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 wild type or normal type from 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 is 96% and the R enantiomer is 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. No dose adjustment is required in the elderly, in patients with impaired renal function or mild hepatic impairment.
Contraindications:
Hypersensitivity to bicalutamide or other ingredients of the preparation. The use of the preparation is contraindicated in women and children. The concomitant use of the preparation with terfenadine, astemizole or cisapride is contraindicated.
Precautions:
Caution should be used in patients with moderate or severe hepatic impairment (the results suggest slower metabolism of bicalutamide in patients with impaired hepatic function) and in patients with severe renal impairment (creatinine clearance <30 ml / min). 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:
Not applicable. The preparation is not used in women.
Side effects:
Very common: anemia, dizziness, hot flushes, abdominal pain, constipation, nausea, haematuria, gynecomastia and breast tenderness, weakness, edema. Common: decreased appetite, decreased sex drive, depression, myocardial infarction (fatalities were reported), heart failure, drowsiness, indigestion, bloating, hepatotoxicity, jaundice, hypertransaminasms, alopecia, hirsutism / hypertrichosis, dry skin, pruritus, rash, erectile dysfunction , chest pain, weight gain. Uncommon: hypersensitivity, angioneurotic edema, urticaria, interstitial lung disease (deaths have been reported). Rare: liver failure (deaths have been reported).
Dosage:
Orally. Adults men: 1 tabl. once a day at the same time; treatment with the preparation should be started at least 3 days before starting the use of LHRH analogues or concurrently with surgical castration.
(C)
