degarelix acetate: clinical use

Prescribing considerations

• Assess cardiovascular and QT-risk factors and review concomitant QT-prolonging medicines.
• Use caution in severe renal or hepatic impairment because these populations have not been adequately studied.
• Consider reduced bone density, impaired glucose tolerance and fertility suppression from sustained testosterone suppression.
• Fatigue or dizziness may affect driving or machinery use.
• Exercise particular caution with previous severe untreated asthma, anaphylaxis, urticaria or angioedema because these groups have not been studied.

Contraindications and cautions

• Hypersensitivity to degarelix or any excipient.

Monitoring

• Monitor clinical response and serum PSA.
• Check serum testosterone if response appears suboptimal.
• Monitor liver function in known or suspected hepatic disease.
• Consider more frequent blood-glucose monitoring in people with diabetes.
• Assess cardiovascular, QT and bone-health risks where clinically relevant.

Clinical pharmacology

Degarelix competitively and reversibly antagonises pituitary GnRH receptors, reducing LH, FSH and testicular testosterone without an initial testosterone surge. Following subcutaneous injection, a depot forms and releases degarelix slowly. It undergoes peptide degradation, and clinically important CYP450-mediated interactions are unlikely.

Formulation and product differences

• Supplied as powder with a pre-filled syringe of water for injections.
• It must be reconstituted carefully without shaking; the solution should be clear and free from undissolved material.
• Concentration and administration technique affect depot formation, so preparation instructions must be followed exactly.

Injection

Route: Parenteral

Strengths: 80 mg, 120 mg