Combined contraceptives – the choice of estrogen matters

1. Sech LA, Mishell DR Jr. Oral steroid contraception. Womens Health (Lond) 2015; 11 (6): 743–748. doi: 10.2217/whe.15.82.

2. Hannaford PC, Iversen L, Macfarlane TV et al. Mortality among contraceptive pill users: cohort evidence from Royal College of General Practitioners’ Oral Contraception Study. BMJ 2010; 340: c927. doi: 10.1136/bmj.c927.

3. Madden T, Secura GM, Nease RF et al. The role of contraceptive attributes in women’s contraceptive decision making. Am J Obstet Gynecol 2015; 213 (1): 46.e1–46.e6. doi: 10.1016/ j.ajog.2015.01.051.

4. Stanczyk FZ, Archer DF, Bhavnani BR. Ethinyl estradiol and 17b-estradiol in combined oral contraceptives: pharmacokinetics, pharmacodynamics and risk assessment. Contraception 2013; 87 (6): 706–627. doi: 10.1016/ j.contraception.2012.12.011.

5. Jensen JT. Evaluation of a new estradiol oral contraceptive: estradiol valerate and dienogest. Expert Opin Pharmacother 2010; 11 (7): 1147–1157. doi: 10.1517/146565610037 24713.

6. Kangasniemi MH, Arffman RK, Haverinen A et al. Effects of estradiol- and ethinylestradiol-based contraceptives on adrenal steroids: a randomized trial. Contraception 2022; 116: 59–65. doi: 10.1016/j.contraception.2022.08.009.

7. Stanczyk FZ, Winer SA, Foidart JM et al. Comparison of estrogenic components used for hormonal contraception. Contraception 2024; 130: 110310. doi: 10.1016/j.contraception.2023. 110310.

8. Arnal JF, Lenfant F, Metivier R et al. Membrane and nuclear estrogen receptor alpha actions: from tissue specificity to medical implications. Physiol Rev 2017; 97 (3): 1045–1087. doi: 10.1152/physrev.00024.2016.

9. Battipaglia C, Feliciello L, Genazzani AD et al. Combined oral contraceptive with estetrol plus drospirenone: from pharmacokinetics to clinical applications. Expert Opin Drug Metab Toxicol 2023; 19 (12): 871–879. doi: 10.1080/17425255.2023.2279752.

10. Apter D, Zimmerman Y, Beekman L et al. Estetrol combined with drospirenone: an oral contraceptive with high acceptability, user satisfaction, well-being and favourable body weight control. Eur J Contracept Reprod Health Care 2017; 22 (4): 260–267. doi: 10.1080/13625187.2017.1336532.

11. Archer DF, Mansour D, Foidart JM. Bleeding patterns of oral contraceptives with a cyclic dosing regimen: an overview. J Clin Med 2022; 11 (15): 4634. doi: 10.3390/jcm11154634.

12. Gemzell-Danielsson K, Apter D, Zatik J et al. Estetrol-Drospirenone combination oral contraceptive: a clinical study of contraceptive efficacy, bleeding pattern and safety in Europe and Russia. BJOG 2022; 129 (1): 63–71. doi: 10.1111/1471-0528.16840.

13. Riggs BL, Khosla S, Melton LJ 3rd. A unitary model for involutional osteoporosis: estrogen deficiency causes both type I and type II osteoporosis in postmenopausal women and contributes to bone loss in aging men. J Bone Miner Res 1998; 13 (5): 763–773. doi: 10.1359/jbmr.1998.13.5.763.

14. Bilezikian JP. Sex steroids, mice, and men: when androgens and estrogens get very close to each other. J Bone Miner Res 2002; 17 (4): 563–566. doi: 10.1359/jbmr.2002.17.4.563.

15. Harris S, Dawson-Hughes B. Rates of change in bone mineral density of the spine, heel, femoral neck and radius in healthy postmenopausal women. Bone Miner 1992; 17 (1): 87–95. doi: 10.1016/0169-6009 (92) 90713-n.

16. Quigley ME, Martin PL, Burnier AM et al. Estrogen therapy arrests bone loss in elderly women. Am J Obstet Gynecol 1987; 156 (6): 1516–1523. doi: 10.1016/0002-9378 (87) 90025-1.

17. Coelingh Bennink HJ, Heegaard AM, Visser M et al. Oral bioavailability and bone-sparing effects of estetrol in an osteoporosis model. Climacteric 2008; 11 (Suppl 1): 2–14. doi: 10.1080/13697130701798692.

18. Coelingh Bennink HJ, Verhoeven C, Zimmerman Y et al. Pharmacodynamic effects of the fetal estrogen estetrol in postmenopausal women: results from a multiple-rising-dose study. Menopause 2017; 24 (6): 677–685. doi: 10.1097/ GME.0000000000000823.

19. Douxfils J, Klipping C, Duijkers I et al. Evaluation of the effect of a new oral contraceptive containing estetrol and drospirenone on hemostasis parameters. Contraception 2020; 102 (6): 396–402. doi: 10.1016/j.contraception.2020.08.015.

20. Morimont L, Jost M, Gaspard U et al. Low thrombin generation in users of a contraceptive containing estetrol and drospirenone. J Clin Endocrinol Metab 2022; 108 (1): 135–143. doi: 10.1210/clinem/dgac511.

21. Gallez A, Dias Da Silva I, Wuidar V et al. Estetrol and mammary gland: friends or foes? J Mammary Gland Biol Neoplasia 2021; 26 (3): 297–308. doi: 10.1007/s10911-021-09497-0.

22. Gérard C, Blacher S, Communal L et al. Estetrol is a weak estrogen antagonizing estradiol-dependent mammary gland proliferation. J Endocrinol 2015; 224 (1): 85–95. doi: 10.1530/JOE-14-0549.

23. Singer CF, Coelingh Bennink HJ, Natter C et al. Antiestrogenic effects of the fetal estrogen estetrol in women with estrogen-receptor positive early breast cancer. Carcinogenesis 2014; 35 (11): 2447–2451. doi: 10.1093/carcin/bgu144.

24. Gérard C, Foidart JM. Estetrol: from preclinical to clinical pharmacology and advances in the understanding of the molecular mechanism of action. Drugs R D 2023; 23 (2): 77–92. doi: 10.1007/s40268-023-00419-5.

25. Muhn P, Fuhrmann U, Fritzemeier KH et al. Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Ann N Y Acad Sci 1995; 761: 311–335. doi: 10.1111/j.1749-6632.1995.tb31386.x.

26. Preston RA, White WB, Pitt B et al. Effects of drospirenone/17-beta estradiol on blood pressure and potassium balance in hypertensive postmenopausal women. Am J Hypertens 2005; 18 (6): 797–804. doi: 10.2016/j.amjhyper.2004.12.003.

27. Caprio M, Antelmi A, Chetrite G et al. Antiadipogenic effects of the mineralocorticoid receptor antagonist drospirenone: potential implications for the treatment of metabolic syndrome. Endocrinology 2011; 152 (1) : 113–125. doi: 10.1210/ en.2010-0674.