Bicalutamide
Pronunciation: (BYE-kah-LOO-tah-mide)Class: Antiandrogen
Trade Names:
Casodex
- Tablets for oral use 50 mg
Novo-Bicalutamide (Canada)
PMS-Bicaltamide (Canada)
ratio-Bicalutamide (Canada)
Sandoz Bicalutamide (Canada)
Pharmacology
Bicalutamide inhibits the action of androgens.
Pharmacokinetics
Absorption
Well absorbed. T max is 31.3 h (active isomer). C max is 0.77 mcg/mL (active isomer).
Distribution
96% protein bound.
Metabolism
Undergoes stereospecific metabolism. The S-isomer (inactive) is metabolized by glucuronidation. The R-isomer (active) undergoes glucuronidation but is predominantly oxidized to an inactive metabolite.
Elimination
Eliminated in urine and feces; t ½ is 5.8 days (active isomer).
Special Populations
Hepatic Function ImpairmentThe t ½ of the R-isomer is increased about 76% in patients with severe liver disease. No dosage adjustment is necessary.
Indications and Usage
Advanced prostate cancer in combination with a luteinizing hormone releasing hormone (LHRH) analog. Safety and efficacy not established.
Contraindications
Standard considerations.
Dosage and Administration
Advanced Prostate CancerAdults
PO 50 mg (1 tablet) once daily at the same time of day with or without food.
Storage/Stability
Store tablets at controlled room temperature (68° to 77°F).
Drug Interactions
WarfarinProthrombin time may increase when bicalutamide is initiated in patients stabilized on chronic warfarin therapy.
Laboratory Test Interactions
Elevated AST, ALT, bilirubin, BUN, and creatinine, and decreased hemoglobin and white cell count.
Adverse Reactions
Cardiovascular
Angina pectoris; CHF; hypertension.
CNS
Myasthenia; anxiety; depression; confusion; somnolence; nervousness; loss of libido; neuropathy.
Dermatologic
Dry skin; pruritus; alopecia.
Endocrine
Hot flashes; gynecomastia; breast pain; diabetes mellitus.
GI
Anorexia; dyspepsia; rectal hemorrhage; melena; increased liver function enzymes.
Genitourinary
Impotence; nocturia; hematuria; reduced sperm count.
Musculoskeletal
Arthritis; myalgia; leg cramps; hypertonia.
Respiratory
Increased cough; pharyngitis; bronchitis; pneumonia; rhinitis; lung disorder.
Precautions
Pregnancy
Category X .
Lactation
Bicalutamide is not indicated for use in women.
Children
Safety and efficacy not established.
Hepatic Function
Use bicalutamide with caution in patients with moderate to severe hepatic function impairment.
Gynecomastia/Breast pain
Reported in patients treated for prostate cancer.
Hepatotoxicity
Generally occurred within the first 3 to 4 mo of treatment.
Women
Do not use in women.
Patient Information
- Notify health care provider if any of the following symptoms occur: nausea, vomiting, abdominal pain, fatigue, anorexia, “flu-like” symptoms, dark urine, jaundice, right upper quadrant tenderness.
- Bicalutamide and the LHRH analog will be initiated at the same time. Do not interrupt or stop taking these medications without consulting health care provider.
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More Bicalutamide resources
Bicalutamide - Includes detailed dosage instructions.
Bicalutamide Drug Interactions
