Absorption
Rapidly and completely absorbed from GI tract. T max is 1 h (single and multiple doses). Absolute bioavailability is 56%. Mean C max is decreased 20%; AUC is decreased 12.4% by food.
Distribution
Vd is 31 L (IV). Protein binding and binding to human albumin is greater than 98%.
Metabolism
Completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid. CYP-450 enzymes, mainly CYP3A4, are involved in N?dealkylation to oxidized dicarboxylic acid (M2), then to the aromatic amine (M1), and acyl glucuronide (M7) (inactive metabolites).
Excretion
Completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid. CYP-450 enzymes, mainly CYP3A4, are involved in N?dealkylation to oxidized dicarboxylic acid (M2), then to the aromatic amine (M1), and acyl glucuronide (M7) (inactive metabolites).
Special Populations
Renal Insufficiency
AUC and C max increased in severe renal function impairment.
Hepatic Impairment
Higher and more prolonged serum concentrations in patients with moderate to severe hepatic function impairment.
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Tags: Conditions & Treatments, Medications, Prandin (Repaglinide), Type 2 Diabetes