Pharmacodynamics of combined estrogen-progestin oral contraceptives: Effects on metabolism
Abstract
INTRODUCTION: The pharmacodynamic effects of various combined oral estrogen-progestin combinations (COC) are examined for their components alone or in the various combined formulations. Special emphasis is given to products containing natural estrogens. Areas covered: Recent information on the effect of androgens, estrogens, progestins, as well as various COC combinations on the coagulation cascade will be reviewed aiming at providing an updated picture. The present article reviews hemostatic changes occurring during use of classic and modern combinations of estrogens (ethinyl estradiol, estradiol, estradiol valerate and estetrol) and new progestins (desogestrel, gestodene, dienogest, drospirenone, nomegestrol acetate), compared to classic compounds, such as levonorgestrel. Both pro- and anti-coagulatory effects of COC in healthy women are detailed and possible links with incidence of thromboembolic events are discussed. Expert commentary: Overall, the picture is reassuring: the use of natural estrogens and of new generation progestins has reduced pro-coagulatory changes in healthy subjects, although the observed differences in the risk of venous thromboembolism between second and third generation progestins is still incompletely understood. At the same time, there still is a need for large comparative and surveillance studies before firm conclusions can be drawn. At any rate, available evidence indicates that hemostatic effects of the newer COC, especially those utilizing natural estrogens, are minimal and often remain with the normal range.
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The type of progestin used in COCs determines their endocrine and metabolic effects.
“The type of progestin used in COCs also determines their endocrine and metabolic effects.”
From Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone (2021) · cites this paper as [7]
Newer progestins such as drospirenone (DRSP) bind more specifically to the progesterone receptor.
“The newer progestins such as drospirenone (DRSP) bind more specifically to the progesterone receptor.”
From Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone (2021) · cites this paper as [7]
DRSP maintains contraceptive efficacy.
“This results in a reduction in androgenic, estrogenic, and glucocorticoid-related side effects, and a more neutral effect on metabolic parameters [7] , while maintaining contraceptive efficacy.”
From Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone (2021) · cites this paper as [7]
DRSP results in a reduction in androgenic, estrogenic, and glucocorticoid-related side effects.
“This results in a reduction in androgenic, estrogenic, and glucocorticoid-related side effects, and a more neutral effect on metabolic parameters [7] , while maintaining contraceptive efficacy.”
From Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone (2021) · cites this paper as [7]
DRSP has a more neutral effect on metabolic parameters.
“This results in a reduction in androgenic, estrogenic, and glucocorticoid-related side effects, and a more neutral effect on metabolic parameters [7] , while maintaining contraceptive efficacy.”
From Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone (2021) · cites this paper as [7]
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- Authors
- Bastianelli, C., Farris, M., Rosato, E., Brosens, I., & Benagiano, G.
- Affiliations
- Sapienza University of Rome (IT)
- Leuven Institute for Fertility and Embryology (BE)
- Corresponding author
- Farris, Manuela
- Venue
- Expert Review of Clinical Pharmacology
- Publisher
- Informa UK Limited
- Published
- 2016-12-15
- Volume
- 10
- Issue
- 10
- Pages
- 1129-1144
- ISSN
- 1751-2433 (ISSN-L)
- 1751-2441
- OpenAlex
- W2560857678
- Cited by
- 50
- References
- 9
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 3 · 2023: 13 · 2022: 3 · 2021: 8 · 2020: 8 · 2019: 6 · 2018: 2 · 2017: 3
- FWCI
- 3.65
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Review of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- IRIS Research product catalog (Sapienza University of Rome) (submittedVersion)
- Topics
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Health Sciences › Medicine › Internal Medicine › Venous Thromboembolism Diagnosis and Management
- Health Sciences › Medicine › Hematology › Blood Coagulation and Thrombosis Mechanisms
- Keywords
- combined oral contraceptives, estrogen-progestin combination, pharmacodynamics, coagulation, hemostasis, thromboembolism, venous thromboembolism risk, natural estrogens, ethinyl estradiol, estradiol valerate, estetrol, progestins, desogestrel, gestodene, dienogest, drospirenone, nomegestrol acetate, levonorgestrel, androgens
- MeSH terms
- Contraceptives, Oral, Combined, Contraceptives, Oral, Hormonal, Estrogens, Female, Humans, Progestins, Bone Density, Carbohydrate Metabolism, Lipid Metabolism
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