Obstetrics and GynecologyObstetrics and GynecologyАкушерство и гинекология0300-90922412-5679Bionika Media63215410.18565/aig.2024.103Guidelines for the PractitionerВ помощь практическому врачуResearch ArticleCombined hormonal contraceptive containing estetrol and drospirenone: pharmacokinetics and opportunities forclinical useКомбинированный гормональный контрацептив, содержащий эстетрол и дроспиренон: фармакокинетика и возможности клинического примененияNazarovaNiso M.НазароваНисо Мирзоевна
Russian Federation

Dr. Med. Sci., Leading Researcher

д.м.н., в.н.с.

grab2@yandex.ruPrilepskayaVera N.ПрилепскаяВера Николаевна
Russian Federation

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

профессор, д.м.н., заведующий научно-поликлиническим отделением

vprilepskaya@mail.ruAcademician V.I. Kulakov National Medical Research Centre for Obstetrics, Gynecology and Perinatology, Ministry of Health of RussiaФГБУ «Национальный медицинский исследовательский центр акушерства, гинекологии и перинатологии имени академика В.И. Кулакова» Минздрава России1704202441561611705202417052024Copyright ©; 2024, Bionika MediaCopyright ©; 2024, ООО «Бионика Медиа»2024Bionika MediaООО «Бионика Медиа»https://journals.eco-vector.com/0300-9092/article/view/632154

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.

В России и ряде стран зарегистрирован новый комбинированный гормональный контрацептив (КГК), содержащий 15 мг эстетрола и 3 мг дроспиренона (E4/DRSP). Эстетрол (Е4) представляет собой нативный фетальный эстроген III поколения, вырабатываемый клетками печени плода во время беременности. Дроспиренон – первый синтетический прогестин, полученный из 17-α-спиронолактона. Е4 отличается от других эстрогенов (17-β-эстрадиола или этинилэстрадиола) высокоселективным избирательным действием на различные ткани, а также антипролиферативными свойствами.

В данной статье представлены исследования фармакокинетики КГК, содержащего E4/DRSP, и возможности клинического применения с учетом характеристики компонентов. Показано, что E4/DRSP оказывает минимальное влияние на параметры гемостаза, липидный профиль, обладает антипролиферативными свойствами.

Заключение: Особенности фармакокинетики E4/DRSP позволяют рассматривать его в качестве препарата первого выбора для молодых женщин, впервые планирующих использование гормональной контрацепции, при нежелательных эффектах (длительные кровянистые выделения/кровотечения, боли в молочных железах, склонность к отекам) на фоне применения других комбинированных оральных контрацептивов.

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