Table. powl. 50 mg: treatment of advanced stage prostate cancer in combination with luteinising hormone releasing hormone (LHRH) analog therapy or surgical castration.Table. powl. 150 mg: monotherapy or adjuvant therapy for radical prostatectomy or radiotherapy in patients with locally advanced prostate cancer, in the high risk of disease progression.
Composition:
1 tabl powl. contains 50 mg or 150 mg of bicalutamide.
Action:
A non-steroidal antiandrogen lacking other endocrine activity. It binds to androgen receptors 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 (no significant effect of food on the bioavailability of the drug has been demonstrated). The S enantiomer is excreted rapidly, in contrast 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.
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:
Especially cautiously use in patients with moderate or severe hepatic impairment (it has been proven that severe hepatic failure causes a slower elimination of bicalutamide). Use with caution in patients with severe renal impairment (creatinine clearance <30 ml / min). In the case of severe hepatic dysfunction, treatment should be discontinued. In patients with progression of disease and increased PSA levels, discontinuation of bicalutamide therapy should be considered. 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. It is not recommended for use in children and adolescents.
Pregnancy and lactation:
Not applicable. The preparation is not used in women.
Side effects:
Very common: sudden hot flushes, gynecomastia, tenderness of the breast glands, decreased libido, erectile dysfunction, impotence. Common: asthenia, pruritus, diarrhea, nausea, increased transaminases, hyperbilirubinemia, cholestasis, jaundice, hepatomegaly, edema, generalized pain, pelvic pain, chills, rash, hyperhidrosis, hirsutism, constipation, dizziness, insomnia, increased body weight, diabetes, anemia. Uncommon: interstitial lung disease, hematuria, hypersensitivity reactions including angioneurotic edema and urticaria, depression, abdominal pain, chest pain, headache, back pain, neck pain, hair loss, dry mouth, dyspepsia, flatulence , drowsiness, anorexia, hyperglycemia, weight loss, frequent urination at night, shortness of breath. Rare: dry skin, vomiting. Very rare: hepatic failure (causal relationship not established), thrombocytopenia, heart failure, angina pectoris, cardiac conduction disorders, including prolongation of PR and QT intervals, arrhythmias and non-specific ECG changes. In some patients, after the end of bicalutamide treatment, antiandrogen withdrawal syndrome may occur.
Dosage:
Orally. Adult men, including the elderly.Table. powl. 50 mg: 1 tabl. once a day. Treatment with bicalutamide should be started at least 3 days before treatment with the LHRH analogue or concurrently with surgical castration.Table. powl. 150 mg: 1 tabl. once a day.Treatment should be continued for at least 2 years or until disease progression. No dose adjustment is required in patients with impaired renal function or mild hepatic impairment. The tablets should be swallowed whole, with or without food, with liquid.
(C)
