Treatment of advanced prostate cancer in combination with a luteinizing hormone releasing hormone (LHRH) analogue or surgical castration.
Composition:
1 tabl powl. contains 50 mg of Bicalutamide (and 56 mg of lactose).
Action:
A non-steroidal antiandrogen lacking other endocrine activity. It binds to the wild type or normal androgen receptor, without causing gene expression; in this way, it inhibits androgen stimulation. The result of this inhibition is regression of the prostate tumor. The preparation is a racemic mixture, the antiandrogen activity shows almost exclusively the (R) -enantiomer. After oral administration, bicalutamide is well absorbed from the gastrointestinal tract (food does not affect the bioavailability of the drug). (S) -enantiomer is rapidly excreted compared to the (R) -enantiomer of which T0,5 is about 1 week. Bicalutamide is strongly bound to plasma proteins: the racemic mixture is 96%, and the (R) -enantiomer is more than 99.6%. The drug is extensively metabolised by oxidation and conjugation with glucuronic acid. Metabolites are excreted in the bile and urine of approximately equal proportions.
Contraindications:
Hypersensitivity to bicalutamide or to any of the excipients. The use of the drug is contraindicated in women, children and adolescents. Concomitant use with terfenadine, astemizole or cisapride.
Precautions:
Treatment should be started under the close supervision of a specialist. In patients with severe renal impairment (creatinine clearance <30 ml / min), bicalutamide should only be used with extreme caution. In patients with moderate or severe hepatic impairment, bicalutamide should be used with caution. During the use of the drug, periodic liver function tests should be considered. The occurrence of most changes is expected during the first 6 months of treatment. If the changes are severe, bicalutamide should be discontinued. In male patients treated with agonists with LHRH, reduced Glucose tolerance was observed. This can manifest as diabetes or loss of glycemic control in people with pre-existing diabetes. Therefore, monitoring of blood glucose in patients receiving bicalutamide in combination with LHRH agonists should be considered. During treatment with Bicalutamide, drugs primarily metabolised by CYP3A4 should be used with extreme caution. 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 drug is contraindicated in female patients and must not be administered to pregnant women or women during breastfeeding.
Side effects:
Very common: anemia, dizziness, flushing, abdominal pain, constipation, nausea, hematuria, gynecomastia and breast tenderness, weakness, swelling. Common: decreased appetite, decreased sex drive, depression, drowsiness, myocardial infarction (fatal cases), heart failure, indigestion, flatulence, hepatotoxicity, jaundice, hypertransaminasia, alopecia, hair growth and / or hair regrowth, dry skin, pruritus, rash, impotence, pain in the chest, weight gain. Uncommon: hypersensitivity reactions (including angioneurotic edema and urticaria), interstitial lung disease (deaths have been reported). Rare: liver failure (deaths have been reported).
Dosage:
Adults, including elderly patients: 1 tablet once a day. Treatment should be started at least 3 days before the start of LHRH analogue or concurrent with surgical castration. No dose adjustment is necessary in patients with impaired renal function and in patients with mild hepatic impairment. There is no experience in patients with severe renal impairment (creatinine clearance <30 ml / min). In patients with moderate or severe hepatic impairment, increased accumulation may occur.
(C)
