Combined hormonal contraceptive containing estetrol and drospirenone: pharmacokinetics and opportunities forclinical use

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Abstract

A new combined hormonal contraceptive (CHC) containing estetrol 15 mg and drospirenone 3 mg (E4/DRSP) is now registered in Russia and in a number of countries around the world. Estetrol (E4) is a third-generation native fetal estrogen produced by fetal liver cells during pregnancy. Drospirenone is the first synthetic progestin derived from 17-α-spirolactone. E4 differs from other estrogens (17-β-estradiol or ethinyl estradiol) by its highly selective action on various tissues, as well as by its antiproliferative properties.

This article presents studies on the pharmacokinetics of CHC containing E4/DRSP and the possibility of its clinical use taking into account the characteristics of the components. E4/DRSP has been shown to have minimal effect on hemostasis parameters, lipid profile, and antiproliferative properties.

Conclusion: The pharmacokinetic features of E4/DRSP make it possible to consider it as the first-line drug for young women who plan to use hormonal contraception for the first time with undesirable side effects (prolonged spotting/bleeding, pain in the mammary glands, tendency to swelling) while using other combined oral contraceptives.

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About the authors

Niso M. Nazarova

Academician V.I. Kulakov National Medical Research Centre for Obstetrics, Gynecology and Perinatology, Ministry of Health of Russia

Author for correspondence.
Email: grab2@yandex.ru

Dr. Med. Sci., Leading Researcher

Russian Federation, Moscow

Vera N. Prilepskaya

Academician V.I. Kulakov National Medical Research Centre for Obstetrics, Gynecology and Perinatology, Ministry of Health of Russia

Email: vprilepskaya@mail.ru

Dr. Med. Sci., Professor, Head of the Scientific Polyclinic Department

Russian Federation, Moscow

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