bicalutamide (Rx)

>10%

Hot flashes (53%)

General pain (35%)

Back pain (25%)

Asthenia (22%)

Constipation (22%)

Pelvic pain (21%)

Infection (18%)

Nausea (15%)

Dyspnea (13%)

Edema (13%)

Peripheral edema (13%)

Diarrhea (12%)

Hematuria (12%)

Nocturia (12%)

Abdominal pain (11%)

Anemia (11%)

1-10%

Gynecomastia (9%)

Rash (9%)

UTI (9%)

Chest pain (8%)

Hypertension (8%)

Vomiting (8%)

Flu like symptoms (7%)

Headache (7%)

LFTs elevation (7%)

Weight loss (7%)

Anorexia (6%)

Breast pain (6%)

Anxiety (5%)

Arthritis (5%)

Postmarketing reports

Photosensitivity

Interstitial lung disease including interstitial pneumonitis and pulmonary fibrosis

Contraindications

Hypersensitivity

Female patients (esp pregnant-may harm fetus)

Cautions

Hepatic impairment

Severe liver injury resulting in hospitalization or death reported

Spermatogenesi inhibition reported

Gynecomastia and breast pain reported during therapy when used as single agent

May reduce glucose tolerance in males when used in combination with LHRH; monitor blood glucose

Monitor prostate specific antigen (PSA) progression if PSA increases

Antiandrogen therapy may cause morphological changes in spermatozoa; based on findings in animal reproduction studies and its mechanism of action, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 130 days after administering final dose administered

Based on animal studies, therapy can lead to inhibition of spermatogenesis and may impair fertility in males of reproductive potential; long-term effects on male fertility not studied

Pregnancy

Contraindicated for use in pregnant women because it can cause fetal harm; not indicated for use in females; there are no human data on use in pregnant women; in animal reproduction studies, oral administration of bicalutamide to pregnant rats during organogenesis caused abnormal development of reproductive organs in male fetuses at exposures approximately 0.7 to 2 times the human exposure at recommended dose

Lactation

Not indicated for use in pregnant women; there is no information available on presence of bicalutamide in human milk, or on effects on breastfed infant or on milk production; bicalutamide has been detected in rat milk

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Nonsteroidal antiandrogen, competitively binds androgen receptors and inhibits testosterone stimulation of cell growth in prostate cancer

Pharmacokinetics

Half-Life: 5.8 d

Peak plasma time: 31 hr

Peak plasma concentration: 0.77 mcg/mL

Protein Bound: 96%

Metabolism: Liver

Clearance: 0.32 L/hr

Excretion: Urine (36%), feces (42%)

Dialyzable: No