Evolution and innovation among estrogens

Tyan O.V.

Main
Publications
Evolution and innovation among estrogens

May 16, 2024

299

Obstetrics and Gynecology

Tyan O.V.

УДК: 613.888

DOI: 10.32471/umj.1680-3051.161.254053

Keywords :

combined oral contraception,

hormonal contraception,

Дровеліс,

естетрол

Specialities :

Obstetrics and Gynecology

Resume

The estrogen component in combined oral contraceptives provides sufficient control of the cycle, enhances contraceptive effect, but on the other hand, it is the main risk factor for the development of undesirable effects like: fluid retention, effect on hemostasis, lipids, carbohydrates, libido. The launch of the new estrogen — estetrol among combined oral contraceptions is an innovative solution for both doctors and women. Estetrol E4 is the only natural, selective estrogen with specific agonistic or antagonistic activity in tissues (Native Estrogen with Selective Tissue activity — NEST) due to a special interaction more with nuclear estrogen receptors than with membrane ones. The effects of estetrol E4 are realized without influence on metabolism in the liver through the cytochrome P450 system, so there is no formation of «active» metabolites, increasing proliferation and without a negative effect on the genome. Estetrol E4 has no effect on the synthesis of transport proteins of cortisol and testosterone in the liver, on c-reactive protein, on aldosterone, therefore, a neutral effect on weight, blood pressure, libido and rheological properties of blood are noted. The pharmacological properties of E4 make it beneficial for hormonal therapy and contraception (Drovelis).

References

1. Abou-Ismail M., Sridhar D., Nayak L. (2020) Estrogen and thrombosis: a bench to bedside review. Thromb. Res., 192: 40–51.
2. Adeel M., Song X., Wang Y. et al. (2017) Environmental impact of estrogens on human, animal and plant life: a critical review. Environ. Int., 99: 107–119. doi: 10.1016/j.envint.2016.12.010.
3. Archer D.F., Mansour D., Foidart J.M. (2022) Bleeding patterns of oral contraceptives with a cyclic dosing regimen: an overview. J. Clin. Med., 11(4634): 1–15. doi: 10.3390/jcm11154634.
4. Creinin M.D., Cagnacci A., Spaczyński R.Z. et al. (2024) Experts’ view on the role of oestrogens in combined oral contraceptives: emphasis on oestetrol (E4). Front. Glob. Womens Health, 5: 1395863. doi: 10.3389/fgwh.2024.1395863.
5. Douxfils J., Bouvy C., Morimont L. (2023) Evaluation of activated protein C resistance using thrombin generation test. Methods Mol. Biol., 2663: 211–224. doi: 10. 1007/978-1-0716-3175-1_12.
6. DrugBank. Ethinylestradiol. DrugBank Online. (2022) go.drugbank.com/drugs/DB00977.
7. Foidart J.M., Gaspard U., Pequeux C. et al. (2019) Unique vascular benefits of estetrol, a native fetal estrogen with specific actions in tissues (NEST). In: Brinton R., Genazzani A., Simoncini T., Stevenson J. (Eds.) Sex Steroids’ Effects on Brain, Heart and Vessels ISGE Series. Cham: Springer. p. 169–195. http://www.researchgate.net/publication/333465497_Unique_Vascular_Benefits_of_Estetrol_a_Native_Fetal_Estrogen_with_Specific_Actions_in_Tissues_NEST.
8. Gemzell-Danielsson K., Cagnacci A., Chabbert-Buffet N. et al. (2022) A novel estetrol-containing combined oral contraceptive: European expert panel review. Eur. J. Contracept. Reprod. Health Care, 27: 373–383.
9. Gialeraki A., Valsami S., Pittaras T. et al. (2018) Oral contraceptives and HRT risk of thrombosis. Clin. Appl. Thromb., 24(2): 217–225. doi: 10.1177/1076029616683802.
10. Heikinheimo O., Toffol E., Partonen T. et al. (2022) Systemic hormonal contraception and risk of venous thromboembolism. Acta Obstet. Gynecol. Scand., 101(8): 846–855. doi: 10.1111/aogs.14384.
11. Mukherjee T.K., Reynolds P.R., Hoidal J.R. (2005) Differential effect of estrogen receptor alpha and beta agonists on the receptor for advanced glycation end product expression in human microvascular endothelial cells. Biochim. Biophys. Acta, 1745 (3): 300–309. doi: 10.1016/j.bbamcr.2005.03.012.
12. Nappi R.E., Tiranini L., Sacco S. et al. (2022) Role of estrogens in menstrual migraine. Cells, 11: 18–25. doi: 10.3390/cells11081355.
13. Rogan E.G., Badawi A.F., Devanesan P.D. et al. (2003) Estrogen metabolism and risk of brest cancer: a prospective study of the 2:26alfa- hydroxyestrone ratio in premenopausal and postmenopausal women. Carcinogenesis, 24(4): 697–702.
14. Seidman L., Kroll R., Howard B. et al. (2015) Ovulatory effects of three oral contraceptive regimens: a randomized, open-label, descriptive trial. Contraception, 91(6): 495–502. doi: 10.1016/j.contraception.2015.03.001.
15. Sitruk-Ware R., Nath A. (2011) Metabolic effects of contraceptive steroids. Rev. Endocr. Metab. Disord., 12(2): 63–75. doi: 10.1007/s11154-011-9182-4.
16. Speroff L. (1982) The formulation of oral contraceptives: does the amount of estrogen make any clinical difference? Johns Hopkins Med. J., 150(5): 170–176.
17. Tang Z., Liu Z.H., Wang H. et al. (2021) A review of 17α-ethynylestradiol (EE2) in surface water across 32 countries: sources, concentrations, and potential estrogenic effects. J. Environ. Manage, 292: 112804. doi: 10.1016/j.jenvman.2021.112804.
18. Yu K., Huang Z.Y., Xu X.L. et al. (2022) Estrogen receptor function: impact on the human endometrium. Front Endocrinol (Lausanne), 13: 827724. doi: 10.3389/fendo.2022.827724.