Abstract
The therapy with statin and ezetimibe combination is a beneficial method in high risk patients because it inhibits both mechanisms of LDL-cholesterol (LDL-C) level increase. Ezetimibe is the first agent of a class of selective cholesterol absorption inhibitors.
Ezetimibe inhibits the absorption of biliary and dietary cholesterol from the small intestine without affecting the absorption of fat-soluble vitamins, triglycerides or bile acids. The site of its pharmacological action is the brush border of the small intestine where it decreases cholesterol uptake into the enterocytes.
There are many preclinical and clinical studies demonstrating lipidlowering properties of ezetimibe as monotherapy and its synergistic effect in combination with HMGCoA reductase inhibitors (statins). When given in monotherapy or in combination with a statin, ezetimibe significantly reduces LDL-cholesterol and increases HDL-cholesterol.
The fixed combination of atorvastatin and ezetimibe, one of the most extensively studied products, has been approved in several countries, including the United States. Depending on the atorvastatin dose, this combination provides LDL-C reduction of 50-60%, triglycerides reduction of 30-40% and HDL-cholesterol (HDL-C) increases of 5-9%.
The results are more pronounced than with atorvastatin alone. There are also trials what confirm the effects of simvastatin and ezetimibe combination as well as a significant reduction in cardiovascular risk which was dependent on LDL-C level decrease.
The combination of atorvastatin with ezetimibe induced greater regression of atherosclerotic changes than atorvastatin alone. This combination is generally well tolerated.
The IMPROVE-IT study provides an overview of the evidence supporting the inclusion of atorvastatin with ezetimibe in the treatment of dyslipidemia.