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Absorption
T max is 3 to 4 h and bioavailability is 64% for 10 mg oral tablet. T max is 2 to 2.5 h and bioavailability is 73% (63% if taken with food) for 5 mg chewable tablet. T max is 2 h for 4 mg chewable tablet. The 4 mg granule formulation is bioequivalent to the 4 mg chewable tablet when administered in fasted state. Administration of granules with high-fat meal does not affect AUC but prolongs T max to 6.4 h.
Distribution
Protein binding more than 99%. Vd is 8 to 11 L/kg.
Metabolism
Extensively metabolized; plasma concentrations of metabolites are undetectable at steady state. CYP-450 3A4 and 2C9 are involved in metabolism.
Elimination
Plasma Cl averages 45 mL/min and mean plasma t ½ is 2.7 to 5.5 h; 86% recovered in feces and less than 0.2% in urine.
Special Populations
Hepatic Function Impairment
AUC increased 41% and t ½ was prolonged to 7.4 h in patients with mild to moderate hepatic function impairment.
Elderly
Plasma t ½ is slightly longer.
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