Bicalutamide

Bicalutamide

Class:Cytostatic

Mechanism of action

Bicalutamide binds competitively and reversibly to the androgen receptor of the prostate cell without  activating gene expression.It thus inhibits the simulatory effect of androgens and results in regression of prostatic tumour.

Pharmacokinetics

Absorption:rapid and complete.Protein binding:96 percent.Metabolism:extensive;stereospecific metabolism.Half life:up to 10 days.Elimination:not yet studied.

Indications

Treatment of advanced prostate cancer in combination with LHRH analogue therapy or surgical castration.

Contraindications

Bicalutamide is contraindicated in females and children.

Precautions

Bicalutamide is extensively metabolized in the liver.Data suggests that its elimination may be slower in subjects with severe hepatic impairment and this could lead to some accumulation of bicalutamide.Therefore,bicalutamide should be used with caution in patients with moderate to severe hepatic impairement.

Side effects

Hot flashes,angina pectoris,congestive heart failure,edema,anxiety,depression,confusion,somnolence,nervousness,fever,chills,dry skin,pruritis,alopecia,breast pain,diabetes mellitus,decreased libido,dehydration,gout,anorexia,dyspepsia,xerostomia,weight gain,urinary retention,cough increased,myalgia,pneumonia,diarrhea.

Pregnancy

Pregnancy risk factor X.

Drug interaction

There is no evidence of interaction between bicalutamide and LHRH analogues.

Dosage

Adult males including the elderly:one tablet(50mg) once a day.Treatment with bicalutamide should be started at the same time as the treatment with an LHRH analogue or castration.

Brands

Tabs.Casodex 50 mg.