Ezetimibe

Ezetimibe

Basics

Ezetimibe belongs to the group of cholesterol absorption inhibitors and is a lipid-lowering agent used to lower blood cholesterol levels. It is mainly used as an add-on therapy for the treatment of primary hyperlipidemia and in familial hypercholesterolemia.

The discovery and research of ezetimibe began in the early 1990s after intravenous administration of ezetimibe to rats showed that the drug accumulates in the enterocytes of the intestinal villi. This finding prompted studies to investigate the effect of ezetimibe on intestinal cholesterol absorption.

Effect

Pharmacodynamics

The cholesterol-lowering effect in the blood is mainly prompted by ezetimibe selectively inhibiting the absorption of cholesterol and phytosterol by the small intestine, but without interfering with the absorption of fat-soluble vitamins and nutrients. Inhibition of transport of lipids into the blood is achieved through inhibited binding to the transport protein NPC1L1. As a result, the amount of circulating cholesterol in the blood is reduced.
Ezetimib senkt neben dem Gesamtcholesterin auch das LDL-Cholesterin, das Apo-B-Protein und Triglyzeride und kann eine Erhöhung des HDL-Cholesterins bewirken.

Pharmacokinetics

Ezetimibe is rapidly absorbed after oral administration and metabolized to its major active metabolite, ezetimibe glucoronide, and subsequently excreted via bile. The highest concentration of ezetimibe in blood plasma is reached after 4-12 hours, that of ezetimibe glucoronide after 1-2 hours, and circulates with approximately 99% (ezetimibe) and approximately 90% (ezetimibe glucoronide) bound to proteins. Elimination occurs in the feces and to a lesser extent in the urine.

Interactions

Interactions may occur with antacids, colestyramine, fibrates, and warfarin, among others.

Toxicity

Side effects

Adverse effects such as abdominal pain, diarrhea, flatulence, or fatigue may occur during treatment with ezetimibe.

Toxicological Data

LD50 (oral and intraperitoneal, rat): > 2000 mg/kg

Chemical & physical properties

ATC Code C10AX09
Formula C24H21F2NO3
Molar Mass (g·mol−1) 409,4252
Physical State solid
Melting Point (°C) 163
PKS Value 9,48
CAS Number 163222-33-1
PUB Number DB00973
Drugbank ID DB00973

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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