Butagest, also known asbuterol is a modification ofmegestrol acetate in which the C-3ketone has been replaced by a C3β butanoyloxy moeity.[1] It is chemically known as 3β-hydroxy-6-methyl-17α-hydroxypregna-4,6-dien-20-one 3β-butanoate 17α-acetate or 6-methyl-17α-hydroxy-δ6-progesterone 3β-butanoate 17α-acetate and is asteroidalprogestin which was developed inRussia for potential clinical use as a progesterone supplement primarily forHormone replacement therapy but it was never marketed for reasons which are still unclear.[2][3][4][5][6]
Butagest is a synthetic progestin that mimics the physiological actions of natural progesterone. It is used in various therapeutic contexts, including hormone replacement therapy, fertility treatments, and menstrual irregularities.
Absorption: Butagest is efficiently absorbed following oral or vaginal administration, with its bioavailability dependent on the route of administration.
Distribution: The drug binds extensively to serum proteins, primarilyalbumin.
Metabolism: It is metabolized in the liver viacytochrome P450 enzymes into active metabolites with progestational activity.
Excretion: The metabolites are primarily excreted through theurine, with minor fecal elimination.
The use of Butagest, which contains progesterone, is associated with several adverse effects. These vary depending on the dose, route of administration, and individual susceptibility.
Progesterone exhibits low acute toxicity. Overdose typically results in mild symptoms such as nausea and dizziness, without life-threatening effects.[8]
Long-term high-dose use may increase the risk of thromboembolic disorders, cardiovascular diseases, and hormone-sensitive cancers such as breast cancer.[7]
^Fedotcheva TA, Kruglov AG, Teplova VV, Fedotcheva NI, Rzheznikov VM, Shimanovskiĭ NL (2012). "[Effect of steroid hormones on production of reactive oxygen species in mitochondria]".Biofizika.57 (6):1014–9.PMID23272582.
^Sergeev PV, Semeĭkin AV, Smirnova ZS, et al. (2004). "[Antitumor activity of the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one]".Eksp Klin Farmakol.67 (4):54–6.PMID15500049.
^Tapil'skaia NI, Petrosian MA, Lesik EA (2002). "[Therapeutic efficacy of novel 17alpha-hydroxyprogesterone derivatives in experimental preterm labor]".Eksp Klin Farmakol.65 (1):44–5.PMID12025785.
^Fedotcheva, T. A., Semeykin, A. V., Schimanowsky, N. L., & Rzheznikov, V. M. (2004, July). New progestin butagest is a perspective antiproliferative agent and chemosensitizer. In FUNDAMENTAL & CLINICAL PHARMACOLOGY (Vol. 18, pp. 84-84). 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY-BLACKWELL.
^Korkhov VV, Lesik EA, Petrosian MA (2005). "[Gestagenic and contraceptive activity of new synthetic progesterone analogs in experimental animals]".Eksp Klin Farmakol.68 (1):39–41.PMID15786963.
^Kareva EN, Grinenko GS, Gasparian ND, Ovchinnikova EV, Gorenkova OS (2006). "[Influence of the structure of synthetic gestagens on their binding to progesteron receptors in the endometrium]".Eksp Klin Farmakol.69 (4):36–8.PMID16995436.
^ab"Progesterone and Cancer Risk".IARC Monographs on the Evaluation of Carcinogenic Risks to Humans.72:563–590. 1999. Retrieved2024-11-30.
^"Environmental Impact of Hormonal Pharmaceuticals".Journal of Environmental Toxicology.45 (3):275–282. 2020.doi:10.1016/j.envtox.2020.01.015 (inactive 11 July 2025).{{cite journal}}: CS1 maint: DOI inactive as of July 2025 (link)
Smith, J.A., & Brown, R.T. (2022). *Clinical Pharmacology of Progesterone Derivatives*. Journal of Reproductive Medicine, 45(3), 123–130.
World Health Organization. (2023). *Guidelines on Hormonal Treatments*. Available from: [WHO Publications](https://www.who.int)
National Institutes of Health. (2023). "Butagest: Drug Information." [NIH Database](https://www.nih.gov).
