Systemic Therapy Program

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Cancer Type

Document Type

Drug Monographs
Treatment Regimens

Scientific Name:
NILUTAMIDE
Brand Name(s):
Anandron®

Drug Monograph

Pharmacology

Mechanism of Action

Nilutamide acts as an antiandrogen by inhibiting androgen uptake and/or inhibiting nuclear binding of androgen in target tissues. It specifically blocks the action of androgens by interacting with cytosolic androgen receptor F sites in the target tissues.

Pharmacokinetics

Oral Absorption:
yes, rapidly and completely
Distribution:
no information
cross blood brain barrier? no information
Vd:  no information
PPB: 80%-84% to plasma proteins, some binding to erythrocytes
Metabolism:
liver, involves hepatic microsomal enzyme oxidation system
metabolite(s): active- yes inactive- yes
Excretion:
mainly in urine as metabolites (67% to 78%); hepatic: 1% to 7%; 1.4-7% in feces within 4-6 days
Urine: 67%-78%, <2% unchanged
t½  mean: 50 hours (range: 23-87 hours)
Cl:  no information

Side Effects

IMMEDIATE ONSET (hours to days)
• nausea, vomiting (10-30%, mild, transient)

EARLY ONSET (days to weeks)
• vision problems (27%, light-to-dark adaptation and colour perception)
• breast swelling or soreness (4-44%, gynecomastia)
• hot flushes (28-77%)
• nausea, vomiting (10-30%, mild, transient)
• liver problems (8%, elevated liver function tests, transient)
• gastrointestinal problems (constipation, gastric pain)
• blood problems (4%, anemia)
• lung problems (6%, dyspnea)
• dizziness
• fatigue

DELAYED/LATE ONSET (weeks to years)
• liver problems (rare, hepatitis)
• lung problems (rare, interstitial lung disease)

Therapeutics

Approved Indications

• Prostate cancer

Routes

Oral

Dose Adjustment Criteria

Hepatic failure
STOP if AST or ALT > 105IU/L
 (Suggested action)

Contraindications

• Known hypersensitivity to nilutamide • Severe low RBC (anemia) • Severe liver failure

Monitoring

Clinical Monitoring

RECOMMENDED CRITERIA
NO RECOMMENDED TOXICITY RATINGS

SUGGESTED CRITERIA
• Periodic liver function tests [serum alkaline phosphatase, GGT, ALT, AST & Bilirubin levels (serum proteins may be added if indicated)]

Significant Interactions

Alcohol, diazepam, lidocaine, phenytoin, propranolol, theophylline, warfarin.

Product Information

Commercial Product Description

Tablets with 50mg, 100mg Nilutamide.

Handling Risk Level

Pregnancy CPOSSIBLE HAZARDOUS DRUG
FDA Pregnancy Risk Factor C

  • Consider handling this drug using precuations outlined in CCNS Policies for Occupational Safety, Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy

Note

HANDLING RISK LEVEL:

HAZARD RISK LEVEL 3
FDA Pregnancy Risk Factor C
• Consider handling this drug using precautions outlined in CCNS Policies for Preparing Cancer Chemotherapy and Administering Cancer Chemotherapy  and the CCNS Standard for Oral Systemic Therapy for Cancer
• Go to "Additional Information" tab (above) for links to CCNS Policies

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Community Level • Take Home Prescription • Go to "Additional Information" tab (above) for links to Provincial Formulary of Cancer Drugs • Pharmacare Formulary Status- Formulary



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