Estradiol-containing birth control pill
Combined birth control pills that contain natural estradiol or an estradiol ester (e.g., estradiol valerate) include:[1][2][3]
- Estradiol valerate and cyproterone acetate (brand name Femilar) – introduced in Finland (only) in 1993[3]
- Estradiol valerate and dienogest (brand names Qlaira, Natazia) – introduced in Europe in 2009 and the U.S. in 2010[4]
- Estradiol and nomegestrol acetate (brand name Zoely) – introduced in Europe in 2011[5]
| Estradiol-containing oral contraceptive | |
|---|---|
| Background | |
| Type | Hormonal |
| First use | 1993 (Finland) |
| Pregnancy rates (first year) | |
| Perfect use | ? |
| Typical use | ? |
| Usage | |
| Reversibility | Yes |
| User reminders | ? |
| Advantages and disadvantages | |
| STI protection | No |
Estradiol, mainly as esters including estradiol valerate, estradiol cypionate, and estradiol enanthate, is also the exclusive estrogen used in combined injectable contraceptives.[6]
Side effects
Birth control pills containing estradiol have less impact on liver protein synthesis than ethinylestradiol-containing birth control pills, and it is thought that for this reason, they may pose less of a risk of venous thromboembolism (VTE).[7][8] In accordance, although birth control pills containing estradiol valerate/dienogest are associated with a significantly increased risk of VTE, they are associated with a significantly lower risk of venous thromboembolism than birth control pills containing ethinylestradiol and a progestin.[9] The risk of VTE with estradiol/nomegestrol acetate birth control pills is under study.[10]
Incidence of irregular vaginal bleeding may be higher with estradiol-containing birth control pills in relation to the fact that estradiol is a weaker estrogen than ethinylestradiol in the endometrium.[3]
Pharmacology
The pharmacodynamics and pharmacokinetics of estradiol in the context of use in birth control pills have been studied and reviewed.[11][2][8]
Research
Experimental estradiol-containing birth control pills that were studied but never marketed include:[3]
- Estradiol/norethisterone (Netagen, Netagen 403)
- Estradiol/estriol/norethisterone (Netagen 423)
- Estradiol/estriol/norethisterone acetate
- Estradiol/desogestrel
- Estradiol cyclooctyl acetate/desogestrel
- Estradiol/ethinylestradiol/dienogest
A large randomized controlled trial of a birth control pill containing ethinylestradiol/norethisterone acetate versus a birth control pill containing estradiol/estriol/norethisterone acetate has been conducted.[12]
See also
References
- De Leo V, Musacchio MC, Cappelli V, Piomboni P, Morgante G (2016). "Hormonal contraceptives: pharmacology tailored to women's health". Human Reproduction Update. 22 (5): 634–46. doi:10.1093/humupd/dmw016. PMID 27307386.
- Stanczyk FZ, Archer DF, Bhavnani BR (2013). "Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment". Contraception. 87 (6): 706–27. doi:10.1016/j.contraception.2012.12.011. PMID 23375353.
- Fruzzetti F, Bitzer J (2010). "Review of clinical experience with estradiol in combined oral contraceptives". Contraception. 81 (1): 8–15. doi:10.1016/j.contraception.2009.08.010. PMID 20004267.
- Guida M, Bifulco G, Di Spiezio Sardo A, Scala M, Fernandez LM, Nappi C (2010). "Review of the safety, efficacy and patient acceptability of the combined dienogest/estradiol valerate contraceptive pill". International Journal of Women's Health. 2: 279–90. doi:10.2147/IJWH.S6954. PMC 2990895. PMID 21151673.
- Burke A (2013). "Nomegestrol acetate-17b-estradiol for oral contraception". Patient Preference and Adherence. 7: 607–19. doi:10.2147/PPA.S39371. PMC 3702550. PMID 23836965.
- http://www.wjpps.com/download/article/1412071798.pdf
- Nelson AL (2015). "An update on new orally administered contraceptives for women". Expert Opinion on Pharmacotherapy. 16 (18): 2759–72. doi:10.1517/14656566.2015.1100173. PMID 26512437. S2CID 207481206.
- Jensen, Jeffrey; Bitzer, Johannes; Serrani, Marco (2013). "Comparison of the pharmacologic and clinical profiles of new combined oral contraceptives containing estradiol". Open Access Journal of Contraception: 39. doi:10.2147/OAJC.S50693. ISSN 1179-1527.
- Fruzzetti F, Cagnacci A (2018). "Venous thrombosis and hormonal contraception: what's new with estradiol-based hormonal contraceptives?". Open Access J Contracept. 9: 75–79. doi:10.2147/OAJC.S179673. PMC 6239102. PMID 30519125.
- Douxfils J, Morimont L, Bouvy C (October 2020). "Oral Contraceptives and Venous Thromboembolism: Focus on Testing that May Enable Prediction and Assessment of the Risk". Semin Thromb Hemost. doi:10.1055/s-0040-1714140. PMID 33080636.
- Kuhnz W, Gansau C, Mahler M (September 1993). "Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17β-estradiol". Arzneimittelforschung. 43 (9): 966–73. ISSN 0004-4172. PMID 8240460.
- "A randomized, double-blind study of two combined oral contraceptives containing the same progestogen, but different estrogens. World Health Organization Task Force on Oral Contraception". Contraception. 21 (5): 445–59. May 1980. doi:10.1016/0010-7824(80)90010-4. PMID 7428356.