Ezetimibe for Management of Hypercholesterolemia

Abstract

Based on the data currently available, it appears that ezetimibe has a potential role in the treatment of primary hypercholesterolemia; however further data are needed to determine its long-term tolerability and efficacy. The potential roles for ezetimibe include its concurrent use with a statin to further enhance the lowering of LDL-C. Other possible roles for ezetimibe include its concurrent use with a statin to permit a lowering of statin dosage to avoid statin-related complications or its use as monotherapy to treat hypercholesterolemia when statin use cannot be tolerated or is contraindicated. Outcome data demonstrating that cardiovascular morbidity and/or mortality are reduced by ezetimibe therapy have yet to be generated.

Effect of ezetimibe on incretin secretion in response to the intestinal absorption of a mixed meal

“…However, several studies have reported that ezetimibe treatment results in a modest decrease in plasma triglyceride concentrations (3,18,29), most likely due to a specific reduction of saturated fat absorption (26). Ezetimibe inhibits intestinal cholesterol absorption up to 92-96% in a dose-dependent manner (45,47,49).…”

Efficacy of Combination Drug Pulse Therapy in Maintaining Lipid Levels in Patients Intolerant of Daily Statin Use

“…Studies have shown that when used in combination with statins, ezetimibe results in incremental lowering of total and LDL cholesterol. [3][4][5][6] Moreover, it does not increase the incidence of myopathy or rhabdomyolysis when administered with statins. Similarly, the addition of colesevelam to statin therapy effectively lowers total and LDL cholesterol and does not cause any adverse effects on liver and skeletal muscles.…”

Ezetimibe (Zetia)

“…Mean percent change from treated HMG-CoA reductase inhibitor therapy was -17% for total cholesterol, -25% for LDL-C, -14% for triglycerides, and +3% for HDL-C [1,2].…”

“…In patients with primary hypercholesterolemia, ezetimibe as monotherapy reduced LDL-C by 18%, reduced total cholesterol by 13%, reduced triglycerides by 9% and raised HDL by 1% [1,2].…”

“…It can be used as monotherapy for primary hypercholesterolemia but most likely will be used in combination therapy with statins in which it results in incremental lowering of total and LDL cholesterol [1][2][3][4]. It can also be used as part of therapy for homozygous familial hypercholesterolemia and homozygous sitosterolemia.…”