Comparison of pharmacodynamic properties of various estrogen formulations
Abstract
A group of 23 healthy postmenopausal women received one or more 2-week courses of daily administration of the following estrogen preparations: piperazine estrone sulfate (Ogen), 0.3, 0.625, 1.25, 2.5, and 5.0 mg; micronized estradiol (Estrace), 1, 2, and 10 mg; conjugated estrogens (Premarin), 0.3, 0.625, 1.25, and 2.5 mg; ethinyl estradiol (Estinyl), 10 and 20 micrograms; and diethylstilbestrol, 0.1 and 0.5 mg. Each dosage of each formulation was ingested by three women. In those women who received more than one dosage, each course was separated by a drug-free interval of at least 4 weeks. Pretreatment and posttreatment levels of follicle-stimulating hormone (FSH), luteinizing hormone (LH), corticosteroid-binding globulin-binding capacity, sex hormone-binding globulin-binding capacity, angiotensinogen, estrone, and estradiol were determined. The relative potency of these five estrogen formulations was determined by parallel line analysis for each of these responses, except LH. On a weight basis, piperazine estrone sulfate and micronized estradiol were equipotent for all responses. Conjugated estrogens suppressed FSH in a fashion equipotent to that of the other nonsynthetic estrogens; however, for all three hepatic parameters, the response was exaggerated twofold to threefold. The synthetic estrogens, diethylstilbestrol and ethinyl estradiol, were relatively more potent on a weight basis for every response and produced the most marked response (fourfold to eighteenfold in excess of their FSH suppression) for the hepatic parameters.
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Ethinylestradiol is a potent estrogen having up to 600 times greater effect on hepatic protein synthesis than natural estradiol (E2).
“It is a potent estrogen having up to 600 times greater effect on hepatic protein synthesis than natural estradiol (E2)”
From Ethinylestradiol in combined hormonal contraceptive has a broader effect on serum proteome compared with estradiol valerate: a randomized controlled trial (2023) · cites this paper as Mashchak et al., 1982
In the liver, combined oral contraceptives stimulate the synthesis of steroid-binding globulins, such as sex hormone-binding globulin (SHBG), thereby affecting circulating free steroid levels.
“In the liver, COCs stimulate the synthesis of steroid-binding globulins, such as sex hormone-binding globulin (SHBG), thereby affecting circulating, free steroid levels”
From Ethinylestradiol in combined hormonal contraceptive has a broader effect on serum proteome compared with estradiol valerate: a randomized controlled trial (2023) · cites this paper as Mashchak et al., 1982
EE increases SHBG, CBG and angiotensinogen multifold compared with estradiol.
“EE increases SHBG, CBG and angiotensinogen multifold compared with estradiol (Mashchak et al., 1982).”
From Ethinylestradiol in combined hormonal contraceptive has a broader effect on serum proteome compared with estradiol valerate: a randomized controlled trial (2023) · cites this paper as Mashchak et al., 1982
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- Authors
- Mashchak, C. A., Lobo, R. A., Dozono-Takano, R., Eggena, P., Nakamura, R. M., Brenner, P. F., & Mishell, D. R.
- Affiliations
- University of Southern California (US)
- Corresponding author
- Mishell, Daniel R.
- Venue
- American Journal of Obstetrics and Gynecology
- Publisher
- Elsevier BV
- Published
- 1982-11
- Volume
- 144
- Issue
- 5
- Pages
- 511-518
- ISSN
- 0002-9378 (ISSN-L)
- OpenAlex
- W1593764750
- Cited by
- 316
- References
- 10
- Citations by year
- 2026: 2 · 2025: 8 · 2024: 5 · 2023: 5 · 2022: 11 · 2021: 8 · 2020: 7 · 2019: 1 · 2018: 5 · 2017: 10 · 2016: 4 · 2015: 13 · 2014: 3 · 2013: 10 · 2012: 15
- FWCI
- 2.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- American Journal of Obstetrics and Gynecology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
- Health Sciences › Medicine › Pathology and Forensic Medicine › Phytoestrogen effects and research
- Keywords
- pharmacodynamics, postmenopausal women, micronized estradiol, conjugated estrogens, ethinyl estradiol, diethylstilbestrol, luteinizing hormone, sex hormone-binding globulin, corticosteroid-binding globulin, angiotensinogen, estrone, estradiol, relative potency, synthetic estrogens
- MeSH terms
- Angiotensinogen, Diethylstilbestrol, Estradiol, Estrogens, Conjugated (USP), Estrogens, Estrone, Ethinyl Estradiol, Female, Follicle Stimulating Hormone, Humans, Luteinizing Hormone, Menopause, Sex Hormone-Binding Globulin, Transcortin
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