The reduction of circulating atherogenic
lipoproteins through lifestyle modification and pharmacologic intervention is an important therapeutic goal in patients at risk for acute cardiovascular events. A large number of clinical trials have demonstrated that the reduction of
low-density lipoprotein cholesterol (
LDL-C) is associated with significant decreases in the incidence of all cause mortality,
stroke, fatal and nonfatal
myocardial infarction, and the need for revascularization with
coronary artery bypass grafting and percutaneous transluminal coronary angioplasty.
Therapy with 3-hydroxy-3-methylglutaryl
coenzyme A (
HMG CoA) reductase inhibitors (i.e.,
statins) are the agents of choice for treating a variety of
dyslipidemias, particularly when
LDL-C levels are elevated. The
statins are highly efficacious; however, not all patients are able to tolerate the higher doses of these medications due to adverse side-effects such as hepatoxicity and
myotoxicity. Moreover, many patients cannot achieve their various
lipoprotein targets at even the highest doses of these medications.
Ezetimibe is a novel
cholesterol absorption inhibitor that blocks the translocation of dietary and biliary
cholesterol from the gastrointestinal lumen into the intracellular space of jejunal enterocytes.
Ezetimibe undergoes enterohepatic recirculation with minimal systemic exposure and not does not adversely impact the pharmacokinetic profile of
statins.
Ezetimibe significantly reduces serum
LDL-C. It is safe when used as monotherapy or when used in combination with
statins.
Ezetimibe is indicated in the management of
hyperlipidemia,
familial hypercholesterolemia, and
sitosterolemia and significantly increases the percentage of patients able to reach their
lipid-lowering goals.