Sign Out
Pharmacology: Pharmacodynamics: Bicalutamide is a nonsteroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen.
Pharmacokinetics: Absorption: Rapid and complete; unaffected by food.
Protein binding: 96%.
Metabolism: Extensively hepatic; glucuronidation and oxidation of the R (active) enantiomer to inactive metabolites; the S enantiomer is inactive.
Half-life elimination: Active enantiomer: ~6 days, ~10 days in severe liver disease.
Time to peak, plasma: Active enantiomer: ~31 hours.
Excretion: Urine (36%, as inactive metabolites); feces (42%, as unchanged drug and inactive metabolites).
Continue with Google