Triptorelin Acetate/GnRH Triptorelin

Triptorelin, sold under the brand name Decapeptyl among others, is a medication that acts as an agonist analog of gonadotropin-releasing hormone, repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).^[3][4]

It is a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂) and a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.

Primary indications include endometriosis,^[5] for the reduction of uterine fibroids, to treat prostate cancer, and to treat male hypersexuality with severe sexual deviation.^[4] The drug has also been used off label to delay puberty in patients with gender dysphoria.^[6]

It was patented in 1975 and approved for medical use in 1986.^[7] It is on the World Health Organization’s List of Essential Medicines.^[8]

Medical uses

See also: Gonadotropin-releasing hormone agonist § Medical uses

Triptorelin is used to treat prostate cancer as part of androgen deprivation therapy.^[9]

Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people (in conjunction with estradiol valerate for trans women or testosterone for trans men). Spironolactone and cyproterone acetate are other drugs used by trans people to suppress sex hormones, but these drugs have a completely different mechanism of action.^[10] It can also be used as a puberty blocker.^[11]

Triptorelin has been used as a chemical castration agent for reducing sexual urges in sex offenders.^[12]

Drug action

Triptorelin is a gonadorelin analogue, also known as luteinizing hormone releasing analogue (GnRH analogue, LHRH analogue).^[3] The drug binds to receptors in the pituitary gland and stimulates secretion of gonadotropins (namely luteinizing hormone LH and follicle-stimulating hormone FSH). This causes an initial phase of LH and FSH stimulation, prior to down-regulation of the gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotropins in the long term, which in turn leads to the inhibition of androgen and estrogen production.^[4]

Side-effects

General side effects can include:^[4]

• Anaphylaxis
• Arthralgia
• Asthenia
• Asthma
• Breast tenderness (males and females)
• Changes in blood pressure
• Changes in breast size
• Depression
• Ovarian cysts
• Mood changes
• Skin rashes
• Hot flushes
• Weight changes

References

1. ^“Prescription medicines: registration of new chemical entities in Australia, 2015”. Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
2. ^“Triptodur- triptorelin kit”. DailyMed. U.S. National Library of Medicine. 28 April 2022. Retrieved 15 May 2022.
3. ^ Jump up to:^ab “gonadorelin analogue”. Encyclopedia.com. Retrieved 2019-09-21.
4. ^ Jump up to:^ab c d Joint Formulary Committee (2018). British National Formulary (BNF) 70. London: Pharmaceutical Press. p. 635. ISBN 978-0-85711-173-9.
5. ^Leone Roberti Maggiore U, Scala C, Remorgida V, Venturini PL, Del Deo F, Torella M, et al. (June 2014). “Triptorelin for the treatment of endometriosis”. Expert Opinion on Pharmacotherapy. Informa Healthcare. 15 (8): 1153–1179. doi:1517/14656566.2014.916279. PMID 24832495. S2CID 23843087.
6. ^Cohen D, Barnes H (September 2019). “Gender dysphoria in children: puberty blockers study draws further criticism”. BMJ. 366: l5647. doi:1136/bmj.l5647. PMID 31540909. S2CID 202711942.
7. ^Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 514. ISBN 9783527607495.
8. ^World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
9. ^“triptorelin (Intramuscular route)”. Drugs.com. Retrieved 11 November 2016.
10. ^Wylie KR, Fung Jr R, Boshier C, Rotchell M (2009). “Recommendations of endocrine treatment for patients with gender dysphoria”. Sexual and Relationship Therapy. 24(2): 175–187. doi:1080/14681990903023306. S2CID 20471537.
11. ^Shumer DE, Nokoff NJ, Spack NP (August 2016). “Advances in the Care of Transgender Children and Adolescents”. Advances in Pediatrics. 63(1): 79–102. doi:1016/j.yapd.2016.04.018. PMC 4955762. PMID 27426896.
12. ^“Study: Drug effectively treats pedophilia”. CNN. 11 February 1998.

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