Cited by 201Reproductive Health and ContraceptionEstrogen and related hormone effectsMenopause: Health Impacts and Treatments

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Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment

Stanczyk, Frank Z., Archer, David F., Bhavnani, Bhagu R.·2013·Contraception

DOI 10.1016/j.contraception.2012.12.011

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Abstract

The need to seek improved combined oral contraceptive (COC) efficacy, with fewer health risks and better acceptability, has been ongoing since the introduction of COCs more than 50 years ago. New progestin formulations combined with lower doses of ethinyl estradiol (EE), the predominant estrogenic component of COCs, have reduced the incidence of venous thromboembolism and other negative outcomes of COC treatment. Previous attempts to use endogenous 17β-estradiol (E₂) instead of EE were limited primarily by poor cycle control. The recent introduction of E₂-based formulations has renewed interest to determine if there are potential benefits of using E₂ in COCs. These formulations have been shown to have similar efficacy and cycle control as EE-based COCs. This review provides a brief summary of the pharmacology of EE and E₂, including metabolism, pharmacokinetics and pharmacodynamics, as well as adverse effects of these estrogens.

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Authors: Stanczyk, F. Z., Archer, D. F., & Bhavnani, B. R.
Affiliations: University of Southern California (US)
Eastern Virginia Medical School (US)
St. Michael's Hospital (CA)
ORCID: Stanczyk, Frank Z.
Archer, David F.
Venue: Contraception
Publisher: Elsevier BV
Published: 2013-06
Volume: 87
Issue: 6
Pages: 706-727
ISSN: 0010-7824 (ISSN-L)
DOI: 10.1016/j.contraception.2012.12.011
OpenAlex: W2072831812
Cited by: 201
References: 268
Citations by year: 2026: 14 · 2025: 17 · 2024: 29 · 2023: 18 · 2022: 25 · 2021: 25 · 2020: 16 · 2019: 12 · 2018: 9 · 2017: 8 · 2016: 4 · 2015: 11 · 2014: 10 · 2013: 2
FWCI: 1.29
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Contraception (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
Keywords: ethinyl estradiol, estradiol, combined oral contraceptives, estrogen metabolism, endogenous estradiol, venous thromboembolism, cycle control, contraceptive efficacy, risk assessment
MeSH terms: Contraceptives, Oral, Combined, Dose-Response Relationship, Drug, Drug Interactions, Estradiol, Estrogens, Ethinyl Estradiol, Female, Humans, Menstrual Cycle, Progestins, Progesterone, Risk Assessment

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Ethinyl estradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment

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