Formation of Ethinyl Estradiol in Women during Treatment with Norethindrone Acetate
Abstract
CONTEXT: The significance of the conversion of norethindrone acetate (NET-A), a commonly prescribed, synthetic, oral progestogen, to ethinyl estradiol (EE(2)) is controversial. OBJECTIVE: We sought to determine accurately the extent to which NET-A may be converted to EE(2), and if so, whether circulating levels of EE(2) would be of clinical significance. DESIGN, SUBJECTS, AND INTERVENTIONS: We administered NET-A 10, 20, or 40 mg once daily for 7 d to 20 regularly menstruating premenopausal women and measured NET-A and EE(2) levels before drug intake; at 1, 2, 4, 8, and 24 h after the first dose; and 2 h after the seventh dose. RESULTS: The mean EE(2) maximum serum concentration obtained from the 10-, 20-, and 40-mg doses of NET-A in this study is 58, 178, and 231 pg/ml, respectively. The conversion ratio of NET-A to EE(2) ranged from 0.20 to 0.33% for the different doses. CONCLUSIONS: NET-A is converted to EE(2), and although the conversion rate is relatively small, higher doses of NET-A, as used clinically, give rise to substantial levels of EE(2).
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NETA is partly metabolized to estrogens, with positive effects on bone metabolism.
“In addition, NETA is partly metabolized to estrogens [17,18], with subsequent positive effects on bone metabolism.”
From Oral and depot progestin therapy for endometriosis: towards a personalized medicine (2017) · cites this paper as [17]
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- Authors
- Chu, M. C., Zhang, X., Gentzschein, E., Stanczyk, F. Z., & Lobo, R. A.
- Affiliations
- Columbia University (US)
- University of Southern California (US)
- ORCID
- Stanczyk, Frank Z.
- Venue
- The Journal of Clinical Endocrinology & Metabolism
- Publisher
- The Endocrine Society
- Published
- 2007-06
- Volume
- 92
- Issue
- 6
- Pages
- 2205-2207
- ISSN
- 0021-972X (ISSN-L)
- 1945-7197
- OpenAlex
- W2054703956
- Cited by
- 100
- References
- 9
- Citations by year
- 2026: 5 · 2025: 7 · 2024: 7 · 2023: 8 · 2022: 10 · 2021: 6 · 2020: 8 · 2019: 3 · 2018: 6 · 2017: 4 · 2016: 5 · 2015: 6 · 2014: 1 · 2013: 2 · 2012: 6
- FWCI
- 3.78
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- The Journal of Clinical Endocrinology & Metabolism (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Effects and risks of endocrine disrupting chemicals
- Keywords
- norethindrone acetate, ethinyl estradiol, oral contraceptives, premenopausal women, serum estradiol levels
- MeSH terms
- Norethindrone Acetate, Adult, Contraceptives, Oral, Synthetic, Ethinyl Estradiol, Female, Humans, Norethindrone, Premenopause, Area Under Curve
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