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PHARMACOLOGY OF Degarelix (Firmagon); Overview, mechanism of action, Uses, Effects, Pharmacokinetics

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Degarelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used primarily in the treatment of advanced prostate cancer. Here's an overview of its pharmacology:

Mechanism of Action:
GnRH Receptor Antagonist: Degarelix binds to GnRH receptors in the anterior pituitary gland, blocking the interaction with GnRH. This results in a rapid and sustained reduction in the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

Testosterone Suppression: The reduction in LH and FSH levels leads to a decrease in testosterone production, which is crucial for the management of prostate cancer.

Pharmacokinetics:
Absorption: Degarelix is administered subcutaneously and is rapidly absorbed.

Distribution: It has a volume of distribution greater than 1000 L.

Metabolism: Degarelix is metabolized via peptide hydrolysis in the liver.

Excretion: The drug and its metabolites are excreted primarily via the feces (70-80%) and to a lesser extent via the urine (20-30%).

Elimination Half-Life: The elimination half-life is approximately 53 days for the loading dose and 31 days for the maintenance dose.

Clinical Use:
Advanced Prostate Cancer: Degarelix is indicated for the treatment of advanced hormone-dependent prostate cancer in adult males. It is used to achieve and maintain suppression of testosterone levels3.

Side Effects:
Common Side Effects: Injection-site reactions (pain, erythema, swelling), hot flushes, and weight gain.

Serious Side Effects: Potential for allergic reactions, liver enzyme abnormalities, and cardiovascular events.

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