Each Film-Coated Tablet contains Bicalutamide 50 mg.
Pharmacology: Pharmacokinetics: Bicalutamide is well absorbed after oral doses. It undergoes extensive metabolism in the liver, the active R-enantiomer mainly by oxidation, the inactive S-enantiomer mainly by glucuronidation. It is excreted as metabolites in urine and feces. The half-life of the R-enantiomer is about 6 to 7 days, and may be prolonged still further in severe hepatic impairment. The S-enantiomer is cleared more rapidly. Bicalutamide is about 96% bound to plasma proteins.
It is indicated for use in combination therapy with luteinizing hormone-releasing hormone (LHRH) analog for the treatment of Stage D2 metastatic carcinoma of the prostate.
Bicalutamide (Bicatero 50) is not approved for use alone or with other treatment.
The usual dose of Bicalutamide when used with gonadorelin analogue in the palliative treatment of advances prostatic cancer, is 50 mg daily. The treatment is started at least 3 days before the gonadorelin analogue to suppress the flare reaction. A similar dose is used with surgical castration, starting on the same day as surgery.
It has been used as monotherapy in localised disease, but there is some evidence to suggest that in men without high risk of disease progression who would otherwise be managed with watchful waiting, the immediate use of Bicalutamide may increase the risk of death.
Bicalutamide inhibits various cytochrome P450 isoenzymes, particularly CYP3A4, in vitro, and licensed product information recommends that Terfenadine, Astemizole, and Cisapride should not be given with Bicalutamide, and that other drugs with narrow therapeutic index that are metabolised by cytochrome P450 isoenzymes should be used with caution. In vitro studies have shown that Bicalutamide can displace Warfarin from its protein binding sites.
Initiation of treatment should be under the direct supervision of a specialist. Bicalutamide is extensively metabolised in the liver. Data suggests that its elimination may be slower in subjects with severe hepatic impairment and this could lead to increased accumulation of Bicalutamide. Therefore, Bicalutamide should be used with caution in patients with moderate to severe hepatic impairment. Periodic liver function testing should be considered due to the possibility of hepatic changes. The majority of changes are expected to occur within the first 6 months of Bicalutamide therapy. Severe hepatic changes and hepatic failure have been observed rarely with Bicalutamide, and fatal outcomes have been reported (see Adverse Reactions). Bicalutamide therapy should be discontinued if changes are severe. A reduction in glucose tolerance has been observed in males receiving LHRH agonists. This may manifest as diabetes or loss of glycaemic control in those with pre-existing diabetes. Consideration should therefore be given to monitoring blood glucose in patients receiving Bicalutamide in combination with LHRH agonists. Bicalutamide has been shown to inhibit cytochrome P450 (CYP 3A4), as such caution should be exercised when co-administered with drugs metabolised predominantly by CYP 3A4 (see Contraindications). Cases of death or hospitalization due to severe liver injury (hepatic failure) have been reported in association with the use of bicalutamide.
Use in Special Population: Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Pruritus, asthenia, alopecia, hair regrowth, and dry skin occurs commonly with Bicalutamide. Hypersensitivity reactions, including angioedema and urticaria, have been reported infrequently. Cardiovascular effects including angina, heart failure, arrhythmias, and ECG changes have been reported rarely. Intestinal pneumonitis and pulmonary fibrosis have also been reported rarely. There is some evidence that Bicalutamide is associated with an incidence of diarrhea. Gynecomastia and breast pain are frequent adverse effects of nonsteroidal anti-androgens used to treat prostate cancer. Nearly 90% of patients treated with Bicalutamide in the Early Prostate cancer programme experienced breast pain, gynecomastia, or both. Some patient who develop gynecomastia will accept it as tolerable adverse effect of therapy but others will require specific treatment, and a number of different measures have been tried for both prevention and treatment. The risk of breast changes can be reduced by the use of prophylactic low-dose irradiation of breast area before Bicalutamide therapy is started.
However, skin irritation can occur, and the long-term risk for development of breast cancer is unknown. Irradiation is unlikely to be effective once breast enlargement has occurred but it can help to reduce pain. Empirical use of oral analgesics or topical local anesthetics may be considered for breast pain.
Store at temperatures not exceeding 30°C.
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
Bicatero 50 FC tab 50 mg