Triptorelin

A synthetic hormone used in medicine

Chemical structure of triptorelin

Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used in the treatment of hormone-sensitive conditions. It is a synthetic decapeptide analog of the natural gonadotropin-releasing hormone (GnRH). Triptorelin is primarily used in the management of prostate cancer, endometriosis, and precocious puberty.

Medical uses

Triptorelin is used in the treatment of several medical conditions:

• Prostate cancer: Triptorelin is used as part of androgen deprivation therapy to reduce the levels of testosterone in the body, which can help slow the growth of prostate cancer cells.

• Endometriosis: By suppressing the production of estrogen, triptorelin can help alleviate the symptoms of endometriosis, a condition where tissue similar to the lining inside the uterus grows outside the uterus.

• Precocious puberty: Triptorelin is used to delay early onset puberty in children by suppressing the release of gonadotropins.

Mechanism of action

Triptorelin acts as an agonist of the gonadotropin-releasing hormone receptor (GnRHR). Initially, it stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a temporary increase in sex hormone levels. However, with continuous administration, it causes downregulation of the GnRHR, resulting in decreased production of LH and FSH, and subsequently, a reduction in sex hormone levels.

Side effects

Common side effects of triptorelin include hot flashes, decreased libido, and mood changes. Long-term use can lead to osteoporosis due to decreased bone density.

Chemistry

Triptorelin is a decapeptide with the sequence pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2. It is available in various formulations, including depot injections that provide sustained release of the drug over time.

History

Triptorelin was first synthesized in the 1970s and has been used clinically since the 1980s. It is marketed under various brand names, including Decapeptyl and Trelstar.

Related pages

• Gonadotropin-releasing hormone
• Prostate cancer
• Endometriosis
• Precocious puberty