Degarelix Acetate

Indications

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

Adult Dose

Subcutaneous Hormone-dependent Advanced Prostate Carcinoma (Stage D) 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.

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

Moderate to severe renal (CrCl <50 mL/min) and severe hepatic impairment. Hypersensitivity: Anaphylaxis, urticaria and angioedema have been reported. Discontinue Degarelix if a severe hypersensitivity reaction occurs and manage as clinically indicated QT Interval Prolongation: Androgen deprivation therapy treatment with Degarelix may prolong the QT interval. Patient with congenital long QT syndrome, history of or risk factors for QT prolongation (e.g. cardiac failure, electrolyte imbalance) and CV disease. Embryo-Fetal Toxicity: Degarelix can cause fetal harm. MONITORING PARAMETERS Monitor bone density.

Pregnancy-Lactation

Pregnancy & Lactation Pregnancy Safety and efficacy not established in women Animal data Based on findings in animal studies and mechanism of action, drug can cause fetal harm and loss of pregnancy when administered to a pregnant woman; there are no human data on use of drug in pregnant women to inform drug-associated risk; in animal developmental and reproductive toxicity studies in rats and rabbits, oral administration of degarelix during organogenesis caused embryo-fetal lethality and abortion as well as increased post-implantation loss and decreased number of live fetuses in animals at doses less than clinical loading dose based on body surface area; advise pregnant patients and females of reproductive potential of potential risk to fetus Based on findings in animals and the mechanism of action, degarelix may impair fertility in males and females of reproductive potential Lactation Safety and efficacy not established in females; there are no data on presence of drug in human milk, effects on breastfed child, or on milk production; because many drugs are present in human milk and because of potential for serious adverse reactions in a breastfed child from therapy, a decision should be made whether to discontinue nursing or discontinue drug taking into account importance of drug to mother

Interactions

Increased risk of QT prolongation with class IA (e.g. disopyramide) or class III (e.g. amiodarone) antiarrhythmics, antipsychotics, methadone and moxifloxacin. This drug is not a substrate for the human CYP450 system; degarelix is not an inducer or inhibitor of the CYP450 system in vitro; clinically significant CYP450 pharmacokinetic drug-drug interactions are unlikely.

Adverse Effects

Side effects of Degarelix Acetate : >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.