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.

摘要

背景: 多年来, 复方口服避孕药(COCs)的雌激素成分发生了变化, 目的是减少雌激素相关的副作用和风险, 同时保持雌激素的有益作用, 特别是在周期控制方面。

目的: 描述COCs中常用的不同雌激素的药理学特征, 为根据妇女的需要量身定做避孕处方提供见解。

结果: 所有COCs均保证了较高的避孕效果。与炔雌醇(EE)相比, 含有天然雌激素雌二醇(E2)、戊酸雌二醇(E2V)和雌三醇(E4)的COCs对肝脏代谢、脂肪和碳水化合物代谢、止血和性激素结合球蛋白水平的影响有限。使用E2和E2V的COCs与含EE的药片相比, 静脉血栓栓塞症的风险似乎也较低。目前还没有E4-COC的流行病学数据。与EE-COCs相比, 含有E2和E2V的COCs似乎对子宫内膜的稳定作用较小。E4-COC导致了一个可预测的出血模式, 具有较高的计划出血率和每个周期最少的非计划出血。基于体外和体内动物数据, E4似乎与细胞乳腺增殖的较低影响有关。

结论: 目前, 不同种类的COCs含有不同的雌激素。处方开具者必须熟悉每种雌激素的不同性质, 考虑其安全性和避孕效果, 以及妇女的需求和偏好, 为其提供量身定制的避孕建议。

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.