estradiol and norelgestromin contraceptive patch is also known by its developmental code nameRWJ-10553.[22]
Atransdermalgel formulation of norgelstromin andethinyl estradiol was under development by Antares Pharma for use as a method of birth control with the code name AP-1081 but development was discontinued.[23]
^Philibert D, Bouchoux F, Degryse M, Lecaque D, Petit F, Gaillard M (October 1999). "The pharmacological profile of a novel norpregnance progestin (trimegestone)".Gynecological Endocrinology.13 (5):316–326.doi:10.3109/09513599909167574.PMID10599548.
^US 7345183, Tombari DG, Vecchioli A, "Process for obtaining norelgestromin in different relations of isomers E and Z", issued 18 March 2008, assigned to Gador SA.
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Graziottin A (2006). "A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch".Treatments in Endocrinology.5 (6):359–365.doi:10.2165/00024677-200605060-00004.PMID17107221.S2CID21033630.
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