GnRH analogue used in hormonal treatment of carcinoma prostate?
Correct Answer: Goserelin
Description: Ans. a (Goserelin) (Ref. KDT 6th/pg. 239)Many analogues of GnRH, e.g. Buserelin, Goserelin, Leuprolide, Nafarelin, Triptorelin, have been developed: are 15-150 times more potent than natural Gn RH and longer acting. The superactive GnRH agonists are used as nasal spray or injected s.c. Long-acting preparations for once a month s.c. injection have been produced (triptorelin depot). The resulting reversible pharmacological oophorectomy /orchiectomy is being used in precocious puberty, prostatic carcinoma, endometriosis, premenopausal breast cancer, uterine leiomyoma, PCOD and to assist induced ovulation. It also has potential to be used as contraceptive for both males and females.# Goserelin is a drug often used in prostate carcinoma. Goserelin can cause gynecomastia as a side effect.# Anastrozole is a selective nonsteroidal inhibitor of aromatase. It is presently approved for first-line treatment of postmenopausal women with metastatic breast cancer that is ER-positive.# Letrozole is a nonsteroidal competitive inhibitor of aromatase that is significantly more potent than aminoglutethimide and acts in the same way as anastrozole. It is also indicated for first-line treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer.# Exemestane is a steroidal hormonal agent that binds to and irreversibly inactivates aromatase. It is indicated for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed on tamoxifen therapy.1.BicalutamideNonsteroidal anti-androgens2.Finasteride5-alpha reductase inhibitor3.OxybutyninMuscarinic receptor antagonists4.GoserelinLHRH analogue5.SildenafilPDE5 inhibitor6.Cyproterone acetateSteroidal anti-androgens7.TamsulosinAlpha blocker# Prostate cancer is classically treated with diethylstilbesterol (DES) acting as an estrogen at the level of the hypothalamus to downregulate hypothalamic luteinizing hormone (LH) production, resulting in decreased elaboration of testosterone by the testicle. For this reason, orchiectomy is equally as effective as moderate-dose DES.# In the event that orchiectomy is not accepted by the patient, testicular androgen suppression can also be effected by luteinizing hormone-releasing hormone (LHRH) agonists such as leuprolide and goserelin. These agents cause tonic stimulation of the LHRH receptor, with the loss of its normal pulsatile activation resulting in its desensitization and decreased output of LH by the anterior pituitary. Therefore, as primary hormonal manipulation in prostate cancer one can choose orchiectomy or leuprolide, not both.# The addition of actual antagonists of androgens acting at the androgen receptor, including flutamide or bicalutamide, is of uncertain additional benefit in extending overall response duration, but it clearly prevents the activation of androgen receptors by adrenal androgens, and the combined use of orchiectomy or leuprolide plus flutamide is referred to as "total androgen blockade."
Category:
Pharmacology
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