The characteristics of pharmacokinetics and the biological effects of gonadotropin-releasing hormone agonists

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Abstract

This paper presents a literature review of the physiological and pharmacokinetic features of used gonadotropin-releasing hormone (GnRH) agonists. It considers in detail the mechanism of action of drugs of this group at the level of receptors, as well as their mediated physiological effects. GnRH agonists initially stimulate and then inhibit sex hormone secretion by desensitizing pituitary GnRH receptors. There are examples of the clinical use of GnRH agonists. The latter are used to treat hormone-dependent diseases, such as endometriosis, uterine leiomyoma, pubertas precox, breast cancer, as well as in assisted reproductive technology protocols. Decreased bone mineralization due to hypoestrogenism is known to be one of the extremely negative effects of long-term use of GnRH agonists. The article discusses the ways of reducing the frequency and severity of GnRH side effects, including add-back therapy or changing the regimen of prescribing GnRH agonists.

Conclusion: The introduction of GnRH agonists was another breakthrough in gynecological practice and made it possible to successfully overcome previously unsolvable problems, such as infertility, severe endometriosis. Further joint developments by physiologists, biochemists, and clinicians suggest the increase in the efficacy of drugs and the expansion of their therapeutic abilities while reducing the risks of their use.

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About the authors

Nikolai N. Rukhliada

Saint Petersburg State Pediatric Medical University, Ministry of Health of Russia

Author for correspondence.
Email: nickolasr@mail.ru
ORCID iD: 0000-0002-3548-0468

Dr. Med. Sci., Professor, Head of the Department of Obstetrics and Gynecology

Russian Federation, Saint Petersburg

Elena I. Birukova

I.I. Dzhanelidze Saint Petersburg Research Institute of Emergence Care

Email: 79112252131@yandex.ru

Ph.D., Head of the Department of Gynecology No. 2

Russian Federation, Saint Petersburg

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