Which nonstatin medication is most effective at lowering LDL-C?

Prepare for the Lippincott Pharmacology Exam with interactive flashcards and multiple-choice questions, each accompanied by detailed hints and explanations. Master your exam with ease!

Alirocumab is a monoclonal antibody that specifically inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). By binding to PCSK9, it prevents this protein from promoting the degradation of LDL receptors in the liver. This action leads to increased availability of LDL receptors on hepatocyte surfaces, resulting in enhanced uptake of LDL cholesterol (LDL-C) from the bloodstream. Consequently, this mechanism of action makes alirocumab one of the most effective nonstatin medications for lowering LDL-C levels.

In contrast, niacin primarily works by inhibiting liver synthesis of VLDL (very low-density lipoprotein), which subsequently lowers LDL-C, but its degree of LDL-C reduction is generally less than that achieved with PCSK9 inhibitors like alirocumab. Cholestyramine is a bile acid sequestrant that binds bile acids in the gut, preventing their reabsorption, which leads to increased conversion of cholesterol to bile acids and a modest reduction in LDL-C. Ezetimibe functions by inhibiting the intestinal absorption of cholesterol, also leading to some reduction in LDL-C; however, its effect is not as pronounced as that of PCSK9 inhibitors.

Overall, the mechanism and efficacy

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