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Information about Histrelin

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

Liver safety of Histrelin

Histrelin 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 Histrelin

Histrelin (his trel' in) is a nonapeptide analogue of gonadotropin releasing hormone 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.  Histrelin 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.  Histrelin, 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 Histrelin

Histrelin was approved for use in the United States in 1991 and as a once-yearly implant formulation in 2004.  The major indications for histrelin are advanced prostate cancer and precocious puberty. 

Brand name for Histrelin

Histrelin is available generically and under the brand names Supprelin (for precocious puberty) and Vantas (for prostate cancer) in solution as implants of 50 mg, which are inserted subcutaneously in the inner aspect of the upper arm at 12 month intervals. 

Side effects of Histrelin

Histrelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration") and its 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 include hypersensitivity reactions and transient tumor flare with the first injection.


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