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.