The site of the Media Sphera Publishers contains materials intended solely for healthcare professionals.
By closing this message, you confirm that you are a certified medical professional or a student of a medical educational institution.

Deryabina E.G.

Ural Research Institute for Maternal and Child Care

Ethinylestradiol and oral contraception: what we know after 60 years of use? (a review)

Authors:

Deryabina E.G.

More about the authors

Journal: Russian Journal of Human Reproduction. 2024;30(4): 90‑100

Read: 1529 times


To cite this article:

Deryabina EG. Ethinylestradiol and oral contraception: what we know after 60 years of use? (a review). Russian Journal of Human Reproduction. 2024;30(4):90‑100. (In Russ.)
https://doi.org/10.17116/repro20243004190

Recommended articles:
Hormonal contraception methods and multiple scle­rosis. S.S. Korsakov Journal of Neurology and Psychiatry. 2025;(1):24-30

References:

  1. United Nations, Department of Economic and Social Affairs, Population Division (2019). Contraceptive Use by Method 2019. Data Booklet (ST/ESA/SER.A/435). Published online 2019. Accessed June 14, 2024. https://www.un.org/development/desa/pd/sites/www.un.org.development.desa.pd/files/files/documents/2020/Jan/un_2019_contraceptiveusebymethod_databooklet.pdf
  2. Federalnaya sluzhba gosudarstvennoj statistiki. Zdravooxranenie v Rossii-2021. 2.37. Ispolzovanie sredstv kontracepcii. Accessed June 14, 2024. (In Russ.). https://gks.ru/bgd/regl/b21_34/Main.htm
  3. Natsionalnye meditsinskie kriterii priemlemosti metodov kontratseptsii. Adaptirovannyy document «Meditsinskie kriterii priemlemosti ispolzovaniya metodov kontratseptsii VOZ, 5 izdanie, 2015». M. 2023. Accessed June 14, 2024. (In Russ.). https://roag-portal.ru/news-76
  4. Mansour D. Qlaira: a «natural» change of direction. Journal of Family Planning and Reproductive Health Care. 2009;35(3):139-142.  https://doi.org/10.1783/147118909788707878
  5. Yang LPH, Plosker GL. Nomegestrol Acetate/Estradiol. Drugs. 2012;72(14):1917-1928. https://doi.org/10.2165/11208180-000000000-00000
  6. Lee A, Syed YY. Estetrol/Drospirenone: a review in oral contraception. Drugs. 2022;82(10):1117-1125. https://doi.org/10.1007/s40265-022-01738-8
  7. Ministerstvo zdravookhraneniia Rossiiskoi Federatsii. Gosudarstvennyi reestr lekarstvennykh sredstv. Accessed June 14, 2024. (In Russ.). https://grls.rosminzdrav.ru/grls.aspx
  8. Estrogen and Progestogen Drugs. Accessed June 14, 2024. https://www.chemsrc.com/en/Catg/187.html
  9. Perone N. The history of steroidal contraceptive development: the progestins. Perspectives in Biology and Medicine. 1993;36(3):347-362.  https://doi.org/10.1353/pbm.1993.0054
  10. Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. 2005;8(sup1):3-63.  https://doi.org/10.1080/13697130500148875
  11. Goldzieher JW, Stanczyk FZ. Oral contraceptives and individual variability of circulating levels of ethinyl estradiol and progestins. Contraception. 2008;78(1):4-9.  https://doi.org/10.1016/j.contraception.2008.02.020
  12. Makepeace AW, Weinstein GL, Friedman MH. The effect of progestin and progesterone on ovulation in the rabbit. American Journal of Physiology — Legacy Content. 1937;119(3):512-516.  https://doi.org/10.1152/ajplegacy.1937.119.3.512
  13. Djerassi C, Miramontes L, Rosenkranz G, Sondheimer F, Longo LD. Steroids LIV. Synthesis of 19-nor-17α-ethynyltestosterone and 19-nor-17α-methyltestosterone. 1954. American Journal of Obstetrics and Gynecology. 2006;194(1):289-290.  https://doi.org/10.1016/j.ajog.2005.02.118
  14. Colton FB. Steroids and «the pill»: early steroid research at Searle. Steroids. 1992;57(12):624-630.  https://doi.org/10.1016/0039-128x(92)90015-2
  15. Pincus G. The hormonal control of ovulation and early development. Postgraduate Medicine. 1958;24(6):654-660.  https://doi.org/10.1080/00325481.1958.11692305
  16. Stanczyk FZ, Archer DF, Bhavnani BR. Ethinylestradiol and 17β-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception. 2013;87(6):706-727.  https://doi.org/10.1016/j.contraception.2012.12.011
