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Following oral administration of 14 C-ezetimibe20 mgto human subjectstotal ezetimibeezetimibeezetimibe-glucuronideaccounted for approximately 93of the total radioactivity in plasmaAfter 48 hoursthere were no detectable levels of radioactivity in the plasma.
ZETIA reduces total-CLDL-CApo Bnon-HDL-Cand TGand increases HDL-C in patients with hyperlipidemiaMaximal to near maximal response is generally achieved within 2 weeks and maintained during chronic therapy.
Ezetimibewhich is water insolubleis absorbed and extensively conjugated to an active phenolic glucuronideezetimibeglucuronideafter oral intakeAfter a single dosemean ezetimibe peak plasma concentrationsC maxof 3.4 to 5.5 ngmL were obtained within 4 to 12 hoursT maxThe extent of ezetimibe absorption is not affected by taking it with high-fat or nonfat mealsHoweverthe C max value of ezetimibe is increased by 38when taken with a high-fat mealOverallezetimibe may be taken with or without food3
ZETIAadministered in combination with a 3-hydroxy-3-methylglutaryl-coenzyme AHMG-CoAreductase inhibitorstatinis indicated as adjunctive therapy to diet for the reduction of elevated totalCLDL-CApo Band non-HDL-C in patients with primaryheterozygous familial and non-familialhyperlipidemia.
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