Information about Leuprolide
Leuprolide is a parenterally administered, gonadotropin releasing hormone (GnRH) agonist which causes an inhibition of estrogen and androgen production and is used predominantly to treat advanced prostate cancer.
Liver safety of Leuprolide
Leuprolide 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 Leuprolide
Leuprolide (loo' proe lide), also called leuprorelin (loo" proe rel' in), is a nonapeptide analogue of gonadotropin releasing hormone (GnRH) that acts as a partial agonist of the gonadotropin receptors in the pituitary that induce secretion of luteinizing hormone (LH) and follicle stimulating hormone (FSH). These gonadotropins cause production and secretion of testosterone by the male testes and estrogen by the female ovaries. The continued receptor occupancy by leuprolide, however, ultimately causes a down-regulation of production of LH and FSH and a resultant decrease in testosterone and estrogen levels. Leuprolide, alone or in combination with other antiandrogens, has been found to be palliative in advanced prostate cancer.
FDA approval information for Leuprolide
Leuprolide was approved for use in the United States in 1989 and is still widely used, being considered a first line therapy in management of prostate cancer, the GnRH agonists having largely replaced surgical castration in the medical management of prostate cancer. Leuprolide is also used off label for hormonally sensitive benign conditions such as endometriosis, uterine fibroids, precocious puberty and infertility.
Brand name for Leuprolide
Leuprolide is available generically and under the brand name Lupron in solution for daily subcutaneous injections (1 mg) or in long acting depot forms which are administered intramuscularly every 1 (7.5 mg), 3 (22.5 mg), 4 (30 mg) or 6 (45 mg) months.
Side effects of Leuprolide
Leuprolide 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 immediate hypersensitivity reactions, pituitary apoplexy and, with long term use, weight gain, metabolic changes, diabetes and osteoporosis.