  17. Inman WHW, Vessey MP, Westerholm B, Engelund A. Thromboembolic disease and the steroidal content of oral contraceptives. A Report to the Committee on Safety of Drugs. BMJ.1970;2(5703):203-209.  https://doi.org/10.1136/bmj.2.5703.203
  18. Kangasniemi MH, Arffman RK, Joenväärä S, Haverinen A, Luiro K, Tohmola T, Renkonen R, Heikinheimo O, Tapanainen JS, Piltonen TT. Ethinylestradiol in combined hormonal contraceptive has a broader effect on serum proteome compared with estradiol valerate: a randomized controlled trial. Human Reproduction. 2023;38(1):89-102.  https://doi.org/10.1093/humrep/deac250
  19. Cauci S, Xodo S, Buligan C, Colaninno C, Barbina M, Barbina G, Francescato MP. Oxidative Stress Is Increased in Combined Oral contraceptives users and is positively associated with high-sensitivity C-reactive protein. Molecules. 2021;26(4):1070. https://doi.org/10.3390/molecules26041070
  20. Pírek O, Budinskaya K, Nováková Z. Effects of peroral hormonal contraception on cardiovascular system: analysis of selected cardiovascular parameters in an adolescent cohort; a pilot project. Physiological Research. 2022;71(suppl 2):S203-S210. https://doi.org/10.33549/physiolres.934997
  21. Fotherby K, Akpoviroro J, Abdel-Rahman HA, Toppozada HK, de Souza JC, Coutinho EM, Koetsawang S, Nukulkarn P, Sheth UK, Mapa MK, Gopalan S, Plunkett ER, Brenner PF, Hickey MV, Grech ES, Lichtenberg R, Gual C, Molina R, Gomez-Rogers C, Kwon E, Kim SW, Chan T, Ratnam SS, Landgren BM, Shearman RP, Goldzieher JW, Dozier TS.Pharmacokinetics of ethynyloestradiol in women from different populations. Contraception. 1981;23(5):487-496.  https://doi.org/10.1016/0010-7824(81)90076-7
  22. Sitruk-Ware R, Plu-Bureau G, Menard J, Conard J, Kumar S, Thalabard JC, Tokay B, Bouchard P. Effects of oral and transvaginal ethinyl estradiol on hemostatic factors and hepatic proteins in a randomized, crossover study. The Journal of Clinical Endocrinology and Metabolism. 2007;92(6):2074-2079. https://doi.org/10.1210/jc.2007-0026
  23. de Bastos M, Stegeman BH, Rosendaal FR, Van Hylckama Vlieg A, Helmerhorst FM, Stijnen T, Dekkers OM. Combined oral contraceptives: venous thrombosis. The Cochrane Database of Systematic Reviews. 2014;(3):CD010813. https://doi.org/10.1002/14651858.CD010813.pub2
  24. Dinger JC, Bardenheuer K, Assmann A. International Active Surveillance Study of Women Taking Oral Contraceptives (INAS-OC Study). BMC Medical Research Methodology. 2009;9(1):77.  https://doi.org/10.1186/1471-2288-9-77
  25. Christin-Maitre S. History of oral contraceptive drugs and their use worldwide. Best Practice and Research. Clinical Endocrinology and Metabolism. 2013;27(1):3-12.  https://doi.org/10.1016/j.beem.2012.11.004
  26. Weill A, Dalichampt M, Raguideau F, Ricordeau P, Blotière PO, Rudant J, Alla F, Zureik M. Low dose oestrogen combined oral contraception and risk of pulmonary embolism, stroke, and myocardial infarction in five million French women: cohort study. BMJ. 2016;353:i2002. https://doi.org/10.1136/bmj.i2002
  27. Rodrigues AD. Drug interactions involving 17α‐Ethinylestradiol: considerations beyond cytochrome P450 3A induction and inhibition. Clinical Pharmacology and Therapeutics. 2022;111(6):1212-1221. https://doi.org/10.1002/cpt.2383
  28. Wang Q, Würtz P, Auro K, Morin-Papunen L, Kangas AJ, Soininen P, Tiainen M, Tynkkynen T, Joensuu A, Havulinna AS, Aalto K, Salmi M, Blankenberg S, Zeller T, Viikari J, Kähönen M, Lehtimäki T, Salomaa V, Jalkanen S, Järvelin MR, Perola M, Raitakari OT, Lawlor DA, Kettunen J, Ala-Korpela M. Effects of hormonal contraception on systemic metabolism: cross-sectional and longitudinal evidence. International Journal of Epidemiology. 2016;45(5):1445-1457. https://doi.org/10.1093/ije/dyw147
  29. Medical Eligibility Criteria for Contraceptive Use. 5th ed. Geneva: World Health Organization; 2015. Accessed June 14, 2024. https://www.ncbi.nlm.nih.gov/books/NBK321151/
