Treatment of advanced prostate cancer in combination with LHRH analogues or surgical castration.
Composition:
1 tabl powl. contains 50 mg of bicalutamide.
Action:
A non-steroidal antiandrogen lacking other endocrine activity. It binds to the androgen receptor without causing gene expression, which inhibits androgen stimulation. The result of this inhibition is regression of the prostate tumor. The preparation is a racemic mixture, the antiandrogen activity is almost exclusively the R enantiomer. After oral administration, Bicalutamide is well absorbed from the gastrointestinal tract (simultaneous food intake does not affect the bioavailability of the drug). The S enantiomer is rapidly excreted in comparison to the R enantiomer whose half-life is about 1 week. Bicalutamide is strongly bound to plasma proteins: the racemic mixture at 96% and the R enantiomer at over 99%. The drug is primarily metabolised in the liver by oxidation and conjugation with glucuronic acid. Metabolites are excreted in the bile and in the urine in equal proportions.
Contraindications:
Hypersensitivity to bicalutamide or to any of the excipients. Use with terfenadine, astemizole or cisapride. Women and children.
Precautions:
Particularly caution should be used in patients with moderate or severe hepatic impairment (severe hepatic insufficiency has been shown to result in slower elimination of the R-enantiomer) and when co-administered with medicinal products metabolised by the CYP3A4 isoenzyme. The product contains lactose and should not be used in patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of the preparation in women is contraindicated. Do not use the drug in pregnant women and during breast-feeding.
Side effects:
Very common: gynecomastia, increased tension of the mammary glands, hot flushes. Common: nausea, diarrhea, pruritus, fatigue, increase in liver enzymes, cholestasis in the bile ducts, jaundice. Uncommon: interstitial lung disease, hypersensitivity reactions including angioneurotic edema, urticaria. Rare: thrombocytopenia, angina pectoris, heart failure, heart conduction, vomiting, dry skin. Very rare: liver failure.
Dosage:
Orally. Adults men: 1 tabl. once a day at the same time; treatment with the preparation should be initiated simultaneously with the use of LHRH analogues or simultaneously with surgical castration. No dose adjustment is required in elderly patients; patients with impaired renal function; patients with mild hepatic impairment (patients with moderate or severe hepatic impairment may accumulate).
(C)
