Degarelix

Registered South African indications:

• Prostate cancer

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Severe renal impairment
• Severe hepatic impairment
• Males of reproductive potential
• Long-term androgen deprivation therapy
• History of a corrected QT interval over 450msec
• History of or risk factors for torsades de pointes 
• History of severe untreated asthma
• History of anaphylactic reactions
• Severe urticaria or angioedema
• Orchiectomy patients
• Diabetes mellitus
• Cardiovascular risk factors
• May impair ability to drive or operate machinery

Forms avail. in SA and covered in this monograph: inj

Used for the treatment of

• Advanced hormone-dependent prostate cancer
  - In whom androgen deprivation is warranted

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Consult specialist for dosages and regimens

Not indicated for use in children

Pregnancy

• Not indicated for use in women
• There is no relevant indication for use of degarelix in women

Breastfeeding

• Not indicated for use in women
• There is no relevant indication for use of degarelix in women

Fertility

• Degarelix may inhibit male fertility as long as the testosterone is suppressed

Renal Impairment

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no information available
  Degarelix has not been studied in severe renal impairment

Hepatic Impairment

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no information available
  Patients with severe hepatic dysfunction have not been studied

Elderly

• No dose adjustment recommended

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dizziness
• Headache
• Mental impairment
• Hypoaesthesia
• Insomnia
• Depression
• Decreased libido
• Fatigue

Cardiovascular Disorders

• Cardiac arrhythmia
• Atrial fibrillation
• Palpitations
• QT prolongation
• Myocardial infarction
• Cardiac failure
• Hot flush
• Hypertension
• Vasovagal reaction
• Hypotension

Respiratory Disorders

• Dyspnoea

Gastrointestinal Disorders

• Diarrhoea
• Nausea and vomiting
• Constipation
• Abdominal pain
• Abdominal discomfort
• Dry mouth

Hepatobiliary Disorders

• Increased hepatic transaminases
• Increased bilirubin
• Increased alkaline phosphatase

Genitourinary Disorders

• Pollakiuria
• Micturition urgency
• Dysuria
• Nocturia
• Renal impairment
• Incontinence
• Gynaecomastia
• Testicular atrophy
• Erectile dysfunction
• Testicular pain
• Breast pain
• Pelvic pain
• Genital irritation
• Ejaculation failure

Endocrine and Metabolic Disorders

• Increased weight
• Hyperglycemia
• Diabetes mellitus
• Increased cholesterol
• Decreased weight
• Decreased appetite
• Changes in blood calcium

Musculoskeletal Disorders

• Musculoskeletal pain and discomfort
• Osteoporosis
• Osteopenia
• Arthralgia
• Muscular weakness
• Muscle spasms
• Joint swelling/stiffness
• Rhabdomyolysis

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis
• Night sweats
• Rash
• Urticaria
• Skin nodule
• Alopecia
• Pruritus
• Erythema
• Injection site adverse reactions

Immune, Blood and Lymphatic System Disorders

• Anaemia
• Neutropenic fever
• Hypersensitivity
• Anaphylactic reactions
• Chills
• Fever
• Influenza-like illness
• Peripheral oedema

Sensory Disorders

• Blurred vision

• QT prolonging agents  
• Agents able to induce Torsades de pointes  
• Class I antiarrhythmics  
• Qunidine  
• Disopyramide  
• Class III antiarrhythmics  
• Amiodarone  
• Sotalol  
• Dofetilide  
• Ibutilide  
• Methadone  
• Moxifloxacin  
• Antipsychotics  

• Prostate-specific antigen
• Serum testosterone levels

Specific cases may require:

• Hepatic function
• Electrolytes
• Bone mineral density
• ECG
• Blood glucose
• Blood pressure
• Lipid profile

Degarelix is a selective gonadotrophin releasing-hormone (GnRH) antagonist that competitively and reversibly binds to the pituitary GnRH receptors, thereby rapidly reducing the release of the gonadotrophins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), and thereby reducing the secretion of testosterone (T) by the testes. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that removes the source of androgen. Unlike GnRH agonists, GnRH antagonists do not induce a LH surge with subsequent testosterone surge/tumour stimulation and potential symptomatic flare after the initiation of treatment.

Injection (per vial) 80mg

• Firmagon (Ferring) originator

Injection (per vial) 120mg

• Firmagon (Ferring) originator