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QuickView for Ezetimibe (compound)


PubChem
Name: ezetimibe
PubChem Compound ID: 10573550
Molecular formula: C24H21F2NO3
Molecular weight: 409.425 g/mol
DrugBank
Identification
Name: ezetimibe
Name (isomeric): DB00973
Drug Type: small molecule
Brand: Ezetrol, Zetia, Ezedoc
Brand name mixture: Inegy(Simvastatin + Ezetimibe)
Category: Cholesterol Absorption Inhibitors, Anticholesteremic Agents
CAS number: 163222-33-1
Pharmacology
Indication: For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.
Pharmacology:
Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hyperchole...
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Mechanism of Action: Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
Protein binding: >90%
Biotransformation: Hepatic, intestinal wall
Route of elimination: Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation (a phase II reaction) with subsequent biliary and renal excretion. In humans, ezetimibe is rapidly metabolized to ezetimibe-glucuronide.
Half Life: 22 hours
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
CyclosporineCyclosporine may increase the therapeutic and adverse effects of ezetimibe.
CholestyramineCholestyramine may decrease the levels of ezetimibe.

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