Ezetimibe Pharmacokinetics

Within 4–12 hours of the articulate administering of a 10-mg dosage to abnegation adults, the accomplished beggarly ezetimibe aiguille claret assimilation (Cmax) was 3.4–5.5 ng/ml. Following articulate administration, ezetimibe is captivated and abundantly conjugated to a phenolic glucuronide (active metabolite). Beggarly Cmax (45–71 ng/ml) of ezetimibe-glucuronide is accomplished aural 1–2 h. The accessory administering of aliment (high-fat vs. nonfat meals) has no aftereffect on the admeasurement of assimilation of ezetimibe. However, coadministration with a high-fat meal increases the Cmax of ezetimibe by 38%. The complete bioavailability cannot be determined, back ezetimibe is baffling in aqueous media acceptable for injection. Ezetimibe and its alive metabolite are awful apprenticed to animal claret proteins (90%).

Ezetimibe is primarily metabolized in the alarmist and the baby civil via glucuronide alliance with consecutive renal and biliary excretion. Both the ancestor admixture and its alive metabolite are alone from claret with a half-life about 22 hours, acceptance for once-daily dosing. Ezetimibe lacks cogent inhibitor or inducer furnishings on cytochrome P-450 isoenzymes, which explains its bound amount of biologic interactions. No dosage acclimation is bare in patients with renal dearth or balmy hepatic dysfunction (Child-Pugh account 5–6). Due to bereft data, the architect does not acclaim ezetimibe for patients with abstinent to astringent hepatic crime (Child-Pugh account 7–15). In patients with mild, moderate, or astringent hepatic impairment, the beggarly AUC ethics for absolute ezetimibe are added about 1.7-fold, 3– to 4-fold, and 5– to 6-fold, respectively, compared to advantageous subjects.