Bicalutamide possibly enhances anticoagulant effect of coumarins

Nausea, vomiting,diarrheoa, asthnia, gynaecomastia, breast tenderness,

Hot flushes,pruritus, dry skin, alopecia Hirsurism, decreased libido,impotence,weight gain,

Less commonly, hypersensitivity reactiuons, including angioneurotic oedema and urticaria, Intestitial lung disease

Rarely abdominal pain, Cardiovascular disorders (including angina, heart failure and arrhythmias) Depression, dyspepsia, haematuria,cholestatis jaundice, thrombocytopenia

Hypersensitivity

Females

Children

Pregnancy Lactation

Indication-

Advanced prostrate cancer

Dosage-

When used with gonadorelin analoge - Usual dose 50mg once daily

May be started with or at least 3 days before starting gonadorelin analogue therapy

Safety 

Contraindication- Females.Children.Pregnacy ana lactation. Concomittant use of terfenamide.stemizole or cisapride

Special Precautions-

Patients with history of or risk factors for QT prolongation,heart failure,frequent electrolyte abnormalities,alcohol  abuse,,family history of risk factors for osteoporosis,diabetes, moderate to  severe hepatic impairment.

Patient councelling-

Avoid excessive exposure to sunlight or UV light and  utilise adequate sun protection(sun protection) eg. wear protective clothing, use of sunscreen)

Monitor- LFT at baseline and regularly  during the 1st and 4th month of therapy, then peridically therfater, CBC , electrolyte,ECG

Pharmacology-

Baculutamide is a racemic mixture it antandrogenic activity being almost exclusively exhibited by the r-enatomer and the B-enatiomer is essentially inactive.

The mode of action of the AAs results in theblockasde of the androgen receptors of the prostrate cells. Bicalutamide competes with androgen for the binding of the androgen receptors, consequently blocking the action of androgens and testicular origin which stimulates the growth of normal malignant tissue

Pharmacokinetics-

Bicalutamide is well absorbed following oral admin although the absolute bioavailability is unknown. The S-(inactive) isomer is metabolised primarily by glucoronidation. The R(active) isomer also undergoes glucuronidation but is predominantly oxidised to an inactive metabolite glucuronides by glucoronidation .

Both the partent and metabolite glucoronides are eliminated in the urine and feaces. The S-enantiomer is rapidly cleared relative to the R-enantiomer, with the R-enatiomer accounting for 99% of total steady -state plasma levels. It has a half-lfe of 5-9 days.

Take with or without food

Use contraindicated . Observe caution