Triptorelin
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Overview
Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used in the treatment of hormone-sensitive conditions such as prostate cancer, endometriosis, and precocious puberty. It is a synthetic decapeptide analog of the natural GnRH, which is involved in the regulation of the pituitary gland's secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
Mechanism of Action
Triptorelin acts by initially stimulating the release of LH and FSH from the pituitary gland, leading to a temporary increase in testosterone and estrogen levels. However, with continuous administration, it causes downregulation of the GnRH receptors in the pituitary, resulting in decreased secretion of LH and FSH. This leads to a significant reduction in the production of sex hormones, such as testosterone in men and estrogen in women, which is beneficial in treating hormone-sensitive conditions.
Clinical Uses
Triptorelin is primarily used in the management of:
- Prostate cancer: By reducing testosterone levels, triptorelin helps in slowing the growth of hormone-sensitive prostate cancer.
- Endometriosis: It alleviates symptoms by decreasing estrogen levels, which reduces the growth of endometrial tissue.
- Precocious puberty: Triptorelin is used to delay the onset of puberty in children with this condition by suppressing the premature release of sex hormones.
Administration
Triptorelin is administered via intramuscular injection. The dosing schedule can vary depending on the condition being treated, with formulations available for monthly or quarterly administration.
Side Effects
Common side effects of triptorelin include:
- Hot flashes
- Decreased libido
- Fatigue
- Mood changes
- Injection site reactions
In men, there may be an initial "flare" of symptoms due to the temporary increase in testosterone levels before they decrease.
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Contributors: Prab R. Tumpati, MD