Treatment of advanced prostate cancer in combination with LHRH analogue therapy or surgical castration.
Composition:
1 tabl powl. contains 50 mg of bicalutamide. The tablets contain 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 the active substance or any of the excipients. Women and children. Concomitant use with terfenadine, astemizole or cisapride.
Precautions:
The initiation of treatment should be under the direct supervision of a specialist. The drug should be used with caution in patients with moderate and severe hepatic impairment. Periodic monitoring of liver function should be considered. In most cases, hepatic dysfunction may occur during the first 6 months of treatment with bicalutamide. In case of severe disorders, bicalutamide therapy should be discontinued. A reduction in Glucose tolerance was observed in patients treated with LHRH agonists. This may result in diabetes or reduced glycemic control in patients with pre-diabetes. Blood glucose monitoring should be considered in patients treated with bicalutamide with LHRH agonists. Exercise caution with the simultaneous use of bicalutamide with medicinal products metabolised specifically by CYP3A4. There is no experience in the use of bicalutamide in patients with severe renal impairment (creatinine clearance <30 ml / min). 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 preparation is contraindicated for use in women.
Orally. Adults, also elderly people: 50 mg once a day. Swallow the tablets whole with a drink. The use of bicalutamide should be started at least 3 days before initiating therapy with the LHRH analogue or concurrently with surgical castration. No dose adjustment is necessary in patients with impaired renal function and in patients with mild hepatic impairment.
(C)
