Some text some message..
Back 💡 Ezetimibe (Cholesterol Absorption Inhibitor) 22 May, 2025

🔬 Mechanism of Action (MOA):

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.


⚠️ Adverse Effects of Ezetimibe:

🩺 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)

📌 Clinical Note:

  • 🧠 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.