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The page below is a sample from the LabCE course Pharmacology of Antihyperlipidemic Medications for Laboratory Professionals. Access the complete course and earn ASCLS P.A.C.E.-approved continuing education credits by subscribing online.

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Cholesterol Absorption Inhibitors

Drug example: Ezetimibe

Mechanism of action: Normally, transporters exist in the GI tract to facilitate the absorption of cholesterol from digested foods. Ezetimibe inhibits a transporter involved in this process, which causes a decrease in the amount of cholesterol absorbed. This initiates a series of changes in the liver that ultimately results in a decreased in LDL.

Use: Ezetimibe can decrease LDL cholesterol by 15-20% alone. It is often combined with a “statin” in patients who need to obtain an even larger decrease in LDL cholesterol than a statin alone can provide.

Drug toxicity: There is little to say about the side effects or toxicity of ezetimibe, as it is well tolerated by patients. If it is used with a statin, however, there is an increased risk of liver toxicity.