Suction
After oral administration, it is quickly and completely absorbed from the digestive tract. Simultaneous food intake does not affect absorption.
Distribution
With a daily intake of bicalutamide in a dose of 50 mg Css (R) -enantiomer in plasma is about 9 μg / ml. At an equilibrium state, about 99% of all enantiomers circulating in the blood form the active (R) -enantiomer.
With a daily intake of the drug, the concentration of the (R) enantiomer in the plasma increases approximately 10-fold due to the long half-life, which allows you to take the drug 1 time per day.
The association with plasma proteins is high (for a racemic mixture of 96%, for the (R) -enantiomer 99.6%).
Metabolism
Intensively metabolized in the liver by oxidation and the formation of conjugates with glucuronic acid.
Excretion
Metabolites are excreted in urine and bile approximately in equal proportions.
(S) -enantiomer is eliminated from the body much faster (R) -enantiomer, the half-life of the latter is about 7 days.
Pharmacokinetics in special clinical cases
The pharmacokinetics of the (R) -enantiomer are not affected by age, renal dysfunction, mild or moderate hepatic impairment.
There is evidence that in patients with severe impairment of liver function, the elimination of the (R) enantiomer from the plasma is slowed.
In patients with moderate and severe violations of liver function, cumulation of bicalutamide in the body can be observed.