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-containing oral contraceptive
First use1993 (Finland)
Pregnancy rates (first year)
Perfect use?
Typical use?
User reminders?
Advantages and disadvantages
STI protectionNo

Estradiol, mainly as esters including estradiol valerate, estradiol cypionate, and estradiol enanthate, is also the exclusive estrogen used in combined injectable contraceptives.[6]

Side effectsEdit

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]

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]


The pharmacodynamics and pharmacokinetics of estradiol in the context of use in birth control pills have been studied and reviewed.[10][2][8]


Experimental estradiol-containing birth control pills that were studied but never marketed include:[3]

See alsoEdit


  1. ^ 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.
  2. ^ a b 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.
  3. ^ a b c d 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.
  4. ^ 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.
  5. ^ 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.
  6. ^
  7. ^ 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.
  8. ^ a b Jensen, Jeffrey; Bitzer, Johannes; Serrani, Marco (2013). "Comparison of the pharmacologic and clinical profiles of new combined oral contraceptives containing estradiol" (PDF). Open Access Journal of Contraception: 39. doi:10.2147/OAJC.S50693. ISSN 1179-1527.
  9. ^ 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.
  10. ^ 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.