Table. 50 mg: treatment of advanced prostate cancer in combination with LHRH analogues or surgical castration.Table. 150 mg: treatment of locally advanced prostate cancer as monotherapy or as adjuvant treatment after complete removal of the prostate gland or after radiotherapy in patients at high risk of disease progression.
Composition:
1 tabl powl. contains 50 mg or 150 mg of bicalutamide. The preparation contains lactose.
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 a reduction in the prostate tumor. Bicalutamide is a racemate whose antiandrogenic activity is almost exclusively associated with the R-enantiomer. After oral administration, bicalutamide is well absorbed from the gastrointestinal tract (food does not affect the bioavailability of the drug). The S-enantiomer is rapidly eliminated compared to the R-enantiomer of which T0,5 is about 1 week. After daily administration of Bicalutamide, the concentration of R-enantiomer accumulates in the plasma to about 10-fold greater result of its long T0,5. Bicalutamide binds strongly to proteins (96% racemate, R-enantiomer> 99%) and is extensively metabolised (by oxidation and conversion to glucuronides): bicalutamide metabolites are excreted by the kidneys and bile in almost equal proportions.
Contraindications:
Hypersensitivity to bicalutamide or other ingredients of the preparation. The use of the preparation is contraindicated in women, children and adolescents. The concomitant use of the preparation with terfenadine, astemizole or cisapride is contraindicated.
Precautions:
Use with caution in patients with moderate to severe hepatic impairment. Periodic liver function tests should be considered. Most changes are expected to occur in the first 6 months of drug administration. In the event of severe hepatic impairment, bicalutamide should be discontinued. In patients who have had disease progression with elevated PSA values, discontinuation of bicalutamide therapy should be considered. In men using LHRH analogs, a decrease in Glucose tolerance was observed, which may result in diabetes or loss of glycemic control in patients with previously diagnosed diabetes. Blood glucose control should be considered in patients taking bicalutamide in combination with LHRH analogues. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
The use of bicalutamide in women is contraindicated.
Side effects:
Table. powl. 50 mg. Very common: anemia, dizziness, hot flushes, abdominal pain, constipation, nausea, hematuria, gynecomastia and breast pain (may be reduced by simultaneous castration), asthenia, edema. Common: decreased appetite, decreased libido, depression, drowsiness, myocardial infarction (fatal cases have been reported), heart failure, indigestion, flatulence, hepatotoxicity, jaundice, hypertransaminasms, alopecia, hair growth or re-growth, rash, dry skin , pruritus, erectile dysfunction, chest pain, weight gain. Uncommon: hypersensitivity reactions, angioneurotic edema, urticaria, interstitial pneumonitis (deaths have been reported). Rare: liver failure (deaths have been reported).Table. powl. 150 mg. Very common: rash, gynecomastia and breast pain, asthenia. Common: anemia, decreased appetite, decreased libido, depression, dizziness, drowsiness, hot flushes, abdominal pain, constipation, nausea, indigestion, bloating, hepatotoxicity, jaundice, hypertransaminasms, alopecia, hair growth or re-growth of hair, dryness skin, pruritus, hematuria, erectile dysfunction, chest pain, edema, weight gain.Uncommon: hypersensitivity reactions, angioneurotic edema, urticaria, interstitial pneumonitis (deaths have been reported). Rare: liver failure (deaths have been reported).
Dosage:
Orally.Table. 50 mg. Adults, including elderly males: 1 tablet (50 mg) daily. Treatment with bicalutamide should be started at least 3 days before initiating therapy with the LHRH analogue or concurrently with surgical castration.Table. 150 mg. Adults, including elderly males: 1 tablet (150 mg) daily. Treatment with the product should be carried out continuously for at least 2 years or until the disease progresses. In patients with renal insufficiency and in patients with mild hepatic impairment no dose adjustment is necessary. In patients with moderate or severe hepatic impairment, bicalutamide may accumulate. Table. should be swallowed whole with water.
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