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Goserelin

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Information about Goserelin

Goserelin is a parenterally administered, gonadotropin releasing hormone (GnRH) agonist which causes an inhibition of estrogen and androgen production and is used predominantly to treat prostate cancer. 

 

Goserelin
Goserelin
Goserelin
Goserelin

Liver safety of Goserelin

Goserelin has been associated with a modest rate of serum enzyme elevations during therapy, but has not been convincingly linked to instances of clinically apparent acute liver injury

Mechanism of action of Goserelin

Goserelin (goe" se rel' in) is a synthetic decapeptide analogue of gonadotropin releasing hormone that acts as a partial agonist of the gonadotropin receptors in the pituitary that regulate luteinizing hormone (LH) and follicle stimulating hormone (FSH) secretion. 

These gonadotropins cause production and secretion of testosterone by the male testes and estrogen by the female ovaries. 

Zoladex Goserelin
Zoladex Goserelin

The continued receptor occupancy by goserelin, however, ultimately causes a down-regulation of production of LH and FSH and a resultant decrease in testosterone and estrogen levels. 

Goserelin, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer. 

FDA approval information for Goserelin

Goserelin was approved for use in the United States in 1989 and is still widely used, being considered important adjuvant therapy in management of advanced prostate cancer.

Advanced breast cancer

Goserelin is also approved for use in advanced breast cancer and for several hormonally sensitive benign conditions such as endometriosis

Testosterone levels in long-term androgen deprivation therapy
Testosterone levels in long-term androgen deprivation therapy

Off label use

The GnRH agonists have also been used off label for precocious puberty and infertility

Brand name for Goserelin

Goserelin is available under the brand name Zoladex in solution for administration subcutaneously as implants every 4 (3.6 mg) or 12 (10.8 mg) weeks. 

Goserelin and the other GnRH analogues cause a profound hypogonadism ("chemical castration") .

Side effects of Goserelin

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 side effects

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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