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Multiple Choice

Ezetimibe mechanism and typical combination in therapy?

Ezetimibe works by blocking cholesterol absorption in the intestine through the NPC1L1 transporter in enterocytes. This reduces the amount of cholesterol delivered to the liver, lowering hepatic cholesterol and upregulating LDL receptors, which helps clear LDL cholesterol from the blood. Because of this mechanism, it is typically combined with a statin to achieve a greater LDL-C reduction than either drug alone—the statin reduces cholesterol synthesis in the liver while ezetimibe reduces intestinal cholesterol uptake. It does not increase cholesterol synthesis itself, it does not inhibit bile acid reabsorption (that’s the role of bile acid sequestrants), and it does not markedly raise HDL cholesterol.

Ezetimibe works by blocking cholesterol absorption in the intestine through the NPC1L1 transporter in enterocytes. This reduces the amount of cholesterol delivered to the liver, lowering hepatic cholesterol and upregulating LDL receptors, which helps clear LDL cholesterol from the blood. Because of this mechanism, it is typically combined with a statin to achieve a greater LDL-C reduction than either drug alone—the statin reduces cholesterol synthesis in the liver while ezetimibe reduces intestinal cholesterol uptake. It does not increase cholesterol synthesis itself, it does not inhibit bile acid reabsorption (that’s the role of bile acid sequestrants), and it does not markedly raise HDL cholesterol.