Degarelix

Indications

Degarelix is used for: Hormone-dependent Advanced Prostate Carcinoma (Stage D)

Adult Dose

Subcutaneous Advanced prostate cancer Adult: Loading dose: As 40 mg/mL solution: 240 mg (given as 2 separate injections of 120 mg). Maintenance: As 20 mg/mL solution: 80 mg once every 28 days, starting 28 days after the initial dose. Doses are administered in the abdominal area. Hepatic Impairment Mild-to-moderate: Dose adjustment not necessary Severe: Safety and efficacy not established; use caution

Child Dose

Renal Dose

Renal Impairment >50 mL/min: Dose adjustment not necessary <50 mL/min: Use caution

Administration

Initiation pack contains 2 vials each with 120 mg per vial & 6 mL sterile water for injection diluent Withdraw 3 mL of sterile water for injection diluent (supplied) & add to 1 of the 2 vials, swirl to mix - keep vial vertical at all times, do not shake Inject SC in abdomen within 1 hour of reconstitution Repeat for 2nd injection and use different injection site Maintenance pack contains 1 vial of 80 mg per vial & 4.2 mL sterile water for injection diluent Use 4.2 mL to reconstitute, withdraw 4 mL for dose of 80 mg

Contra Indications

Hypersensitivity. Pregnancy and lactation.

Precautions

Patient with congenital long QT syndrome, history of or risk factors for QT prolongation (e.g. cardiac failure, electrolyte imbalance) and CV disease; diabetes, risk factors for low BMD. Moderate to severe renal (CrCl <50 mL/min) and severe hepatic impairment. Lactation: excretion in milk unknown/not recommended

Pregnancy-Lactation

Pregnancy Category: X Lactation: excretion in milk unknown/not recommended

Interactions

Increased risk of QT prolongation with class IA (e.g. disopyramide) or class III (e.g. amiodarone) antiarrhythmics, antipsychotics, methadone and moxifloxacin.

Adverse Effects

Side effects of Degarelix : >10% Hot flashes (26%) Injection site erythema (17%) Injection site pain (28%) Weight gain (11%) Elevated liver enzymes (10%) 1-10% (selected) Arthralgia Back pain Fatigue HTN Injection site induration/swelling

Mechanism of Action

Degarelix, a synthetic decapeptide, reversibly and competitively binds to gonadotropin-releasing hormone (GnRH) receptors in the anterior pituitary gland, thereby decreasing secretion of luteinising hormone (LH) and follicle stimulating hormone (FSH), and subsequently reducing testicular androgen synthesis.