Clinical pharmacology of transdermal estradiol
Talibov O.B.
The article focuses on the clinical pharmacology of transdermal estradiol formulations used in menopausal hormone therapy (MHT). It discusses the pharmacodynamics of estradiol, its effects on the liver, lipid metabolism, and the risk of gallstone disease, as well as the concept of the liver as an estrogen target organ. The paper describes key pharmacokinetic differences between oral and transdermal formulations, including the hepatic first-pass effect, conversion to estrone and estriol, characteristics of enterohepatic circulation, and safety profile. Various types of transdermal dosage forms (patches, gels, sprays) are analyzed in terms of cutaneous absorption and advantages for patients with cardiometabolic and hepatobiliary risk factors. The paper covers the potential drug interactions, the role of the cytochrome P450 system, the impact of concomitant therapies (including anticoagulants, lipid-lowering agents, L-thyroxine, and incretin receptor agonists) as well as the importance of individualized dosing and route selection in accordance with the international and Russian guidelines. Special attention is given to the selection of formulations, dose titration flexibility of gels, and the use of transdermal estradiol in women with high thrombotic and metabolic risk.
Conclusion: Aggregate data on pharmacokinetics, pharmacodynamics, and drug interactions indicate that transdermal estradiol provides a more physiological exposure profile, exerts less hepatic metabolic and coagulative impact, and thus creates a more favorable benefit–risk balance for women with cardiometabolic and hepatobiliary risk factors compared with oral administration. The article emphasizes the need for an interdisciplinary approach and ongoing therapy reassessment to optimize MHT safety in real-world clinical practice.
Conflicts of interest: Authors declare lack of the possible conflicts of interests.
Funding: The study was carried out without sponsorship.
For citation: Talibov O.B. Clinical pharmacology of transdermal estradiol.
Akusherstvo i Ginekologiya/Obstetrics and Gynecology. 2026; (1): 97-103 (in Russian)
https://dx.doi.org/10.18565/aig.2026.02
Keywords
estradiol
transdermal therapy
menopause
liver
lipid metabolism
gallstone disease
venous thromboembolic complications
pharmacokinetics
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Received 12.01.2026
Accepted 24.01.2026
About the Authors
Oleg B. Talibov, PhD, Associate Professor, Department of Therapy, Clinical Pharmacology and Emergency Medicine, NOI Clinical Medicine named after N.A. Semashko, Russian University of Medicine, Ministry of Health of Russia, 127473, Russia, Moscow, Delegatskaya str., 20 bld. 1, oleg.talibov@gmail.com,https://orcid.org/0000-0001-6381-2450
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