How does Ezetimibe work ?

Created on : #march2025 #april2025

Author: Dr. Om J Lakhani

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Introduction

Ezetimibe is a medication that helps lower cholesterol in your blood. Let me explain how it works in simple terms:

When you eat food containing cholesterol, your body normally absorbs this cholesterol through your small intestine. Ezetimibe works by blocking this absorption process[1][2][3]. It specifically targets and inhibits a protein called Niemann-Pick C1-Like 1 (NPC1L1), which is found in the lining of your small intestine and is responsible for absorbing cholesterol from your food[1][6].

By preventing cholesterol absorption in your intestines, ezetimibe:

  1. Reduces the amount of cholesterol that enters your bloodstream from your diet[2][3]
  2. Decreases the amount of cholesterol delivered to your liver[6]
  3. Forces your liver to take more cholesterol from your bloodstream to compensate for the reduced supply[1][3]
  4. This process ultimately lowers the levels of "bad" cholesterol (LDL) in your blood[4]

Unlike statins (another type of cholesterol medication) that work by reducing cholesterol production in the liver, ezetimibe specifically targets cholesterol absorption in the intestines[7]. This is why doctors sometimes prescribe ezetimibe along with statins for better cholesterol control - they work in different ways to lower cholesterol levels[7][9].

The effects of ezetimibe are usually noticeable within about 2 weeks of starting treatment[7]. Even though you might not feel any different while taking it (since high cholesterol itself doesn't usually cause symptoms), the medication is working to reduce your cholesterol levels and help protect your blood vessels[7].

Ezetimibe is typically prescribed along with a healthy diet to effectively manage cholesterol levels[3][7]. It's often used for people who cannot take statins or for those who need additional cholesterol-lowering beyond what statins alone can provide[2][9].

Mechanism of Action: Ezetimibe INTESTINAL LUMEN Without Ezetimibe NPC1L1 C C C C C Cholesterol Absorbed With Ezetimibe NPC1L1 E C C C C Cholesterol Blocked E Ezetimibe Ezetimibe blocks the NPC1L1 protein, preventing cholesterol absorption in the small intestine

Citations:
[1] https://en.wikipedia.org/wiki/Ezetimibe
[2] https://my.clevelandclinic.org/health/treatments/ezetimibe-tablets
[3] https://www.drugs.com/ezetimibe.html
[4] https://www.webmd.com/drugs/2/drug-64335/ezetimibe-oral/details
[5] https://medlineplus.gov/druginfo/meds/a603015.html
[6] https://go.drugbank.com/drugs/DB00973
[7] https://www.nhs.uk/medicines/ezetimibe/common-questions-about-ezetimibe/
[8] https://www.healthline.com/health/drugs/ezetimibe-oral-tablet
[9] https://www.nhs.uk/medicines/ezetimibe/about-ezetimibe/
[10] https://www.ncbi.nlm.nih.gov/books/NBK532879/