Full Prescribing Info
Each tablet contains: Bicalutamide 50 mg.
Treatment of advanced prostate cancer in combination with LHRH analog therapy or surgical castration.
Prevention of disease flare associated with the use of LHRH agonists.
Dosage/Direction for Use
One tablet (50 mg) once daily, in the morning or evening at the same time each day, with or without food.
Start bicalutamide treatment at the same time as treatment with an LHRH analog or surgical castration.
Hypersensitivity to bicalutamide or any component of the product.
Females and children.
Special Precautions
Hepatitis: The use of bicalutamide has been associated with rare cases of death or hospitalization due to severe liver injury which generally occurred within the first three to four months of treatment.
Liver function tests (bilirubin, transaminases, alkaline phosphatase) should be measured before starting bicalutamide treatment and at regular intervals for the first four months of treatment, and periodically thereafter. Measure serum transaminases (particularly serum alanine aminotransferase, ALT) immediately if clinical signs or symptoms suggestive of liver dysfunction occur (e.g., nausea, vomiting, abdominal pain, fatigue, anorexia, "flu-like" symptoms, dark urine, jaundice, or right upper quadrant tenderness). Discontinue bicalutamide immediately and closely follow-up liver function in the event of clinical and/or biochemical evidence of severe hepatotoxicity (e.g., jaundice or an increase in serum ALT concentration greater than 2 times the upper limit of normal).
Gynecomastia and Breast Pain: Gynecomastia and breast pain have been reported in clinical trials using bicalutamide 150 mg as a single agent for prostate cancer.
Glucose Tolerance: Reduced glucose tolerance manifested as diabetes or loss of glycemic control in patients with pre-existing diabetes, has been observed in males receiving LHRH agonists. Monitor blood glucose levels in patients receiving combination therapy with bicalutamide and LHRH agonists.
Serum Prostate Specific Antigen (PSA) Monitoring: Periodic monitoring of PSA levels may be useful in assessing patient's response to therapy. A treatment-free period of antiandrogen while continuing the LHRH analog may be considered in patients who have increased PSA levels and objective disease progression.
Use in Adult Males with Liver Impairment: Although no dosage adjustment is required in patients with mild liver impairment, increased accumulation may occur in patients with moderate to severe liver impairment.
Use in Adult Males with Renal Impairment: No dosage adjustment is required in patients with renal impairment.
Use In Pregnancy & Lactation
Pregnancy Category X: Bicalutamide is contraindicated in females and must not be given to pregnant or breastfeeding women.
Adverse Reactions
Body (general): Edema, neoplasm, cyst, hernia, infection, fever, chills, sepsis fatigue, and flu syndrome. Pain in the back, pelvic, chest, neck, and abdomen.
Cardiovascular: Angina pectoris, congestive heart failure, hypertension, myocardial infarction, coronary artery disorder, and hot flushes. Conduction defects including PR and QT interval prolongations, arrhythmias and non-specific ECG changes have been observed.
Gastrointestinal: Anorexia, heartburn, dyspepsia, dysphagia, periodontal abscess, rectal hemorrhage, gastrointestinal cancer, dry mouth, melena, flatulence, constipation, diarrhea, nausea, and vomiting.
Endocrine: Breast pain and/or tenderness, gynecomastia and diabetes mellitus.
Metabolic and Nutritional: Weight gain, dehydration, gout, peripheral edema/fluid retention, hyperglycemia, and weight loss.
Hematological: Anemia, leukopenia and thrombocytopenia.
Musculoskeletal: Myasthenia, asthenia, arthritis, myalgia, leg cramps, pathological fracture, bone pain.
CNS: Anxiety, headache, depression, hypertonia, somnolence, confusion, neuropathy, nervousness, dizziness, paresthesia, and insomnia.
Respiratory: Interstitial lung disease, increased cough, pharyngitis, bronchitis, pneumonia, asthma, epistaxis, sinusitis, rhinitis, pulmonary disorders, and dyspnea.
Immune System Disorders: Hypersensitivity reactions, including angioneurotic edema and urticaria.
Skin and Appendages: Pruritus, dry skin, Herpes Zoster, skin carcinoma, alopecia, rash, sweating, and hirsutism.
Hepatic Effects: Jaundice and hepatic failure.
Urogenital: Increased urinary frequency, urinary impairment, dysuria, urinary retention, urinary urgency, nocturia, hematuria, urinary tract infection, impotence, and hydronephrosis.
Special senses: Cataract.
Abnormal Laboratory Test Values: Elevated aspartate aminotransferase (AST), alanine aminotransferase (ALT), bilirubin, blood urea nitrogen (BUN), and creatinine; decreased hemoglobin and white blood cells (WBC). Elevated hepatic enzymes and decreased hemoglobin were less frequently reported.
Drug Interactions
R-bicalutamide has been shown in vitro to be an inhibitor of CYP3A4 activity, with lesser inhibitory effects on CYP 2C9, 2C19 and 2D6. Exercise caution when giving bicalutamide concomitantly with midazolam (a CYP 3A4 substrate) since midazolam Cmax and AUC have been shown to increase 1.5 and 1.9 fold, respectively, in clinical trials.
Bicalutamide displaces warfarin (coumarin anticoagulant) from its protein binding site in vitro. Close monitoring of prothrombin time is therefore recommended in patients who are already receiving coumarin anticoagulants.
Although no pharmacodynamic or pharmacokinetic interaction exists between bicalutamide and LHRH agonists, bicalutamide may prevent the harmful clinical consequences of flare associated with LHRH agonist therapy.
Co-administration of ciclosporin and calcium channel blockers with bicalutamide may theoretically increase bicalutamide's plasma concentrations. Evidence of enhanced or adverse drug effect may warrant dose reduction and close monitoring of patients after initiation or cessation of bicalutamide.
Drugs which inhibit drug oxidation such as cimetidine and ketoconazole may theoretically increase plasma concentrations of bicalutamide which may result in increased side effects.
Concomitant administration with alcohol should be avoided to prevent facial flushing during bicalutamide therapy.
ATC Classification
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Tab 50 mg x 28's.
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in