No

Antineoplastic Agent, Miscellaneous

In combination with surgical castration in treatment of metastatic prostatic carcinoma (Stage D₂); for maximum benefit, nilutamide treatment must begin on the same day as or on the day after surgical castration

C

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

The U.S. Food and Drug Administration (FDA) currently recommends that procedures for proper handling and disposal of antineoplastic agents be considered.

Hepatitis or marked increases in liver enzymes leading to drug discontinuation occurred in 1% of nilutamide patients. There has been a report of elevated hepatic enzymes followed by death in a 65 year old patient treated with nilutamide.

Foreign postmarketing surveillance has revealed isolated cases of aplastic anemia in which a causal relationship with nilutamide could not be ascertained.

13% to 57% of patients receiving nilutamide reported a delay in adaptation to the dark, ranging from seconds to a few minutes. This effect sometimes does not abate as drug treatment is continued. Caution patients who experience this effect about driving at night or through tunnels. This effect can be alleviated by wearing tinted glasses.

>10%:

Central nervous system: Pain, headache, insomnia

Gastrointestinal: Nausea, constipation, anorexia

Genitourinary: Impotence, testicular atrophy, gynecomastia

Endocrine & metabolic: Loss of libido, hot flashes

Neuromuscular & skeletal: Weakness

Ocular: Impaired adaption to dark

1% to 10%:

Cardiovascular: Hypertension

Central nervous system: Flu syndrome, fever, dizziness, depression, hypesthesia

Dermatologic: Alopecia, dry skin, rash

Gastrointestinal: Dyspepsia, vomiting, abdominal pain

Genitourinary: Urinary tract infection, hematuria, urinary tract disorder, nocturia

Ocular: Chromatopsia, impaired adaption to light, abnormal vision

Respiratory: Dyspnea, upper respiratory infection, pneumonia

Miscellaneous: Diaphoresis

One case of massive overdosage has been published. A 79-year old man attempted suicide by ingesting 13 g of nilutamide. There were no clinical signs or symptoms or changes in parameters such as transaminases or chest x-ray. Maintenance treatment (150 mg/day) was resumed 30 days later.

Management is supportive, dialysis not of benefit; induce vomiting if the patient is alert, general supportive care (including frequent monitoring of the vital signs and close observation of the patient)

Store at room temperature (15°C to 30°C/59°F to 86°F); protect from light

Nonsteroidal antiandrogen that inhibits androgen uptake or inhibits binding of androgen in target tissues

Absorption: Rapid and complete

Distribution: Moderately binds to plasma proteins and low binding to erythrocytes.

Metabolism: Extensive

Half-life: 38-59 hours

Elimination: All metabolites excreted primarily in urine

Adults: Oral: 6 tablets (50 mg each) once a day for a total daily dose of 300 mg for 30 days followed thereafter by 3 tablets (50 mg each) once a day for a total daily dose of 150 mg

Food: Can be taken without regard to food

Perform routine chest x-rays before treatment, and tell patients to report immediately any dyspnea or aggravation of pre-existing dyspnea. At the onset of dyspnea or worsening of pre-existing dyspnea any time during therapy, interrupt nilutamide until it can be determined if respiratory symptoms are drug-related. Obtain a chest x-ray, and if there are findings suggestive of interstitial pneumonitis, discontinue treatment with nilutamide. The pneumonitis is almost always reversible when treatment is discontinued. If the chest x-ray appears normal, perform pulmonary function tests.

Measure serum hepatic enzyme levels at baseline and at regular intervals (3 months); if transaminases increase over 2-3 times the upper limit of normal, discontinue treatment. Perform appropriate laboratory testing at the first symptom/sign of liver injury (eg, jaundice, dark urine, fatigue, abdominal pain or unexplained GI symptoms ) and nilutamide treatment must be discontinued immediately if transaminases exceed 3 times the upper limit of normal.

Insomnia is common; may cause dizziness or depression

None reported

No information available to require special precautions

No effects or complications reported

Take as prescribed; do not change dosing schedule or stop taking without consulting prescriber. Avoid alcohol while taking this medication; may cause severe reaction. Periodic laboratory tests are necessary while taking this medication. You may experience dizziness, confusion, or blurred vision (avoid driving or engaging in tasks that require alertness until response to drug is known); loss of light accommodation (avoid night driving and use caution in poorly lighted or changing light situations); impotence; or loss of libido (discuss with prescriber). Report any decreased respiratory function (eg, dyspnea, increased cough); yellowing of skin or eyes; change in color of urine or stool; unusual bruising or bleeding; chest pain; difficulty or painful voiding.

Tablet: 50 mg

Bertagna C, DeGery A, Hucher M, et al, "Efficacy of the Combination of Nilutamide Plus Orchidectomy in Patients With Metastatic Prostatic Cancer, A Meta-Analysis of Seven Randomized Double-Blind Trials (1056 Patients)," Br J Urol, 1994, 73(4):396-402.

Creaven PJ, Pendyala L, and Tremblay D, "Pharmacokinetics and Metabolism of Nilutamide," Urology, 1991, 37(2 Suppl):13-9.

Dole EJ and Holdsworth MT, "Nilutamide: An Antiandrogen for the Treatment of Prostate Cancer," Ann Pharmacother, 1997, 31(1):65-75.

Gaillard-Moguilewsky M, de Gery A, and Ulmann A, "Pharmacology of Nilutamide," Cancer, 1993, 72(12 Suppl):3828-9.

Harris MG, Coleman SG, Faulds D, et al, "Nilutamide. A Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Prostate Cancer," Drugs Aging, 1993, 3(1):9-25.