Trade Names:Nilandron- Tablets 50 mgAnandron (Canada)
Nonsteroidal with antiandrogen activity. It blocks the effects of testosterone at the androgen receptor level. The drug is rapidly and completely absorbed. There is moderate binding of the drug to plasma proteins. It is extensively metabolized. The majority is eliminated in the urine. Fecal elimination is negligible. The mean t ½ ranged from 38 to 59.1 h. Metabolic enzyme inhibition may occur for this drug.
Nilutamide is rapidly and completely absorbed. Steady state is 2 to 4 weeks (multiple dosing).
Nilutamide is moderately binding to plasma proteins and low binding to erythrocytes.
Nilutamide is extensively metabolized. Five metabolites have been isolated with several active.
Nilutamide is excreted in urine 62% (2% as unchanged) and feces 1.4% to 7%. The t ½ is 38 to 59.1 h.
Metastatic prostate cancer in combination with surgical castration.
Severe hepatic impairment; severe respiratory insufficiency; hypersensitivity to nilutamide or any component of this preparation.
PO 300 mg (6 tablets) once daily for 30 days.Maintenance dose
PO 150 mg (3 tablets) once daily.
Store at controlled room temperature (59° to 86°F); protect from light.
Inhibits hepatic CYP-450 enzymes. May alter the elimination of other agents metabolized by the CYP-450 system. Monitor patients for increased serum levels and toxicity during concomitant therapy with warfarin, phenytoin, or theophylline.
Increased ALT and AST.
Peripheral edema, hypertension, chest pain; heart failure.
Insomnia; headache; dizziness; depression; hypesthesia; asthenia; paresthesia.
Sweating; loss of body hair; dry skin.
Low potential for nausea and vomiting; constipation; anorexia; abdominal pain; hemorrhage or melena (2%).
Testicular atrophy; UTI.
Pain; bone pain.
Dyspnea; pneumonia; intestinal pneumonitis.
Delayed adjustment to dark or light; abnormal vision; cataract.
Interstitial pneumonitis has been reported in 2% of patients in clinical trials. Reports of interstitial changes including pulmonary fibrosis leading to hospitalization and death rarely reported in postmarketing surveillance. Most cases were reversible with discontinuation and occurred within the first 3 mo of therapy.
Assess serum transaminase levels prior to starting treatment and at regular intervals for the first 4 mo of treatment and periodically thereafter. Obtain LFTs at the first sign or symptoms suggestive of liver dysfunction.
Category C .
Safety and efficacy in children have not been established.
When passing from a lighted area to a dark area.
Severe liver injury has been reported. Hepatotoxicity in these reports generally occurred within the first 3 to 4 mo of treatment.
Nilutamide has no indication for women.
GI disorders, including nausea and vomiting, malaise, headache, dizziness (600 and 900 mg/day).
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