Bicalutamide

Trade Names:
Casodex
- Tablets for oral use 50 mg

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

The 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

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

Prothrombin 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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