Estradiol acetate (EA), sold under the brand names Femtrace, Femring, and Menoring, is an estrogen medication which is used in hormone therapy for the treatment of menopausalsymptoms in women.[3][4][5][6] It is taken by mouth once daily or given as a vaginal ring once every three months.[2]
Estradiol acetate was introduced for medical use in 2001.[11] It is available in the United States and the United Kingdom.[11][3] The formulation for use by mouth has been discontinued in the United States.[12]
The Women's Health Initiative studies report increased health risks for menopausal women when using unopposed estrogens.[6] Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman.[6]
Available forms
Estradiol acetate comes in the form of 0.45, 0.9, and 1.8 mg oral tablets (Femtrace) and in the form of 12.4 or 24.8 mg vaginal rings that release 50 or 100 μg/day estradiol for 3 months (Femring, Menoring).[5][6][17] However, the Femtrace product was discontinued in the United States.[12]
Estradiol acetate is converted into estradiol in the body.[9][8]
Chemistry
Estradiol acetate is a syntheticestranesteroid and the C3 acetateester of estradiol.[3] It is also known as estradiol 3-acetate or as estra-1,3,5(10)-triene-3,17β-diol 3-acetate.[3] Another common ester of estradiol in use for oral administration is estradiol valerate, which is a C17β ester of estradiol.[8][23]
Estradiol acetate is relatively recent to the market, having been first approved in a vaginal ringformulation as Menoring in the United Kingdom in 2001,[13] followed by a vaginal ring formulation as Femring in the United States in 2002,[2] and finally as an oral preparation as Femtrace in the United States in 2004.[2][11]
Society and culture
Generic names
Estradiol acetate is the generic name of the drug and its USANTooltip United States Adopted Name.[3]
Brand names
Estradiol acetate is marketed under the brand names Femtrace, Femring, and Menoring.[3][25][26]
^"Estradiol: Uses, Dosage & Side Effects". Drugs.com. Retrieved 21 April 2023.
^ a b c dSivanandy MS, Masimasi N, Thacker HL (May 2007). "Newer hormonal therapies: lower doses; oral, transdermal, and vaginal formulations". Cleveland Clinic Journal of Medicine. 74 (5): 369–375. doi:10.3949/ccjm.74.5.369. PMID 17506242. S2CID 35423126.
^ a b c d e f g h"Estradiol Monograph for Professionals".
^Buckler H, Al-Azzawi F (August 2003). "The effect of a novel vaginal ring delivering oestradiol acetate on climacteric symptoms in postmenopausal women". BJOG. 110 (8): 753–759. doi:10.1016/s1470-0328(03)02908-2. PMID 12892687.
^ a b c"Highlights of prescribing information" (PDF). accessdata.fda.gov. 2014. Retrieved 21 April 2023.
^ a b c d e"FEMRING". DailyMed. U.S. National Library of Medicine.
^ a bMcIver B, Tebben PJ (23 September 2010). "Endocrinology". In Ghosh AK (ed.). Mayo Clinic Internal Medicine Board Review. OUP USA. pp. 222–. ISBN 978-0-19-975569-1.
^ a b c d e fKuhl 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.
^ a b c d e f gKuhnz W, Blode H, Zimmermann H (6 December 2012). "Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens". In Oettel M, Schillinger E (eds.). Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. Handbook of Experimental Pharmacology. Vol. 135 / 2. Springer Science & Business Media. p. 261. doi:10.1007/978-3-642-60107-1_15. ISBN 978-3-642-60107-1. Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.
^ a bCirigliano M (June 2007). "Bioidentical hormone therapy: a review of the evidence". Journal of Women's Health. 16 (5): 600–631. doi:10.1089/jwh.2006.0311. PMID 17627398.
^ a b c dBallagh SA (2004). "Vaginal rings for menopausal symptom relief". Drugs & Aging. 21 (12): 757–766. doi:10.2165/00002512-200421120-00001. PMID 15382956. S2CID 20717960.
^ a b"Drugs@FDA: FDA-Approved Drugs".
^ a bSperoff L (October 2003). "Efficacy and tolerability of a novel estradiol vaginal ring for relief of menopausal symptoms". Obstetrics and Gynecology. 102 (4): 823–834. doi:10.1016/s0029-7844(03)00764-6. PMID 14551014. S2CID 10289535.
^Al-Azzawi F, Lees B, Thompson J, Stevenson JC (2005). "Bone mineral density in postmenopausal women treated with a vaginal ring delivering systemic doses of estradiol acetate". Menopause. 12 (3): 331–339. doi:10.1097/01.gme.0000163870.03388.4d. PMID 15879923. S2CID 22295565.
^Utian WH, Speroff L, Ellman H, Dart C (2005). "Comparative controlled trial of a novel oral estrogen therapy, estradiol acetate, for relief of menopause symptoms". Menopause. 12 (6): 708–715. doi:10.1097/01.gme.0000184220.63459.a8. PMID 16278614. S2CID 28927438.
^Speroff L, Haney AF, Gilbert RD, Ellman H (2006). "Efficacy of a new, oral estradiol acetate formulation for relief of menopause symptoms". Menopause. 13 (3): 442–450. doi:10.1097/01.gme.0000182802.06762.b2. PMID 16735941. S2CID 19563197.
^Lowdermilk DL, Perry SE, Cashion MC, Alden KR (18 December 2014). "Reproductive System Concerns". Maternity and Women's Health Care - E-Book. Elsevier Health Sciences. pp. 137–. ISBN 978-0-323-39019-4.
^ a b cLauritzen C (September 1990). "Clinical use of oestrogens and progestogens". Maturitas. 12 (3): 199–214. doi:10.1016/0378-5122(90)90004-P. PMID 2215269.
^Lauritzen C, Studd JW (22 June 2005). Current Management of the Menopause. CRC Press. pp. 95–98, 488. ISBN 978-0-203-48612-2.
^Laurtizen C (2001). "Hormone Substitution Before, During and After Menopause" (PDF). In Fisch FH (ed.). Menopause – Andropause: Hormone Replacement Therapy Through the Ages. Krause & Pachernegg: Gablitz. pp. 67–88. ISBN 978-3-901299-34-6.
^Midwinter A (1976). "Contraindications to estrogen therapy and management of the menopausal syndrome in these cases". In Campbell S (ed.). The Management of the Menopause & Post-Menopausal Years: The Proceedings of the International Symposium held in London 24–26 November 1975 Arranged by the Institute of Obstetrics and Gynaecology, The University of London. MTP Press Limited. pp. 377–382. doi:10.1007/978-94-011-6165-7_33. ISBN 978-94-011-6167-1.
^Cheng ZN, Shu Y, Liu ZQ, Wang LS, Ou-Yang DS, Zhou HH (February 2001). "Role of cytochrome P450 in estradiol metabolism in vitro". Acta Pharmacologica Sinica. 22 (2): 148–154. PMID 11741520.
^Düsterberg B, Nishino Y (December 1982). "Pharmacokinetic and pharmacological features of oestradiol valerate". Maturitas. 4 (4): 315–324. doi:10.1016/0378-5122(82)90064-0. PMID 7169965.
^U.S. Food and Drug Administration (2009). Menopause - Medicines to Help You. GPO FCIC. pp. 3–. ISBN 978-1-61221-026-1.
^Fritz MA, Speroff L (28 March 2012). "Postmenopausal Hormone Therapy". Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 757–. ISBN 978-1-4511-4847-3.