Ezetimibe

Information about Ezetimibe

Ezetimibe is an inhibitor of intestinal cholesterol absorption that is widely used in the therapy of hypercholesterolemia, usually in combination with other agents. Ezetimibe therapy is associated with a low rate of serum aminotransferase elevations and clinically apparent liver injury due to ezetimibe occurs, but is rare.

Mechanism of action of Ezetimibe

Ezetimibe (e zet' i mibe) is a synthetic azetidinone that inhibits cholesterol absorption from the intestine. Ezetimibe acts by binding to and inhibiting the Niemann-Pick C1-like 1 protein (NPC1), the major transporter of cholesterol in the intestinal brush border. Ezetimibe by itself lowers serum cholesterol, but the inhibition of cholesterol absorption is usually followed by a compensatory increase in hepatic cholesterol synthesis, a response that can be blocked by hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors [statins]. For this reason, ezetimibe is commonly used in combination with a statin. Addition of ezetimibe to a maximized dose of statins generally lowers LDL-cholesterol levels by 22% to 24%.

FDA approval information for Ezetimibe

Ezetimibe was approved for use in the United States in 2002 and is usually recommended as an adjunctive therapy to diet or in combination with a statin in management of patients with hypercholesterolemia at high risk for cardiovascular or cerebrovascular disease. It is also used alone in patients who are intolerant of statins and can be combined with other lipid-lowering agents (such as fibrates or anti-PCSK9 monoclonal antibodies).

Dosage and administration for Ezetimibe

Ezetimibe is available in 10 mg tablets under the brand name Zetia and the usually recommended dose is 10 mg daily. Ezetimibe is also available in a fixed combination with simvastatin (20 or 40 mg) under the trade name Vytorin and with atorvastatin (10, 20, 40 or 80 mg) under the trade name Liptruzet. Ezetimibe has achieved wide scale acceptance and several million prescriptions are filled yearly.

Side effects of Ezetimibe

Common side effects of ezetimibe include diarrhea and flatulence. Rare, potentially severe adverse effects include hypersensitivity reactions, myopathy and rhabdomyolysis.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

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