  30. Plu-Bureau G, Maitrot-Mantelet L, Hugon-Rodin J, Canonico M. Hormonal contraceptives and venous thromboembolism: an epidemiological update. Best Practice and Research. Clinical Endocrinology and Metabolism. 2013;27(1):25-34.  https://doi.org/10.1016/j.beem.2012.11.002
  31. Redmond G, Godwin AJ, Olson W, Lippman JS. Use of placebo controls in an oral contraceptive trial: methodological issues and adverse event incidence. Contraception. 1999;60(2):81-85.  https://doi.org/10.1016/S0010-7824(99)00069-4
  32. Kwiecien M, Edelman A, Nichols MD, Jensen JT. Bleeding patterns and patient acceptability of standard or continuous dosing regimens of a low-dose oral contraceptive: a randomized trial. Contraception. 2003;67(1):9-13.  https://doi.org/10.1016/S0010-7824(02)00445-6
  33. Shere M, Bapat P, Nickel C, Kapur B, Koren G. The effectiveness of folate-fortified oral contraceptives in maintaining optimal folate levels to protect against neural tube defects: a systematic review. Journal of Obstetrics and Gynaecology Canada. 2015;37(6):527-533.  https://doi.org/10.1016/S1701-2163(15)30229-2
  34. Adamyan LV, Andreeva EN, Absatarova YuS, Grigoryan OR, Dedov II, Mel’nichenko GA, Suturina LV, Filippov OS, Sheremetyeva EV, Chernukha GE,Yarmolinskaya MI. Clinical guidelines «Polycystic ovary syndrome». Problemy endokrinologii. 2022;68(2):112-127. (In Russ.). https://doi.org/10.14341/probl12874
  35. Endometrioz. Klinicheskie rekomendatsii. 2020. Odobreno Nauchno-prakticheskim Sovetom Ministerstva zdravooxraneniya Rossijskoj Federacii. Accessed June 14, 2024. (In Russ.). https://cr.minzdrav.gov.ru/schema/259_1#doc_a3
  36. Vigil P, Meléndez J, Petkovic G, Del Río JP. The importance of estradiol for body weight regulation in women. Frontiers in Endocrinology. 2022;13:951186. https://doi.org/10.3389/fendo.2022.951186
  37. Gallo MF, Lopez LM, Grimes DA, Carayon F, Schulz KF, Helmerhorst FM. Combination contraceptives: effects on weight. The Cochrane Database of Systematic Reviews. 2014;(1):CD003987. https://doi.org/10.1002/14651858.CD003987.pub5
  38. Edelman AB, Cherala G, Munar MY, McInnis M, Stanczyk FZ, Jensen JT. Correcting oral contraceptive pharmacokinetic alterations due to obesity: a randomized controlled trial. Contraception. 2014;90(5):550-556.  https://doi.org/10.1016/j.contraception.2014.06.033
  39. Jugdutt BI, Stevens GF, Zacks DJ, Lee SJK, Taylor RF. Myocardial infarction, oral contraception, cigarette smoking, and coronary artery spasm in young women. American Heart Journal. 1983;106(4):757-761.  https://doi.org/10.1016/0002-8703(83)90100-X
  40. Sirmans SM, Pate KA. Epidemiology, diagnosis, and management of polycystic ovary syndrome. Journal of Clinical Epidemiology. 2013;6:1-13.2013. https://doi.org/10.2147/CLEP.S37559
  41. Rimm EB, Manson JE, Stampfer MJ, Colditz GA, Willett WC, Rosner B, Hennekens CH, Speizer FE. Oral contraceptive use and the risk of Type 2 (non-insulin-dependent) diabetes mellitus in a large prospective study of women. Diabetologia. 1992;35(10):967-972.  https://doi.org/10.1007/BF00401427
  42. Lopez LM, Grimes DA, Schulz KF. Steroidal contraceptives: effect on carbohydrate metabolism in women without diabetes mellitus. The Cochrane Database of Systematic Reviews. 2019;(11):CD006133. https://doi.org/10.1002/14651858.CD006133.pub5
  43. Amiri M, Ramezani Tehrani F, Nahidi F, Kabir A, Azizi F, Carmina E. Effects of oral contraceptives on metabolic profile in women with polycystic ovary syndrome: A meta-analysis comparing products containing cyproterone acetate with third generation progestins. Metabolism. 2017;73:22-35.  https://doi.org/10.1016/j.metabol.2017.05.001
  44. Collaborative Group on Hormonal Factors in Breast Cancer. Breast cancer and hormonal contraceptives: collaborative reanalysis of individual data on 53 297 women with breast cancer and 100 239 women without breast cancer from 54 epidemiological studies. The Lancet. 1996;347(9017):1713-1727. https://doi.org/10.1016/S0140-6736(96)90806-5
