Triptorelin


Triptorelin, sold under the brand names Decapeptyl and Gonapeptyl among others, is a medication that acts as an agonist analog of Gonadotropin-releasing hormone, thus reversibly repressing of luteinizing hormone and follicle-stimulating hormone.
It is a decapeptide and a gonadotropin-releasing hormone agonist used as the acetate or pamoate salts.
Primary indications include endometriosis, for the reduction of fibroids, for prostatic cancer, 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.

Medical uses

Triptorelin is used to treat prostate cancer as part of androgen deprivation therapy. Another ADT injectable medicine commonly used to treat PCa includes Lupron which also targets the pituitary.
Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people. 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.
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 Leuteinzing hormone releasing analogue. The drug binds to receptors in the pituitary gland and stimulates secretion of gonadotrophins. 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 gonadotrophins in the long term, which in turn leads to the inhibition of androgen and oestrogen production.

Side-Effects

General side effects can include:
Triptorelin should not be used for more than 6 months for endometriosis, and should be used with care in patients with metabolic bone disease and osteoporosis due to the risk of osteopenia.

Society and culture

Brand names

Triptorelin is marketed under the brand names Decapeptyl and Diphereline and Gonapeptyl. In the United States, it is sold by Watson Pharmaceuticals as Trelstar and by Arbor Pharmaceuticals as Triptodur. In Iran, triptorelin is marketed under the brand name Variopeptyl.