Ezetimibe

Indications

• Hypercholesterolaemia

• Homozygous sitosterolemia (phytosterolemia)

Administration/Absorption

Distribution

Mechanism

• Localises at the brush border of the small intestine

  • inhibits the absorption of cholesterol from the intestine

• Binds to a critical mediator of cholesterol absorption:

  • • Niemann-Pick C1-Like 1 (NPC1L1) protein

    • on the gastrointestinal tractepithelial cells^[5] as well as in hepatocytes.^[6]

  • Also, decreased cholesterol absorption leads to an upregulation of LDL-receptors on the surface of cells

    • => increased LDL-cholesterol uptake into cells

    • => decreased plasma levels of LDL

Excretion