Absorption T max is 1 h. Oral bioavailability is 100%. Food does not affect the extent of absorption, but it can decrease C max 20% and delay T max 1.5 h. Steady state is achieved after 2 days of multiple, twice-daily dosing.
Distribution Kinetics are linear over dose range of 500 to 5,000 mg. Less than 10% is protein bound.
Metabolism Not extensively metabolized. Major metabolic pathway is the enzymatic hydrolysis of the acetamide group, which produces the carboxylic acid metabolite ucb L057.
Elimination Plasma t ½ is approximately 7 h. It is eliminated from the systemic circulation by renal excretion as unchanged drug, which represents 66% of dose.
Special Populations Renal Function Impairment Total body Cl decreases 40% in patients with CrCl 50 to 80 mL/min, 50% in patients with CrCl 30 to 50 mL/min, and 60% in patients with CrCl less than 30 mL/min. Dosage reduction is recommended.
Hepatic Function Impairment Severe (Child-Pugh class C) Total body Cl decreases 50%. No dosage adjustment is needed.
Elderly Total body Cl decreased 38%; t ½ was 2.5 h longer.
Children Cl was approximately 40% higher (children 6 to 12 yr of age).
Gender C max and AUC are 20% higher in women.
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