Degarelix

Reconstitute the vials with the provided pre-filled syringes containing sterile water for inj. Add 4.2 mL to a vial containing 80 mg and 3 mL to a vial containing 120 mg. With the syringe attached to the adapter placed on top of the vial, gently swirl the vial until the liquid is clear with no visible particles or powder; do not shake to prevent foaming. Vials may be tilted slightly if the powder adheres to the side of the vial. Dissolution usually takes a few minutes but may take up to 15 minutes in some cases. To withdraw the reconstituted liquid for administration, turn the vial upside down and pull down the plunger up to the line mark on the syringe. Refer to specific product guidelines for further instructions on reconstitution.

Hypersensitivity.

Patient with congenital long QT syndrome, known history of or with other risk factors for QT prolongation (e.g. heart failure, electrolyte abnormalities, concomitant use of drugs known to prolong QT interval); diabetes. Moderate or severe renal and severe hepatic impairment. No relevant indication for use in women.

Significant: Hypersensitivity reactions (e.g. anaphylaxis, urticaria, angioedema), QT prolongation; decreased bone mineral density (prolonged use); increased risk of CV disease (e.g. MI, stroke), decreased glucose tolerance, diabetes.
Blood and lymphatic system disorders: Anaemia.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Nausea, diarrhoea, vomiting, constipation, abdominal pain or discomfort, dry mouth.
General disorders and administration site conditions: Inj site reactions (e.g. pain, erythema), chills, pyrexia, fatigue, influenza-like illness, malaise, peripheral oedema.
Investigations: Increased weight, cholesterol, liver transaminases, bilirubin, and alkaline phosphatase; decreased weight; changes in blood Ca.
Metabolism and nutrition disorders: Decreased appetite.
Musculoskeletal and connective tissue disorders: Musculoskeletal pain and discomfort, osteoporosis or osteopenia, muscular weakness, muscle spasms, arthralgia, joint swelling or stiffness.
Nervous system disorders: Headache, dizziness, hypoaesthesia.
Psychiatric disorders: Insomnia, depression, mental impairment.
Renal and urinary disorders: Pollakiuria, micturition urgency, dysuria, nocturia, renal impairment, incontinence.
Reproductive system and breast disorders: Gynaecomastia, testicular atrophy, erectile dysfunction, testicular pain, genital irritation, pelvic pain, ejaculation failure, breast pain, decreased libido.
Skin and subcutaneous tissue disorders: Hyperhidrosis (including night sweats), rash, erythema, urticaria, skin nodule, alopecia, pruritus.
Vascular disorders: Hot flush, hypertension, vasovagal reaction.

SC: X

Monitor PSA (periodically), serum testosterone levels (if PSA increases), bone mineral density; LFTs (at baseline and occasionally in patients with suspected hepatic dysfunction); electrolytes (e.g. Ca, Mg, K, Na), ECG (at baseline and periodically). Evaluate for diabetes and CV risk prior to treatment initiation and 3-6 months after initiation. Assess for signs and symptoms of hypersensitivity.

May increase the risk of QT prolongation with drugs known to prolong QT interval or drugs that may induce torsades de pointes such as class IA (e.g. quinidine, disopyramide) and class III (e.g. amiodarone, dofetilide, ibutilide, sotalol) antiarrhythmics, methadone, moxifloxacin, and antipsychotics.

May affect the results of diagnostic tests of pituitary gonadotrophic and gonadal functions.

Description:
Mechanism of Action: Degarelix is a gonadotrophin-releasing hormone (GnRH) antagonist. It selectively and reversibly binds to the pituitary GnRH receptors causing a rapid decrease in the release of gonadotrophins, luteinising hormone (LH) and follicle-stimulating hormone (FSH), thereby decreasing the secretion of testosterone by the testes.
Onset: Rapid.
Pharmacokinetics:
Absorption: Bioavailability: Biphasic release: Rapid initial release, then slow release from depot formed after SC inj. Time to peak plasma concentration: Within 2 days (loading dose).
Distribution: Volume of distribution: >1,000 L. Plasma protein binding: Approx 90%.
Metabolism: Metabolised in the liver via peptide hydrolysis.
Excretion: Via faeces (approx 70-80%, mainly as peptide fragments); urine (approx 20-30% as unchanged drug). Elimination half-life: Approx 43-53 days (loading dose); approx 28 days (maintenance dose).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 16136245, Degarelix. https://pubchem.ncbi.nlm.nih.gov/compound/Degarelix. Accessed Nov. 26, 2024.

Store below 30°C. Follow applicable procedures for receiving, handling, administration, and disposal.

Cancer Hormone Therapy

L02BX02 - degarelix ; Belongs to the class of other hormone antagonists and related agents. Used in the treatment of advanced prostate cancer.

Brayfield A, Cadart C (eds). Degarelix. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/11/2024.

Degarelix 120 mg Powder and Solvent for Solution for Injection (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/11/2024.

Degarelix. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 05/11/2024.

Firmagon (Ferring Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/11/2024.

Firmagon 80 mg Powder and Solvent for Solution for Injection (Ferring Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 05/11/2024.

Joint Formulary Committee. Degarelix. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/11/2024.