Pharmacologic class: Antiandrogen
Therapeutic class: Antineoplastic
Pregnancy risk category D
Exerts potent antiandrogenic activity at cellular level by inhibiting androgen uptake or nuclear binding of androgen
Capsules: 125 mg
Indications and dosages
➣ Metastatic prostate cancer
Adults: 250 mg P.O. t.i.d. q 8 hours, given with luteinizing hormone-releasing hormone (LHRH) analog. Total daily dosage is 750 mg.
• Benign prostatic hypertrophy
• Hypersensitivity to drug
• Severe hepatic impairment
• Sleep apnea
• Be aware that leuprolide acetate is the most common LHRH analog given with flutamide.
CNS: drowsiness, confusion, depression, anxiety, nervousness, paresthesia
CV: peripheral edema, hypertension
GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia, dry mouth
GU: erectile dysfunction, loss of libido, gynecomastia, hot flashes
Hematologic: anemia, leukopenia, thrombocytopenia
Skin: rash, photosensitivity
Drug-drug. Warfarin: increased prothrombin time
Drug-diagnostic tests. Alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, blood urea nitrogen, creatine kinase: increased levels
Hemoglobin, platelets, white blood cells: decreased levels
Drug-herbs. Chaparral, comfrey, eucalyptus, germander, pennyroyal, skullcap, valerian: increased risk of hepatotoxicity
Drug-behaviors. Sun exposure: increased risk of photosensitivity
• Monitor CBC and liver function tests.
☞ Watch for bleeding tendency and signs and symptoms of hepatic damage (jaundice, vomiting, dark yellow or brown urine).
• Monitor blood pressure.
☞ Instruct patient to immediately report unusual bleeding or bruising.
• Tell patient to avoid activities that can cause injury. Advise him to use soft toothbrush and electric razor to avoid gum and skin injury.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Instruct patient to minimize GI upset by eating frequent, small servings of healthy food.
• Tell patient he'll undergo regular blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.