In combination therapy with LHRH agonist analogues in treatment of metastatic
prostatic carcinoma. A study has shown that the addition of flutamide to
leuprolide therapy in patients with advanced prostatic cancer increased median
actuarial survival time to 34.9 months versus 27.9 months with leuprolide alone.
To achieve benefit to combination therapy, both drugs need to be started
Known hypersensitivity to flutamide
The U.S. Food and Drug Administration (FDA) currently recommends that
procedures for proper handling and disposal of antineoplastic agents be
considered. Animal data (based on using doses higher than recommended for
humans) produced testicular interstitial cell adenoma. Do not discontinue
therapy without physician's advice. May cause hepatic failure, which can be
fatal. Serum transaminases should be monitored at baseline and monthly for the
first four months of therapy, and periodically thereafter. These should also be
repeated at the first sign and symptom of liver dysfunction. Use of flutamide is
not recommended in patients with baseline elevation of transaminase levels (>
twice the upper limit of normal). Flutamide should be discontinued immediately
at any time if the patient develops jaundice or elevation in serum transaminase
levels (>2 times upper limit of normal).
Gastrointestinal: Nausea, vomiting, diarrhea
Endocrine & metabolic: Loss of libido, hot flashes
1% to 10%:
Endocrine & metabolic: Gynecomastia
Neuromuscular & skeletal: Numbness in extremities
<1%: Hepatic failure, jaundice, flu-like syndrome, abdominal pain,
hypertension, edema, drowsiness, nervousness, confusion, hepatitis
Symptoms of overdose include hypoactivity, ataxia, anorexia, vomiting, slow
Management is supportive, dialysis not of benefit; induce vomiting
CYP3A3/4 enzyme substrate
Store at room temperature
Nonsteroidal antiandrogen that inhibits androgen uptake or inhibits binding
of androgen in target tissues
Absorption: Rapid and complete
Metabolism: Extensively to more than 10 metabolites
Half-life: 5-6 hours
Elimination: All metabolites excreted primarily in urine
Adults: Oral: 2 capsules every 8 hours for a total daily dose of 750
Serum transaminase levels should be measured prior to starting treatment and
should be repeated monthly for the first 4 months of therapy, and periodically
thereafter. LFTs should be checked at the first sign or symptom of liver
dysfunction (eg, nausea, vomiting, abdominal pain, fatigue, anorexia, flu-like
symptoms, hyperbilirubinuria, jaundice, or right upper quadrant tenderness).
Other parameters include tumor reduction, testosterone/estrogen, and phosphatase
|Mental Health: Effects
on Mental Status|
May rarely cause nervousness or confusion
Effects on Psychiatric
|Dental Health: Local
No information available to require special precautions
Effects on Dental Treatment|
No effects or complications reported
Take as directed; do not discontinue without consulting prescriber. You may
experience decreased libido, impotence, swelling of breasts, or decreased
appetite (small frequent meals may help). Report chest pain or palpitation;
acute abdominal pain; pain, tingling, or numbness of extremities; swelling of
extremities or unusual weight gain; difficulty breathing; or other persistent
adverse effects. Pregnancy precautions: This drug will cause fetal
abnormalities - use barrier contraceptives.
Capsule: 125 mg
Brogden RN and Chrisp P,
"Flutamide. A Reivew of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Use in Advanced Prostatic Cancer,"
Drugs Aging, 1991, 1(2):104-15.
Brogden RN and Clissold SP,
"Flutamide. A Preliminary Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Efficacy in Advanced Prostate Cancer,"
Drugs, 1989, 38(2):185-203.
Crawford ED, Eisenberger MA, McLeod DG, et al,
"A Controlled Trial of Leuprolide With and Without Flutamide in Prostatic Carcinoma,"
N Engl J Med, 1989, 321(7):419-24.
Delaere KP and Van Thillo EL,
"Flutamide Monotherapy as Primary Treatment in Advanced Prostatic Carcinoma,"
Semin Oncol, 1991, 18(5 Suppl 6):13-8.
Goldspiel BR and Kohler DR,
"Flutamide: An Antiandrogen for Advanced Prostate Cancer," DICP Ann
Pharmacother, 1990, 24(6):616-23.
Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure.
"The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding,"
January 12, 1987.
"Mechanism of Action and Pure Antiandrogenic Properties of Flutamide,"
Cancer, 1993, 72(12 Suppl):3816-27.
Moller S, Iversen P, and Franzmann MB, "Flutamide-Induced Liver Failure,"
J Hepatol, 1990, 10(3):346-9.
Schott AM, Vial T, Gozzo I, et al, "Flutamide-Induced Methemoglobinemia,"
DICP, 1991, 25(4):600-1.
Yagoda A, "Flutamide-Induced Diarrhea Secondary to Lactose Intolerance," J
Natl Cancer Inst, 1989, 81(23):1839-40.
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