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gonadotropin-releasing hormone agonist (GnRH analog)

Indications: - hormonal treatment of prostate cancer - ovarian cancer - breast cancer - endometriosis - precocious puberty [3] Adverse effects: - may cause an initial surge in testosterone production before lowering testosterone levels - increase in the risk of diabetes [1,2] - increase in the risk of cardiovascular disease [1,2] - osteoporosis & bone fractures [4] Mechanism of action: 1) dminishes testosterone secretion by Leydig cells of the testis by down-regulating GnRH receptors 2) down-regulating GnRH receptors affects LH & FSH release from the anterior pituitary a) initially stimulates LH & FSH release, then b) diminishes LH & FSH release via negative feed-back (loss of pulsatility) 3) diminished LH diminished strimulus for testosterone secretion

Interactions

drug adverse effects of GnRH agonists

Related

gonadotropin-releasing hormone [GNRH] receptor gonadotropin-releasing hormone/factor; gonadoliberin; LH/FSH-releasing hormone (GnRH, LHRH)

Specific

buserelin (Suprecur) deslorelin (Suprelorin, Somagard, Tryptal, Ovuplant) goserelin (Zoladex) leuprolide; leuprorelin (Lupron, Eligard) Lutrepulse (Relisorm, Factrel, GnRH, GnRH1) nafarelin (Synarel) triptorelin (Trelstar LA)

General

endocrine agent

References

  1. FDA MedWatch 05/03/2010 GnRH Agonists: Safety Review of Drug Class Used to Treat Prostate Cancer http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm210576.htm
  2. FDA MedWatch 10/20/2010 GnRH Agonists: Label Change - Increased Risk of Diabetes and Cardiovascular Disease (Update) http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm230359.htm
  3. Deprecated Reference
  4. Smith MR, Lee WC, Brandman J et al. Gonadotropin-releasing hormone agonists and fracture risk: a claims-based cohort study of men with nonmetastatic prostate cancer. J Clin Oncol 2005 Nov 1; 23:7897 PMID: 162580