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==Side effects==
==Side effects==
It is hypothesized that these contraceptives may pose less of a risk of [[blood clot]]s than contraceptives containing [[ethinylestradiol]], which is the conventional [[estrogen (medication)|estrogen]] that is used in oral contraceptives, but this has yet to be proven.<ref name="pmid26512437">{{cite journal | vauthors = Nelson AL | title = An update on new orally administered contraceptives for women | journal = Expert Opinion on Pharmacotherapy | volume = 16 | issue = 18 | pages = 2759–72 | year = 2015 | pmid = 26512437 | doi = 10.1517/14656566.2015.1100173 | url = }}</ref> However, incidence of irregular [[vaginal bleeding]] may be higher with estradiol-containing contraceptives in relation to the fact that estradiol is a weaker estrogen than ethinylestradiol in the [[endometrium]].<ref name="pmid20004267" />
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).<ref name="pmid26512437">{{cite journal | vauthors = Nelson AL | title = An update on new orally administered contraceptives for women | journal = Expert Opinion on Pharmacotherapy | volume = 16 | issue = 18 | pages = 2759–72 | year = 2015 | pmid = 26512437 | doi = 10.1517/14656566.2015.1100173 | url = }}</ref><ref name="JensenBitzer2013" /> 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.<ref name="pmid30519125">{{cite journal | vauthors = Fruzzetti F, Cagnacci A | title = Venous thrombosis and hormonal contraception: what's new with estradiol-based hormonal contraceptives? | journal = Open Access J Contracept | volume = 9 | issue = | pages = 75–79 | date = 2018 | pmid = 30519125 | pmc = 6239102 | doi = 10.2147/OAJC.S179673 | url = }}</ref>


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]].<ref name="pmid20004267" />
Birth control pills containing [[estradiol valerate/dienogest]] (Qlaira, Natazia) are associated with a significantly increased risk of [[venous thromboembolism]].<ref name="pmid30519125">{{cite journal | vauthors = Fruzzetti F, Cagnacci A | title = Venous thrombosis and hormonal contraception: what's new with estradiol-based hormonal contraceptives? | journal = Open Access J Contracept | volume = 9 | issue = | pages = 75–79 | date = 2018 | pmid = 30519125 | pmc = 6239102 | doi = 10.2147/OAJC.S179673 | url = }}</ref> However, they are associated with a significantly lower risk of venous thromboembolism than birth control pills containing [[ethinylestradiol]] and a progestin.<ref name="pmid30519125" />


==Pharmacology==
==Pharmacology==
The [[pharmacodynamics]] and [[pharmacokinetics]] of estradiol in the context of use in birth control pills have been studied and reviewed.<ref name="pmid8240460">{{cite journal | vauthors = Kuhnz W, Gansau C, Mahler M | title = Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17β-estradiol | journal = Arzneimittelforschung | volume = 43 | issue = 9 | pages = 966–73 | date = September 1993 | issn = 0004-4172 | pmid = 8240460 | doi = | url = }}</ref><ref name="pmid23375353" />
The [[pharmacodynamics]] and [[pharmacokinetics]] of estradiol in the context of use in birth control pills have been studied and reviewed.<ref name="pmid8240460">{{cite journal | vauthors = Kuhnz W, Gansau C, Mahler M | title = Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17β-estradiol | journal = Arzneimittelforschung | volume = 43 | issue = 9 | pages = 966–73 | date = September 1993 | issn = 0004-4172 | pmid = 8240460 | doi = | url = }}</ref><ref name="pmid23375353" /><ref name="JensenBitzer2013">{{cite journal|last1=Jensen|first1=Jeffrey|last2=Bitzer|first2=Johannes|last3=Serrani|first3=Marco|title=Comparison of the pharmacologic and clinical profiles of new combined oral contraceptives containing estradiol|journal=Open Access Journal of Contraception|year=2013|pages=39|issn=1179-1527|doi=10.2147/OAJC.S50693|url=https://www.researchgate.net/profile/Jeffrey_Jensen2/publication/274274938_Comparison_of_the_pharmacologic_and_clinical_profiles_of_new_combined_oral_contraceptives_containing_estradiol/links/576c1ac308aef0e50da8c20b/Comparison-of-the-pharmacologic-and-clinical-profiles-of-new-combined-oral-contraceptives-containing-estradiol.pdf}}</ref>


==Research==
==Research==

Revision as of 06:18, 27 December 2019

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

Combined birth control pills that contain natural estradiol or an estradiol ester (e.g., estradiol valerate) include:[1][2][3]

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]

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.[10][2][8]

Research

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

See also

References

  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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  6. ^ http://www.wjpps.com/download/article/1412071798.pdf
  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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  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.


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