Bicalutamide

Registered South African indications:

• Advanced prostate cancer

Contraindications

South African recommendations

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Children
• Females

Recommendations in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Children
• Females
• Coadministration of terfenadine, astemizole or cisapride

Cautions

• Moderate to severe hepatic impairment
• Porphyria
• Males and females of reproductive potential
• History of or risk factors for QT prolongation 
• Objective progression of disease together with increased PSA
• Exposure to excessive sunlight or ultraviolet light
• Patients on anticoagulant therapy
• Lactose allergy
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

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

Dosages below include:

• South African registered indications and dosages

South African registered indications and dosages

Used for the treatment of

Advanced prostate cancer (Additional agent required)
- In combination with luteinising hormone release hormone (LHRH) analogue therapy or surgical castration

• Oral (fct): Initial: 50mg, once daily; Treatment with bicalutamide should be started at least 3 days prior to commencing treatment with a LHRH analogue, or at the same time as surgical castration

Locally advanced prostate cancer (T3-4, any N, M0/T1-2, N+, M0)
- As immediate therapy either alone or as adjuvant to treatment by radical prostatectomy or radiotherapy
- As monotherapy for the management of patients with locally advanced, non-metastatic prostate cancer for whom surgical or medical castration is not appropriate

• Oral (fct): Initial: 150mg, once daily for two years or until progression

Consult specialist for dosages and regimens

Contraindicated

Pregnancy

• Contraindicated
• Bicalutamide is contraindicated in females and should not be used during pregnancy

Breastfeeding

• Contraindicated
• Bicalutamide is contraindicated in females and should not be used during breastfeeding

Fertility

• Reversible impairment of male fertility has been observed in animal studies. A period of subfertility or infertility should be assumed in man
• Antiandrogen therapy may cause morphological changes in spermatozoa. Although the effect of bicalutamide on sperm morphology has not been evaluated and no such changes have been reported for patients who received bicalutamide, patients and/or their partners should follow adequate contraception during and for 130 days after bicalutamide therapy

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Mild (Child-Pugh Class A): No dose adjustment is recommended 
• Moderate-to-severe (Child-Pugh Classes B & C): Caution; no dose adjustment recommended
  Use with caution as clearance may be delayed in severe impairment. If an increase of ALT > 2 times ULN or development of jaundice: discontinue immediately

Elderly            

• No dose adjustment recommended

Porphyria Information

• Possibly porphyrinogenic (PSP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Dizziness
• Somnolence
• Depression
• Asthenia
• Headache

Cardiovascular Disorders

• Cardiac failure
• Angina
• Conduction defects
• PR prolongation
• QT prolongation
• Arrhythmias
• Non-specific ECG changes
• Hot flush
• Chest pain

Respiratory Disorders

• Interstitial lung disease
• Dyspnoea

Gastrointestinal Disorders

• Abdominal pain
• Constipation
• Nausea
• Dyspepsia
• Flatulence

Hepatobiliary Disorders

• Hepatotoxicity
• Jaundice
• Hypertransaminasaemia
• Hepatic failure

Genitourinary Disorders

• Haematuria
• Nocturia
• Gynaecomastia
• Breast tenderness
• Erectile dysfunction
• Decreased libido
• Pelvic pain

Endocrine and Metabolic Disorders

• Decreased appetite
• Increased weight
• Decreased weight
• Hyperglycaemia
• Diabetes mellitus

Skin and Subcutaneous Tissue Disorders

• Alopecia
• Hirsutism
• Hair re-growth
• Dry skin
• Pruritus
• Rash
• Photosensitivity reaction
• Urticaria

Immune, Blood and Lymphatic System Disorders

• Anaemia
• Thrombocytopenia
• Hypersensitivity
• Angioedema
• Oedema
• Chills

• CYP3A4 substrate
• Terfenadine
• Astemizole  
• Cisapride
• Ciclosporin
• Calcium channel blockers
• Agents which may inhibit drug oxidation
• Cimetidine
• Ketoconazole
• Warfarin
• QT prolonging agents
• Class IA antiarrhythmic agents
• Quinidine
• Disopyramide
• Class III antiarrhythmic agents
• Amiodrarone
• Sotalol
• Dofetilide
• Ibutilide
• Midazolam

• Hepatic function
• Full blood count
• Electrocardiogram
• Echocardiogram
• Serum testosterone
• Luteinizing hormone
• Prostate specific antigen

Specific cases may require

• Blood glucose
• Prothrombin time

Bicalutamide is a non-steroidal anti-androgen, devoid of other endocrine activity. It binds to the wild type or normal androgen receptor without activating gene expression, and thus inhibits the androgen stimulus. Regression of prostatic tumours results from this inhibition. Clinically, discontinuation of bicalutamide can result in the 'antiandrogen withdrawal syndrome' in a subset of patients.

Tablet 50mg

• Anandroca (Zydus)
• Bicadex (Cipla)
• Casodex (AstraZeneca) originator
• Sandoz Bicalutamide (Sandoz)
• Spec Bicalutamide (Specpharm)

Film-coated tablet 50mg

• Accord Bicalutamide (Accord)
• Bicalox (Pharmaplan)
• Bicalutamide 50mg Hetero (Hetero Drugs)
• Caloxa (Eurolab)
• Teva Bicalutamide (Teva)

Tablet 150mg

• Casodex (AstraZeneca) originator
• Tasdiam (Eurolab)
• Teva Bicalutamide (Teva)

Film-coated tablet 150mg

• Bicalutamide 150 Accord (Accord)
• Spec Bicalutamide 150 (Specpharm)
• Tasdiam (Eurolab)
• Teva Bicalutamide (Teva)