Teva Pharma


Full Prescribing Info
Each film-coated tablet contains bicalutamide 50 mg.
Excipients/Inactive Ingredients: Tablet core: Microcrystalline cellulose, Povidone, Croscarmellose sodium, Sodium laurilsulfate, Lactose monohydrate, Colloidal silica anhydrous, Magnesium stearate.
Coating: Hypromellose, Polydextrose, Titanium dioxide, Macrogol 4000.
Pharmacology: Pharmacodynamics: Bicalutamide is a non-steroidal antiandrogen without any other endocrine activity. It binds to androgen receptors without activating gene expression and thus inhibits androgen stimulation. Inhibition results in the regression of prostatic tumours. Treatment discontinuation may result in antiandrogen withdrawal syndrome in some patients. Bicalutamide is a racemate, the (R)-enantiomer of which has most of the antiandrogen activity.
Pharmacokinetics: Bicalutamide is well-absorbed after oral administration. Food has not proved to affect significantly the extent bioavailability of bicalutamide. The (S)-enantiomer is rapidly cleared in comparison with the (R)-enantiomer. The plasmatic elimination half-life is approximately one week. After regular daily administration, the plasmatic concentration of the (R)-enantiomer when compared to the (S)-enantiomer is approximately 10 times higher due to its long elimination half-life.
After a daily dose of 50 mg, the plateau plasmatic concentrations of the (R)-enantiomer reach approximately 9 μg/ml. Of the total amount of plasmatic plateau enantiomers, 99% of the (R)-enantiomer is responsible for the therapeutic action.
Age, renal impairment or mild to moderate hepatic impairment do not affect the pharmacokinetics of (R)-enantiomer. It was demonstrated that plasmatic elimination of the (R)-enantiomer is slower in patients with severe hepatic impairment.
Bicalutamide is highly protein bound (racemate 96%, (R)-enantiomer more than 99%) and extensively metabolised (via oxidation and glucoronidation): the metabolites are excreted equally via kidneys and bile.
Treatment of advanced prostatic carcinoma in combination with luteinizing hormone releasing hormone (LHRH) analogues or surgical castration.
Dosage/Direction for Use
Adult men including elderly patients: One tablet once daily at the same time each day (usually in the morning or in the evening).
The treatment should be started concomitantly with an LHRH analogue or surgical castration.
Renal impairment: No adjustment of the dose is needed in patients with impaired renal function.
Hepatic impairment: No adjustment of the dose is needed in patients with mild impairment of hepatic function. Patients with moderate to severe hepatic impairment may experience increased accumulation of the substance.
Children and adolescents: There is no relevant indication for the use of bicalutamide in children or adolescents.
There is no experience with overdose in humans. A specific antidote for overdose is not known and treatment should be symptomatic. Haemodialysis does not have an effect. General supportive treatment including frequent monitoring of vital functions is indicated.
Hypersensitivity to bicalutamide or to any of the excipients.
Females and children.
Pregnancy and lactation.
Special Precautions
Bicalutamide is extensively metabolised in the liver. Available data suggest that the elimination may be slower in patients with severe hepatic impairment, which may lead to increased accumulation of the substance. Therefore, caution is needed if bicalutamide is administered to patients with moderate hepatic impairment.
Monitoring of hepatic function is recommended because of potential hepatic changes. The majority of such cases occur within 4 months from the beginning of treatment.
Severe hepatic changes have been observed rarely; in such cases the treatment with bicalutamide must be discontinued.
Bicalutamide is an inhibitor of cytochrome P450 (CYP) 3A4. Caution is recommended in patients with concomitantly using substances that are metabolised predominantly by CYP 3A4.
This product contains 35 mg lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.
Use In Pregnancy & Lactation
Bicalutamide is not indicated in women; therefore it must not be administered either in pregnancy, or in lactation.
Adverse Reactions
Adverse reaction percentages reported as part of combination regimen with an LHRH analogue.
>10%: Hot flashes, pain, back pain, constipation, weakness, pelvic pain, infection, nausea, peripheral edema, dyspnea, diarrhea, nocturia, hematuria, abdominal pain, anemia.
≥2% to 10%: Dizziness, rash, gynecomastia, urinary tract infection, bone pain, paresthesia, cough, pharyngitis, chest pain, insomnia, hepatic changes, dyspepsia, impotence, weight loss, myasthenia, Flu syndrome, headache, sweating, vomiting, flatulence, anorexia, breast pain, polyuria, hyperglycemia, bronchitis, anxiety, urinary retention, urinary impairment, weight gain, arthritis, depression, urinary incontinence, pathological fracture, pneumonia, rhinitis.
Drug Interactions
No pharmacodynamic or pharmacokinetic interactions have been demonstrated between bicalutamide and LHRH analogues.
In vitro studies suggest that R-bicalutamide acts as a CYP 3A4 inhibitor and has a weaker inhibitory effect on CYP 2C9, 2C19, and 2D6 activities.
Although clinical studies using antipyrine as a marker of CYP activity showed no evidence of an interaction potential with bicalutamide, mean midazolam exposure (AUC) was increased up to 80%, after co-administration of bicalutamide for 28 days. For substances with a narow therapeutic index, such an increase could be relevance.
Therefore, the concomitant administration of terfenadine, astemizole or cisapride is contraindicated and caution is required when concomitantly prescribing ciclosporin and calcium channel blockers. Dosage reduction may be required for these products, particularly if there is evidence of enhanced or adverse effect. For ciclosporin, it is recommended that plasmatic levels and clinical condition should be frequently and regularly monitored at the beginning and after stopping the administration of bicalutamide.
Caution is required during concomitant administration of substances that might inhibit oxidation of bicalutamide, i.e, medicinal products containing ketoconazole or cimetidine. This may be increase the plasmatic levels of bicalutamide and subsequently the adverse effects.
Studies in vitro suggest that bicalutamide can displace the coumarin anticoagulant warfarin from protein binding sites. Therefore, frequent and monitoring of prothrombin time is recommended after starting the administration of bicalutamide to patients who concomitantly use coumarin anticoagulants.
Store below 30°C. Store in the original package. Protect from moisture.
ATC Classification
L02BB03 - bicalutamide ; Belongs to the class of anti-androgens. Used in treatment of neoplastic diseases.
FC tab 50 mg (white to off-white biconvex, debossed with "93" on one side and "220" on the other) x 28's.
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