Class: Antihyperlipidemic, Cholesterol Absorption Inhibitor
Dosage Forms. Tablet: 10 mg
Common FDA Label Indication, Dosing, and Titration.
1. Familial hypercholesterolemia-homozygous: with atorvastatin or simvastatin: Adults and Children older than 10 y of age, 10 mg po daily
2. Mixed hyperlipidemia: 10 mg po daily in combination with fenofibrate
3. Primary hypercholesterolemia: 10 mg po daily, alone or in combination with an HMG-CoA reductase inhibitor (statin)
Off-Label Uses. None
MOA. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins and of fenofibrate.
Drug Characteristics: Ezetimibe
Medication Safety Issues: Ezetimibe
Drug Interactions: Ezetimibe
Adverse Reactions: Ezetimibe
Efficacy Monitoring Parameters. Reduction in total cholesterol, LDL-cholesterol, and triglycerides levels; increase in HDL-cholesterol levels.
Toxicity Monitoring Parameters. Signs/symptoms of rhabdomyolysis (myalgias, dark urine, arthralgias, fatigue), yellowing of eyes or skin, severe abdominal pain, LFT and CBC, SCr.
Key Patient Counseling Points. Take with or without food and may be taken at the same time as a concurrent statin. In patients receiving a bile acid sequestrant concurrently, ezetimibe should be taken at least 2 h before or 4 h after the bile acid sequestrant is taken.
Clinical Pearls. Statins are the most effective lipid-altering agents for decreasing LDL cholesterol, and are considered drugs of choice. Ezetimibe has modest single agent activity and is used in combination with statin or in combination with fenofibrate. Ezetimibe is also available in fixed dose combination with simvastatin.