Ezetimibe selectively inhibits the Niemann-Pick C1-Like 1 (NPC1L1) protein located at the brush border of the small intestine.
✅ This blocks absorption of dietary and biliary cholesterol into enterocytes (intestinal cells).
🔄 As a result:
↓ Cholesterol delivery to the liver
↑ LDL receptor expression in the liver
↑ Clearance of LDL from the blood
📉 Net Effect: ↓ LDL-C (by ~18–25%)
🧪 Often used with statins to enhance LDL lowering synergistically.
🩺 Generally well tolerated, but may cause:
Category | Common Side Effects | Rare but Serious Effects |
---|---|---|
💢 GI Disturbances | Diarrhea, abdominal pain, flatulence | Pancreatitis (rare) |
😴 Systemic | Fatigue, myalgia | Hepatitis (esp. with statins) |
🩸 Hepatic | ↑ Liver enzymes (when combined with statins) | Liver dysfunction (monitor LFTs) |
💊 Hypersensitivity | Rash, angioedema (rare) | Anaphylaxis (extremely rare) |
🧠 Ezetimibe is not affected by CYP450 enzymes, so fewer drug interactions than statins.
🛡️ Good alternative or add-on therapy for patients who cannot tolerate high-dose statins.