Nilutamide

Black Box Warnings

Interstitial pneumonitis has been reported in 2% of patients exposed to nilutamide. Reports of interstitial changes including pulmonary fibrosis leading to hospitalization and death rarely reported in post marketing surveillance. Most cases were reversible with discontinuation and occurred within first 3 months of therapy

Contraindications

Hypersensitivity; severe hepatic, and/or respiratory impairment

Cautions

Hepatic Impairment

Hepatitis reported

Delay in vision adaptation to dark

One case of massive overdosage has been published. A 79-year-old man attempted suicide by ingesting 13 g of nilutamide (i.e., 43 times the maximum recommended dose). Despite immediate gastric lavage and oral administration of activated charcoal, plasma nilutamide levels peaked at 6 times the normal range 2 hours after ingestion. 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.

In repeated-dose tolerance studies, doses of 600 mg/day and 900 mg/day were administered to 9 and 4 patients, respectively. The ingestion of these doses was associated with gastrointestinal disorders, including nausea and vomiting, malaise, headache, and dizziness. In addition, a transient elevation in hepatic enzyme levels was noted in one patient.

Since nilutamide is protein bound, dialysis may not be useful as treatment for overdose. As in the management of overdosage with any drug, it should be borne in mind that multiple agents may have been taken. If vomiting does not occur spontaneously, it should be induced if the patient is alert. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated.

Prostate Cancer

Adjunct to orchiectomy in the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (stage D2).1 2 3 5 6 7 8 24 30 33

Slows progression of the disease, relieves bone pain associated with metastatic disease, and improves overall survival rate after long-term therapy (8.5 years).3 5 6 7 9 30

General

• Determine PSA concentrations periodically during therapy to monitor therapeutic response, including successful remission or possible progression of cancer.9 30

• If PSA concentrations increase substantially and consistently during therapy, evaluate the possibility of clinical progression.29

Administration

Oral Administration

Administer orally once daily without regard to meals.1 9

Dosage

Adults

300 mg once daily for 30 days, followed by 150 mg given once daily thereafter.1 For maximum benefit, initiate nilutamide on the day of or the day after orchiectomy.1

Duration of therapy depends on the duration of clinical response of the patient.29

Inhibits the activity of CYP isoenzymes; may reduce the metabolism of drugs metabolized by these systems.a

Specific Drugs

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Nilutamide Tablets, 150 mg
NDC 62559-173-31
Rx only
30 (3 x 10) Unit-of-Use Tablets

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Nilandron: 150 mg [DSC]

Nilandron: 150 mg [contains corn starch]

Generic: 150 mg

• Nilandron

Interstitial pneumonitis has been reported in 2% of patients in controlled clinical trials in patients exposed to nilutamide. A small study in Japanese patients showed that 17% of patients developed interstitial pneumonitis. Reports of interstitial changes, including pulmonary fibrosis that led to hospitalization and death, have been reported rarely in postmarketing. Symptoms included exertional dyspnea, cough, chest pain, and fever. X-rays showed interstitial or alveolo-interstitial changes, and pulmonary function tests revealed a restrictive pattern with decreased diffusing capacity of lungs for carbon monoxide. Most cases occurred within the first 3 months of treatment with nilutamide, and most reversed with discontinuation of therapy. Perform a routine chest x-ray prior to initiating treatment with nilutamide. Consider baseline pulmonary function tests. Instruct patients to report any new or worsening shortness of breath that they experience while on nilutamide. If symptoms occur, immediately discontinue nilutamide until it can be determined if the symptoms are drug related.

Animal reproduction studies have not been conducted. Nilutamide is not indicated for use in women.

Commonly reported side effects of nilutamide include: nausea, nocturnal amblyopia, and decreased libido. Other side effects include: hemeralopia, visual disturbance, chromatopsia, and loss of body hair. See below for a comprehensive list of adverse effects.