Daily Medication Pearl: Ezetimibe (Zetia)

Article

Ezetimibe (Zetia) is an inhibitor of intestinal cholesterol and related phytosterol absorption indicated as an adjunct to diet to reduce elevated total cholesterol.

Medication Pearl of the Day: Ezetimibe (Zetia)

Indication: Ezetimibe (Zetia) is an inhibitor of intestinal cholesterol and related phytosterol absorption indicated as an adjunct to diet to reduce elevated total cholesterol, low-density lipoprotein cholesterol, Apo B, and non-high-density lipoprotein cholesterol in patients with primary hyperlipidemia, alone or in combination with an HMGCoA reductase inhibitor (statin).

Insight:

  • Dosing: One 10 mg tablet once daily, with or without food.
  • Dosage forms: Tablets 10 mg.
  • Adverse events: Nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, and diarrhea.
  • Mechanism of action: The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. Ezetimibe does not inhibit cholesterol synthesis in the liver or increase bile acid excretion. Instead, ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood. This distinct mechanism is complementary to that of statins and of fenofibrate.

Source: label (fda.gov)

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