After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide (ezetimibe-glucuronide).
Atorvastatin
Maximum plasma atorvastatin concentrations after oral administration occur within 1 to 2 hours. Extent of absorption increases in proportion to atorvastatin dose. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. The low systemic availability is attributed to presystemic clearance in gastrointestinal mucosa and/or hepatic first-pass metabolism. Plasma atorvastatin concentrations are lower (approximately 30% for Cmax and AUC) following evening drug administration compared with morning. However, LDL-C reduction is the same regardless of the time of day of drug administration. Effect of Food on Oral Absorption
LIPTRUZET
A high-fat meal decreased atorvastatin AUC and Cmax 11% and 35%, respectively, of the LIPTRUZET 10/80 tablet. A high-fat meal decreased unconjugated ezetimibe AUC 2% and increased unconjugated ezetimibe Cmax 10% of the LIPTRUZET 10/80 tablet.
LIPTRUZET can be taken with or without food [see Dosage and Administration (2.1)].