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

Rukhlyada N.N., Biryukova E.I.

1) Saint Petersburg State Pediatric Medical University, Ministry of Health of Russia, Saint Petersburg, Russia; 2) I.I. Dzhanelidze Saint Petersburg Research Institute of Emergence Care, Saint Petersburg, Russia
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.

Authors’ contributions: Rukhlyada N.N., Biryukova E.I. – concept and design of the investigation, material collection and processing, selection of literature on the stated topic, writing the text, editing.
Conflicts of interest: The authors declare that there are no conflicts of interest.
Funding: This investigation has not been sponsored.
For citation: Rukhlyada N.N., Biryukova E.I. The characteristics of pharmacokinetics and
the biological effects of gonadotropin-releasing hormone agonists.
Akusherstvo i Ginekologiya/Obstetrics and Gynecology. 2023;(2): 154-158 (in Russian)


gonadotropin-releasing hormone (GnRH)
GnRH agonists
GnRH receptors


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Received 13.02.2023

Accepted 21.02.2023

About the Authors

Nikolai N. Rukhliada, Dr. Med. Sci., Professor, Head of the Department of Obstetrics and Gynecology, St. Petersburg State Pediatric Medical University,
Ministry of Health of Russia, +7(911)913-20-20,,, 194100, Russia, Saint Petersburg, Litovskaya str., 2.
Elena I. Birukova, Ph.D., Head of the Department of Gynecology No. 2, I.I. Dzhanelidze Saint Petersburg Research Institute of Emergence Care, +7(911)225-21-31,, 192242, Russia, Saint Petersburg, Budapeshtskaya str., 3А.

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