Bicalutamide information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancerand hirsutism.It was first launched in 1995 as a combination treatment (with surgical or medical castration) for advanced prostate cancer and subsequently launched as monotherapy for the treatment of earlier stages of the disease.
Pharmacodynamics
Pharmacokinetics
Absorption
Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown. Co-administration of Bicalutamide with food has no clinically significant effect on rate or extent of absorption.
Distribution
Bicalutamide is highly protein-bound (96%)
Metabolism/Elimination
Bicalutamide undergoes stereospecific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation. Both the parent and metabolite glucuronides are eliminated in the urine and feces. The S-enantiomer is rapidly cleared relative to the R-enantiomer, with the R-enantiomer accounting for about 99% of total steady-state plasma levels.
Bicalutamide Indications / Bicalutamide Uses
Information Not Available
Bicalutamide Adverse Reactions / Bicalutamide Side Effects
Nausea, vomiting, diarrhoea, asthenia, gynaecomastia, breat tenderness, hot flushes, pruritus, dry skin, alopecia, hirsutism, decreased libido, impotence, weight gain; less commonly hypersensitivity reactions including angioneurotic oedema & urticaria, intestinal lung disease; rarely abdominal pain, CV disorders ( including angina, heart failure7 arrhythmias) depression, dyspepsia, haematuria, cholestasis, jaundice, thrombocytopenia.
Precautions
Information Not Available
Special Precautions
Monitor liver function regularly in hepatically impaired patients on prolonged therapy. Monitoring serum levels of Prostrate Specific Antigen (PSA) may be useful in evaluating the patients's clinical progress.
Other Drug Interactions
Enhances effects of coumarin anticoagulants
Other Interactions
Information Not Available
Dosage
Oral
Palliative treatment of advanced prostatic cancer:
Adult- When use dwith gonoadrelin analogue.
Usual dose: 50 mg once daily. May be started with or atleast three days before starting with gonoadrelin analogue therapy.
Monotherapy or adjuvant therapy to surgery or radiotherapy in locally advanced prostatic cancer:
Adult- 150mg once daily.
Food(before/after)
Information Not Available
List of Contraindications
Bicalutamide and Pregnancy
Contraindicated in pregnancy
Bicalutamide and Lactation
Contraindicated in lactation
Bicalutamide and Children
Information Not Available
Bicalutamide and Geriatic
Information Not Available
Bicalutamide and Other Contraindications
Hypersensitivity
Bicalutamide is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the tablet’s components. Hypersensitivity reactions including angioneurotic edema and urticaria have been reported
Storage
Information Not Available
Lab interference
Information Not Available
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