1- Triptorelin
Triptorelin, a decapeptide
(pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing
hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing
constant stimulation of the pituitary, it decreases pituitary secretion of
gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH).
Like other GnRH agonists, triptorelin may be used in the treatment of
hormone-responsive cancers such as prostate cancer or breast cancer, precocious
puberty, estrogen-dependent conditions (such as endometriosis or uterine
fibroids), and in assisted reproduction.
Triptorelin is marketed under the brand names Decapeptyl (Ipsen)
and Diphereline and Gonapeptyl (Ferring Pharmaceuticals).
In the United States, it is sold by Watson as Trelstar.
In Iran Triptorelin is marketed under the brand name Variopeptyl
(Varian Darou Pajooh).
During the treatment of prostate cancer it does cause a surge of
testosterone (an initial uplevel of testosterone levels), known as a flare
effect. In men a reduction of serum testosterone levels into the range normally
seen after surgical castration occurs approximately two to four weeks after
initiation of therapy. In contrast, gonadotropin-releasing hormone antagonists
do not cause a surge, but a sudden reduction of testosterone levels.