  45. Harris ML, Feyissa TR, Bowden NA, Gemzell-Danielsson K, Loxton D. Contraceptive use and contraceptive counselling interventions for women of reproductive age with cancer: a systematic review and meta-analysis. BMC Medicine. 2022;20(1):489.  https://doi.org/10.1186/s12916-022-02690-w
  46. Iversen L, Sivasubramaniam S, Lee AJ, Fielding S, Hannaford PC. Lifetime cancer risk and combined oral contraceptives: the Royal College of General Practitioners’ Oral Contraception Study. American Journal of Obstetrics and Gynecology. 2017;216(6):580.e1-580.e9.  https://doi.org/10.1016/j.ajog.2017.02.002
  47. Asthana S, Busa V, Labani S. Oral contraceptives use and risk of cervical cancer— a systematic review and meta-analysis. European Journal of Obstetrics, Gynecology, and Reproductive Biology. 2020;247:163-175.  https://doi.org/10.1016/j.ejogrb.2020.02.014
  48. Cramer DW. The epidemiology of endometrial and ovarian Cancer. Hematology, Oncology Clinics of North America. 2012;26(1):1-12.  https://doi.org/10.1016/j.hoc.2011.10.009
  49. Michels KA, Pfeiffer RM, Brinton LA, Trabert B. Modification of the associations between Duration of oral contraceptive use and ovarian, endometrial, breast, and colorectal cancers. JAMA Oncology. 2018;4(4):516.  https://doi.org/10.1001/jamaoncol.2017.4942
  50. Hannaford PC, Iversen L, Macfarlane T V, Elliott AM, Angus V, Lee AJ. Mortality among contraceptive pill users: cohort evidence from Royal College of General Practitioners’ Oral Contraception Study. BMJ. 2010;340(mar11 1):c927-c927. https://doi.org/10.1136/bmj.c927
  51. Song J, Jin Z, Han H, Li M, Guo Y, Guo H, Guo W, He J. Hormone replacement therapies, oral contraceptives, reproductive factors and colorectal adenoma risk: a systematic review and dose — response meta‐analysis of observational studies. Colorectal Disease. 2019;21(7):748-759.  https://doi.org/10.1111/codi.14582
  52. Karim R, Dang H, Henderson VW, Hodis HN, St John J, Brinton RD, Mack WJ. Effect of reproductive history and exogenous hormone use on cognitive function in mid- and late life. Journal of the American Geriatrics Society. 2016;64(12):2448-2456. https://doi.org/10.1111/jgs.14658
  53. De Giglio L, Marinelli F, Barletta VT, Pagano VA, De Angelis F, Fanelli F, Petsas N, Pantano P, Tomassini V, Pozzilli C. Effect on cognition of estroprogestins combined with interferon beta in multiple sclerosis: analysis of secondary outcomes from a randomised controlled trial. CNS Drugs. 2017;31(2):161-168.  https://doi.org/10.1007/s40263-016-0401-0
  54. Organizaciya okazaniya medicinskoj pomoshchi beremennym, rozhenicam, rodil’nicam i novorozhdennym pri novoj koronavirusnoj infekcii COVID-19. Metodicheskie rekomendacii. Versiya 5 ot 28.12.2021. Ministerstvo Zdravookhraneniya Rossiyskoy Federatsii. 2021. Accessed June 14, 2024. (In Russ.). https://static-0.minzdrav.gov.ru/system/attachments/attaches/000/059/052/original/BMP_preg_5.pdf
  55. Costeira R, Lee KA, Murray B, Christiansen C, Castillo-Fernandez J, Ni Lochlainn M, Capdevila Pujol J, Macfarlane H, Kenny LC, Buchan I, Wolf J, Rymer J, Ourselin S, Steves CJ, Spector TD, Newson LR, Bell JT. Estrogen and COVID-19 symptoms: Associations in women from the COVID Symptom Study. PLoS One. 2021;16(9):e0257051. https://doi.org/10.1371/journal.pone.0257051
  56. Cohen MA, Edelman A, Paynter R, Henderson JT. Risk of thromboembolism in patients with COVID-19 who are using hormonal contraception. The Cochrane Database of Systematic Reviews. 2023;1(1):CD014908. https://doi.org/10.1002/14651858
  57. Official website. ClinicalTrials.gov. Accessed June 14, 2024. https://clinicaltrials.gov/

Email Confirmation

An email was sent to test@gmail.com with a confirmation link. Follow the link from the letter to complete the registration on the site.

Email Confirmation

We use cооkies to improve the performance of the site. By staying on our site, you agree to the terms of use of cооkies. To view our Privacy and Cookie Policy, please. click here.