Treatment of advanced prostate cancer in combination with luteinizing hormone releasing hormone (LHRH) analogues or surgical castration.
Composition:
1 tabl powl. contains 50 mg of bicalutamide. The preparation contains lactose.
Action:
A non-steroidal antiandrogen lacking other endocrine activity. It binds to the androgen receptor, blocking the activation of gene expression and in this way inhibits androgen stimulation. The result of this inhibition is the reduction of prostate cancer. 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 (food does not affect the bioavailability of the drug). The S-enantiomer is rapidly excreted compared to the R-enantiomer of which T0,5 is about 1 week. For regular once daily dosing, the blood concentration of the R enantiomer is about 10 times higher than that of the S-enantiomer. Bicalutamide binds strongly 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. Age, renal failure and mild to moderate hepatic failure do not change the pharmacokinetics of the drug. In patients with severe hepatic impairment, the R enantiomer is more slowly eliminated.
Contraindications:
Hypersensitivity to bicalutamide or any of the excipients. Bicalutamide is contraindicated in women and children. Concomitant use of terfenadine, astemizole and cisapride.
Precautions:
Caution should be used in patients with moderate or severe hepatic impairment (risk of slower metabolism of the drug); with a history of diabetes mellitus in combination with LHRH (risk of loss of glycemic control and onset of diabetes); in the case of combination therapy with drugs that are mainly metabolised by CYP3A4. Bicalutamide should be discontinued in the event of severe hepatic impairment during therapy. Due to the lactose content, do not use in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation is contraindicated for use in women.
Side effects:
Very common: dizziness, hot flushes, abdominal pain, constipation, nausea, hematuria, gynecomastia, breast tenderness, asthenia, chest pain, swelling. Common: anemia, anorexia, decreased libido, depression, drowsiness, indigestion, bloating, changes in liver parameters (including transaminase elevations and jaundice), alopecia, hirsutism, dry skin, pruritus, rash, impotence, weight gain. Uncommon: hypersensitivity reactions (including angioneurotic edema and urticaria), interstitial lung disease. Rare: liver failure. In addition, cardiac failure was observed in clinical trials in patients receiving bicalutamide in combination with the LHRH analogue; however, there is no evidence of a causal relationship to treatment.
Dosage:
Orally. Adults, including elderly patients: 1 tabl. once a day at the same time each day (usually in the morning or evening). Treatment should be started within 1 week before administration of the luteinizing hormone releasing hormone analogue (LHRH) or concurrently with surgical castration. No dosage adjustment is necessary for patients with impaired renal function or for patients with mild hepatic impairment. Patients with moderate or severe hepatic impairment may accumulate bicalutamide.
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