Combined birth control pill
The combined oral contraceptive pill (COCP), often referred to as the birth control pill or colloquially as "the pill", is a type of birth control that is designed to be taken orally by women. The pill contains two important hormones: progesti ...
s that contain natural
estradiol or an
estradiol ester (e.g.,
estradiol valerate) include:
*
Estradiol valerate and
cyproterone acetate (brand name
Femilar) – introduced in
Finland
Finland ( fi, Suomi ; sv, Finland ), officially the Republic of Finland (; ), is a Nordic country in Northern Europe. It shares land borders with Sweden to the northwest, Norway to the north, and Russia to the east, with the Gulf of B ...
(only) in 1993
* Estradiol valerate and
dienogest (brand names Qlaira, Natazia) – introduced in
Europe
Europe is a large peninsula conventionally considered a continent in its own right because of its great physical size and the weight of its history and traditions. Europe is also considered a Continent#Subcontinents, subcontinent of Eurasia ...
in 2009 and the in 2010
*
Estradiol and
nomegestrol acetate (brand name Zoely) – introduced in Europe in 2011
Estradiol, mainly as esters including estradiol valerate,
estradiol cypionate, and
estradiol enanthate
Estradiol enantate (EEn or E2-EN), also spelled estradiol enanthate and sold under the brand names Perlutal and Topasel among others, is an estrogen medication which is used in hormonal birth control for women. It is formulated in combination wi ...
, is also the exclusive estrogen used in
combined injectable contraceptive
Combined injectable contraceptives (CICs) are a form of hormonal birth control for women. They consist of monthly injections of combined formulations containing an estrogen and a progestin to prevent pregnancy.
CICs are different from progestoge ...
s.
As of 2021, more than 95% of prescriptions are for combined hormonal birth control forms containing the
synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to:
Science
* Synthetic chemical or compound, produced by the process of chemical synthesis
* Synthetic o ...
estrogen
ethinylestradiol (EE).
Hence, estradiol-based birth control pills are still not widely used.
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
Venous thrombosis is blockage of a vein caused by a thrombus (blood clot). A common form of venous thrombosis is deep vein thrombosis (DVT), when a blood clot forms in the deep veins. If a thrombus breaks off (embolizes) and flows to the lungs to ...
(VTE).
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.
The risk of VTE with
estradiol/nomegestrol acetate
Nomegestrol acetate/estradiol (NOMAC-E2), sold under the brand names Naemis and Zoely among others, is a fixed-dose combination medication of nomegestrol acetate, a progestogen, and estradiol, an estrogen, which is used in menopausal hormone ther ...
birth control pills is under study.
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
The endometrium is the inner epithelial layer, along with its mucous membrane, of the mammalian uterus. It has a basal layer and a functional layer: the basal layer contains stem cells which regenerate the functional layer. The functional laye ...
.
Pharmacology
The
pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (fo ...
and
pharmacokinetics
Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered ...
of estradiol in the context of use in birth control pills have been studied and reviewed.
Research
Experimental estradiol-containing birth control pills that were studied but never marketed include:
*
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
A randomized controlled trial (or randomized control trial; RCT) is a form of scientific experiment used to control factors not under direct experimental control. Examples of RCTs are clinical trials that compare the effects of drugs, surgical te ...
of a
birth control pill containing
ethinylestradiol/norethisterone acetate
Ethinylestradiol/norethisterone acetate (EE/NETA), or ethinylestradiol/norethindrone acetate, is a combination of ethinylestradiol (EE) and norethisterone acetate (NETA) which is used as birth control and menopausal hormone therapy. EE is an e ...
versus a birth control pill containing
estradiol/estriol/norethisterone acetate has been conducted.
See also
*
Birth control pill formulations
Birth control pills come in a variety of formulations. The main division is between combined oral contraceptive pills, containing both estrogens and synthetic progestogens (progestins), and progestogen only pills. Combined oral contraceptive pills ...
*
Estetrol/drospirenone
Drospirenone/estetrol, sold under the brand name Nextstellis among others, is a fixed-dose combination medication containing drospirenone, a progestin, and estetrol, an estrogen, which is used as a combined birth control pill for the prevention of ...
References
{{Progesterone receptor modulators
Estradiol
Estrogens
Hormonal contraception
Progestogens