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 Follicle-stimulating hormone (FSH) is a gonadotropin, a glycoprotein polypeptide hormone. FSH is synthesized and secreted by the gonadotropic cells of the anterior pituitary gland and regulates the development, growth, pubertal maturation, an ...

(FSH). 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 An acetate is a salt (chemistry), salt formed by the combination of acetic acid with a base (e.g. Alkali metal, alkaline, Alkaline earth metal, earthy, Transition metal, metallic, nonmetallic or radical Radical (chemistry), base). "Acetate" als ...

or pamoate salts. Primary indications include

endometriosis Endometriosis is a disease of the female reproductive system in which cells similar to those in the endometrium, the layer of tissue that normally covers the inside of the uterus, grow outside the uterus. Most often this is on the ovaries, f ...

, for the reduction of uterine fibroids, to treat

prostate cancer Prostate cancer is cancer of the prostate. Prostate cancer is the second most common cancerous tumor worldwide and is the fifth leading cause of cancer-related mortality among men. The prostate is a gland in the male reproductive system that sur ...

, and to treat male hypersexuality with severe sexual deviation. The drug has also been used off label to delay puberty in patients with gender dysphoria. It was patented in 1975 and approved for medical use in 1986. It is on the World Health Organization's List of Essential Medicines.

Medical uses

Triptorelin is used to treat

as part of androgen deprivation therapy. 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. It can also be used as a puberty blocker. Triptorelin has been used as a chemical castration agent for reducing sexual urges in sex offenders.

Drug action

Triptorelin is a gonadorelin analogue, also known as luteinizing hormone releasing analogue (GnRH analogue, LHRH analogue). The drug binds to receptors in the pituitary gland and stimulates secretion of gonadotropins (namely luteinizing hormone LH and

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.

Side-effects

General side effects can include: * 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

Society and culture

Brand names

Triptorelin is marketed under the brand names Decapeptyl ( Ipsen) and Diphereline and Gonapeptyl ( Ferring Pharmaceuticals). In the United States, it is sold by

Watson Pharmaceuticals Actavis Generics (formerly known as Watson Pharmaceuticals and Actavis plc, prior to the acquisition of Irish-based Allergan Inc) is a global pharmaceutical company focused on acquiring, developing, manufacturing and marketing branded pharmaceuti ...

as Trelstar and by Arbor Pharmaceuticals as Triptodur (an extended-release 6-month depot injection). In Iran, triptorelin is marketed under the brand name Variopeptyl. In the UK and Germany, it is sold as Salvacyl.

Research

Triptorelin and other antiandrogens may be effective in the treatment of obsessive–compulsive disorder.

References

External links

* {{Portal bar , Medicine GnRH agonists Peptides Puberty blockers AbbVie brands World Health Organization essential medicines