Triptorelin

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Information about Triptorelin

Triptorelin is a gonadotropin releasing hormone (GnRH) agonist that is a potent inhibitor of the synthesis of testosterone (in men) and estrogen (in women) and is used to treat advanced prostate cancer. 

Liver safety of Triptorelin

Triptorelin is associated with a low rate of transient serum enzyme elevations during therapy, but has not been linked convincingly to cases of clinically apparent acute liver injury.   

Mechanism of action of Triptorelin

Triptorelin (trip" toe rel' in) is a decapeptide analogue of gonadotropin releasing hormone (GnRH) that acts on the pituitary to cause the synthesis and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH), two gonadotropins that act on the male testes to stimulate the production of testosterone and on the female ovaries to induce synthesis of estrogen.  Triptorelin and other GnRH agonists cause an initial surge of gonadotropin release, but then lead to down-regulation of their synthesis and secretion which results in a decline in testosterone and estrogen production.  Triptorelin, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer and as effective as surgical castration. 

FDA approval information for Triptorelin

Triptorelin was approved for use in the United States for prostate cancer in 2000 and is still widely used, being considered a first line treatment of this hormone responsive malignancy.  Triptorelin is available generically and under the brand name Trelstar in an injectable suspension for intramuscular depot administration every 4 weeks (3.75 mg), 12 weeks (11.25 mg) or 24 weeks (22.5 mg).  Triptorelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration").

Side effects of Triptorelin

The common side effects are typical of androgen deprivation, including hot flashes, loss of libido, erectile dysfunction, depression, nausea, diarrhea, weight gain and fluid retention.  Rare, but potentially severe adverse events can include immediate hypersensitivity reactions, pituitary apoplexy and, with long term use, weight gain, metabolic changes, diabetes and osteoporosis.

 


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