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Nilutamide

Pronouncation: (nye-LOO-tah-mide)
Class: Antiandrogen

Trade Names:
Nilandron
- Tablets 50 mg

Anandron (Canada)

Pharmacology

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As a treatment for...	Avg User Ratings [?]
Prostate Cancer	Be the first to rate it 0 comments

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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 59.1ߙh. Metabolic enzyme inhibition may occur for this drug.

Pharmacokinetics

Absorption

Nilutamide is rapidly and completely absorbed. Steady state is 2 to 4 weeks (multiple dosing).

Distribution

Nilutamide is moderately binding to plasma proteins and low binding to erythrocytes.

Metabolism

Nilutamide is extensively metabolized. Five metabolites have been isolated with several active.

Elimination

Nilutamide is excreted in urine 62% (2% as unchanged) and feces 1.4% to 7%. The t _½ is 38 to 59.1 h.

Indications and Usage

Metastatic prostate cancer in combination with surgical castration.

Contraindications

Severe hepatic impairment; severe respiratory insufficiency; hypersensitivity to nilutamide or any component of this preparation.

Dosage and Administration

Prostate Cancer
Adults Initial dose

PO 300 mg (6 tablets) once daily for 30 days.

Maintenance dose

PO 150 mg (3ߙtablets) once daily.

General Advice

Initiate therapy on day of surgical castration or the day after surgery. Nilutamide may be taken without regard to meals.

Storage/Stability

Store at controlled room temperature (59° to 86°F); protect from light.

Drug Interactions

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.

Laboratory Test Interactions

Increased ALT and AST.

Adverse Reactions

Cardiovascular

Peripheral edema, hypertension, chest pain; heart failure.

CNS

Insomnia; headache; dizziness; depression; hypesthesia; asthenia; paresthesia.

Dermatologic

Sweating; loss of body hair; dry skin.

Endocrine

Hot flashes.

GI

Low potential for nausea and vomiting; constipation; anorexia; abdominal pain; hemorrhage or melena (2%).

Genitourinary

Testicular atrophy; UTI.

Hematologic

Anemia.

Metabolic

Alcohol intolerance.

Musculoskeletal

Pain; bone pain.

Respiratory

Dyspnea; pneumonia; intestinal pneumonitis.

Special Senses

Delayed adjustment to dark or light; abnormal vision; cataract.

Miscellaneous

Flu-like syndrome.

Precautions

Warnings

Interstitial pneumonitis

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.

Monitor

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.

Pregnancy

Category C .

Children

Safety and efficacy in children have not been established.

Delay in adaptation to the dark

When passing from a lighted area to a dark area.

Hepatitis

Severe liver injury has been reported. Hepatotoxicity in these reports generally occurred within the first 3 to 4ߙmo of treatment.

Women

Nilutamide has no indication for women.

Overdosage

Symptoms

GI disorders, including nausea and vomiting, malaise, headache, dizziness (600 and 900 mg/day).

Patient Information

Start nilutamide tablets on the day of, or the day after, surgical castration. Patients should not interrupt their dosing of nilutamide or stop taking the medication without consulting their health care provider.
Delays of visual adaptation from light to dark may occur. Advise patients to use caution when driving at night or through tunnels. Patients can use tinted glasses to help decrease the problem.
Nilutamide may cause alcohol-intolerance. Avoid alcohol if facial flushing, malaise, or hypotension occurs after consuming alcoholic beverages.
Notify your doctor at the first sign or symptoms suggestive of liver dysfunction (eg, nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like symptoms, dark urine, jaundice, right upper quadrant tenderness).
Tell health care provider immediately of any dyspnea or aggravation of preexisting dyspnea.
Instruct patients to report any new or worsening shortness of breath that they experience while on nilutamide. If symptoms occur, discontinue nilutamide immediately until it can be determined if the symptoms are drug-related.