Pronunciation: BYE-ka-LOO-ta-mide
Class: Antiandrogen

Trade Names

Bicalutamide
- Tablets 50 mg

Casodex
- Tablets 50 mg

CO Bicalutamide (Canada)
Novo-Bicalutamide (Canada)
PMS-Bicaltamide (Canada)
ratio-Bicalutamide (Canada)
Sandoz Bicalutamide (Canada)

Pharmacology

Bicalutamide inhibits the action of androgens.

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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; half-life is 5.8 days (active isomer).

Special Populations

Renal Function Impairment

No dosage adjustment is necessary.

Hepatic Function Impairment

The half-life of the R-isomer is increased about 76% in patients with severe liver disease. No dosage adjustment is necessary.

Indications and Usage

Stage D ₂ metastatic carcinoma of the prostate in combination with a luteinizing hormone–releasing hormone (LHRH) analog.

Contraindications

Women; pregnancy; hypersensitivity to the drug or any of the tablet components.

Dosage and Administration

Advanced Prostate Cancer
Adults

PO 50 mg (1 tablet) once daily at the same time of day with or without food.

General Advice

• Start bicalutamide at the same time as treatment with an LHRH analog.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F).

Drug Interactions

CYP3A4 substrates (eg, midazolam)

Mean midazolam C _max increased 1.5-fold and AUC increased 1.9-fold when given with bicalutamide. Use caution when coadministered with CYP3A4 substrates.

Warfarin

PT may increase when bicalutamide is initiated in patients stabilized on long-term warfarin therapy.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hot flashes (53%); hypertension (8%); angina pectoris, CHF, coronary artery disease, heart arrest, MI, syncope (2% to 5%).

CNS

Asthenia (22%); dizziness (10%); paresthesia (8%); headache, insomnia (7%); anxiety (5%); depression (4%); confusion, hypertonia, libido decreased, nervousness, neuropathy, somnolence (2% to 5%).

Dermatologic

Rash (9%); sweating (6%); alopecia, dry skin, herpes zoster, pruritus, skin carcinoma, skin disorder (2% to 5%).

GI

Constipation (22%); nausea (15%); diarrhea (12%); abdominal pain (11%); dyspepsia, liver enzymes increased (7%); anorexia, flatulence, vomiting (6%); dry mouth, dysphagia, GI carcinoma, GI disorder, melena, periodontal abscess, rectal hemorrhage (2% to 5%).

Genitourinary

Hematuria, nocturia (12%); gynecomastia, UTI (9%); impotence (7%); breast pain, urinary frequency (6%); impaired urination, urinary retention (5%); urinary incontinence (4%); dysuria, hydronephrosis, urinary tract disorder, urinary urgency (2% to 5%).

Metabolic-Nutritional

Peripheral edema (13%); weight loss (7%); hyperglycemia (6%); alkaline phosphatase increased, weight gain (5%); BUN increased, creatinine increased, dehydration, edema, gout, hypercholesterolemia (2% to 5%).

Musculoskeletal

Back pain (25%); bone pain (9%); myasthenia (7%); arthritis (5%); pathological fracture (4%); leg cramps, myalgia (2% to 5%).

Respiratory

Dyspnea (13%); cough increased, pharyngitis (8%); bronchitis (6%); pneumonia, rhinitis (4%); asthma, epistaxis, lung disorder, sinusitis (2% to 5%); interstitial lung disease, including interstitial pneumonitis and pulmonary fibrosis (postmarketing).

Miscellaneous

General pain (35%); pelvic pain (21%); infection (18%); anemia (11%); chest pain (8%); flu syndrome (7%); cataract specified, chills, cyst, fever, hernia, neck pain, neoplasm, sepsis (2% to 5%).

Precautions

Monitor Regularly monitor prostate-specific antigen and evaluate for clinical progression if levels rise. Measure serum transaminase levels prior to starting bicalutamide, at regular intervals for the first 4 mo, and periodically thereafter. Discontinue if patient develops jaundice or if ALT rises above 2 times the ULN.

Pregnancy

Category X .

Lactation

Bicalutamide is not indicated for use in women.

Children

Safety and efficacy not established.

Hypersensitivity

Reactions, including angioneurotic edema and urticaria, have been reported.

Hepatic Function

Use bicalutamide with caution in patients with moderate to severe hepatic function impairment.

Fertility

Administration of bicalutamide may lead to inhibition of spermatogenesis. Long-term effects are not known.

Hazardous Tasks

Somnolence has been reported during treatment with bicalutamide. Advise patients to use caution when driving or operating machinery.

Glucose tolerance

Reduction in glucose tolerance reported in men receiving LHRH agonists. Consider monitoring blood glucose in patients receiving bicalutamide in combination with LHRH agonists.

Gynecomastia/Breast pain

Reported in patients treated for prostate cancer.

Hepatotoxicity

Rare cases of death or hospitalization because of severe liver injury. Generally occurred within the first 3 to 4 mo of treatment.

Patient Information

• Advise patients to notify health care provider if any of the following symptoms occur: abdominal pain, anorexia, dark urine, fatigue, “flu-like” symptoms, jaundice, nausea, right upper quadrant tenderness, vomiting.
• Inform patients that bicalutamide and the LHRH analog will be initiated at the same time and not to interrupt or stop taking these medications without consulting health care provider.
• Advise patients that bicalutamide may cause drowsiness and to use caution when driving or operating machinery.

Copyright © 2009 Wolters Kluwer Health.