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.
