What is the mechanism of action of ezetimibe?

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Multiple Choice

What is the mechanism of action of ezetimibe?

Ezetimibe works by blocking the NPC1L1 transporter in the small intestine, which is responsible for the uptake of cholesterol from the gut. By inhibiting this transporter, ezetimibe reduces the amount of cholesterol that enters the body from dietary and biliary sources. With less cholesterol delivered to the liver, hepatic cholesterol levels fall, prompting upregulation of LDL receptors and increased clearance of LDL cholesterol from the blood, leading to lower plasma LDL-C. This mechanism is different from inhibitors of HMG-CoA reductase (statins), which reduce cholesterol synthesis in the liver. Ezetimibe’s action also does not directly promote biliary cholesterol excretion as its primary effect; instead, its main impact is reducing intestinal absorption, which complements the statin effect when used together for added LDL lowering.

Ezetimibe works by blocking the NPC1L1 transporter in the small intestine, which is responsible for the uptake of cholesterol from the gut. By inhibiting this transporter, ezetimibe reduces the amount of cholesterol that enters the body from dietary and biliary sources. With less cholesterol delivered to the liver, hepatic cholesterol levels fall, prompting upregulation of LDL receptors and increased clearance of LDL cholesterol from the blood, leading to lower plasma LDL-C.

This mechanism is different from inhibitors of HMG-CoA reductase (statins), which reduce cholesterol synthesis in the liver. Ezetimibe’s action also does not directly promote biliary cholesterol excretion as its primary effect; instead, its main impact is reducing intestinal absorption, which complements the statin effect when used together for added LDL lowering.

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