The drug is completely and rapidly absorbed after oral administration, subjected to biotransformation in the liver. The main metabolite, found in plasma, the maximum concentration is achieved after 2 hours a biologically active α-hydroxylated derivative (2-oksiflutamid). 94-96% of flutamide and 92-94% α-hydroxylated metabolite binds to proteins. Because the body the drug is derived mainly winstrol steroid kidneys, about 4.2% is excreted in the feces within 72 hours. The half-life of the active metabolite in the plasma is about 6 hours (in elderly patients – 8 hours after a single dose and 9.6 hours at a stable concentration). Following multiple oral administration of 250 mg of flutamide 3 times per day stable level concentrations of drug and active metabolite in the plasma is reached after the fourth dose of flutamide.
Treatment of metastatic prostate cancer, when shown the suppression of testosterone action:
• at the beginning of treatment in combination agonists;
• as an additional treatment in patients already receiving therapy with agonists;
• patients with surgical castration;
• the treatment of patients who have other types of hormone therapy were ineffective or intolerance to such therapy.
– Hypersensitivity to flutamide or any other component of the drug.
– Severe hepatic impairment.
– Children’s age (safety and efficacy not established).
With cautious: in patients with impaired liver function, with a tendency to thrombosis and cardiovascular diseases, as well as in conditions predisposing to aniline toxicity (one of the metabolites of flutamide – metilanilinovoe derivative): deficiency of winstrol steroid dehydrogenase, smoking, haemoglobinopathies (M-hemoglobin).
Dosing and Administration
Inside of 250 mg three times a day, every 8 hours. In the case of achieving the positive effect of the drug is used to signs of tumor progression of the disease.
In the case of co-therapy agonists, both drugs may be administered simultaneously or receiving flutamide Pliva begin three days before the first agonist.
The incidence of side effects is described according to the following gradation: the most frequently (10% or higher) is less frequent (1 to 10%), rare (less than 1%).
In applying the drug in monotherapy most often: gynecomastia and / or pain in the breast, sometimes accompanied by galactorrhea. These effects disappear after treatment discontinuation or dose reduction. Less frequently: diarrhea, nausea, vomiting, increased appetite, insomnia, fatigue, transient abnormal liver function, hepatitis. Rare: hepatitis or jaundice (including cholestatic), liver necrosis, hepatic encephalopathy, increased transaminase activity (these side effects are usually reversible upon discontinuation of therapy, however, there were reports of deaths due to severe hepatic failure in the treatment of flutamide); subcutaneous hemorrhage, herpes zoster, pruritus, lupus-like syndrome; anorexia, heartburn, constipation, dyspepsia; decreased libido, headache, “tides” (sensation of heat, excessive sweating), increased blood winstrol steroid pressure, dizziness, weakness, poor visual acuity, thirst, chest pain, edema (fingers, feet, legs), anxiety, depression and thrombocytopenia . Prolonged treatment observed suppression of spermatogenesis. We noted some cases of hemolytic anemia, macrocytic anemia, methemoglobinemia, photosensitivity reaction, increased (including erythema, skin ulceration, bullous rash, epidermal necrolysis). Sometimes patients have changes in urine color from amber to yellow-green.