Ezetimibe: a novel cholesterol absorption inhibitor

Ezetimibe (Zetia), an intestinal cholesterol absorption inhibitor, has a unique mechanism of action, distinct from those of statins and bile acid sequestrants. Ezetimibe, approved in late October, represents the first new class of cholesterol-lowering drugs in 15 years. When used as monotherapy, eze...

Full description

Saved in:
Bibliographic Details
Published inFormulary (Cleveland, Ohio) Vol. 37; no. 12; p. 628
Main Author Caron, Michael F
Format Journal Article
LanguageEnglish
Published North Olmsted Intellisphere, LLC 01.12.2002
MultiMedia Healthcare Inc
Subjects
Acids
Anticholesteremic agents
Bile
Bioavailability
Cardiovascular disease
Cholesterol
Clinical trials
Cytochrome
Dietary supplements
Drug dosages
Drug interactions
Evaluation
Headaches
High density lipoprotein
Hyperlipidemia
Kinases
Lipids
Lipoproteins
Oral administration
Pharmaceuticals
Pharmacokinetics
Product/service Evaluations
Proteins
Statins
Triglycerides
United States
Online AccessGet full text

Cover

More Information
Summary:Ezetimibe (Zetia), an intestinal cholesterol absorption inhibitor, has a unique mechanism of action, distinct from those of statins and bile acid sequestrants. Ezetimibe, approved in late October, represents the first new class of cholesterol-lowering drugs in 15 years. When used as monotherapy, ezetimibe lowers low-density lipoprotein cholesterol (LDL-C) levels up to 18.5%. Coadministration of ezetimibe with statin therapy reduces LDL-C levels up to an additional 22%, further improves levels of high-density lipoprotein cholesterol (up to +3%) and triglycerides (up to 11%), and enables greater numbers of patients (72% vs 19%) to achieve their LDL-C goal. Ezetimibe monotherapy is tolerated as well as placebo, and coadministration of ezetimibe with statins is tolerated as well as statins alone. Ezetimibe has a low potential for drug interactions with cytochrome P450 substrates and does not affect the absorption of fat-soluble vitamins. The article reviews ezetimibe's chemistry, pharmacology, pharmacokinetics, and clinical trial results.
ISSN:1082-801X
1938-1166