Oestrogens in oral contraception: considerations for tailoring prescription to women’s needs

Abstract

Background

The oestrogenic component of combined oral contraceptives (COCs) has changed over years with the aim of reducing oestrogen-related side effects and risks, whilst maintaining oestrogen beneficial effects, particularly on cycle control.

Purpose

To describe the pharmacological profiles of different oestrogens commonly used in COCs to provide insights on contraceptive prescription tailored to women’s needs.

Results

All COCs ensure a high contraceptive efficacy. COCs containing the natural oestrogens oestradiol (E2), oestradiol valerate (E2V) and estetrol (E4) have limited impact on liver metabolism, lipid and carbohydrate metabolism, haemostasis and sex hormone binding globulin levels, compared with ethinylestradiol (EE). COCs with E2 and E2V appear also to entail a lower elevation of the risk of venous thromboembolism vs. EE-containing pills. No epidemiological data are available for E4-COC. E2- and E2V-containing COCs seem to exert a less stabilising oestrogenic effect on the endometrium compared with EE-COCs. The E4-COC results in a predictable bleeding pattern with a high rate of scheduled bleeding and minimal unscheduled bleeding per cycle. Based on in vitro and in vivo animal data, E4 seems to be associated with a lower effect on cell breast proliferation.

Conclusion

Today various COCs contain different oestrogens. Prescribers must be familiar with the different properties of each oestrogen for a tailored contraceptive recommendation, considering their safety and contraceptive efficacy, as well as women’s needs and preferences.

SHORT CONDENSATION

For contraceptive pills physicians can choose among different oestrogens, besides many progestins. Natural oestrogens have less metabolic impact vs EE, while EE and E4 seem to provide a better cycle control. Knowing the different oestrogen characteristics is crucial for adjusting pill prescription to women’s needs and desires.

Keywords:

• Estetrol
• oestradiol
• oestradiol valerate
• ethinylestradiol
• combined oral contraceptives
• contraceptive tailored prescription
• women’s needs

Acknowledgements

The author would like to acknowledge Eleonora Comi, PhD of PRINEOS S.r.l. for medical writing support.

Disclosure statement

Franca Fruzzetti has served as speaker and advisory board member for Theramex, Gedeon-Richeter, Bayer, Organon, Exeltis, Italfarmaco. Tiziana Fidecicchi has no conflict of interest to declare. Marco Gambacciani has served as speaker and advisory board member for Theramex, Gedeon-Richter, Fotona, Organon.

Ethics statement

The authors report that ethics approval was not required for this narrative review.

Data availability statement

Data sharing is not applicable to this article as no new data were created or analysed in this review.