Ezetimibe Pharmacology


About Ezetimibe
Cholesterol Absorption Inhibitor, 2-Azetidinone derivative, Hypolipidemic agent.
Mechanism of Action of Ezetimibe
It reduces the absorption of cholesterol from the intestine by localising at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the diet. Specifically, it appears to bind to the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelium, a critical mediator of cholesterol absorption. This decreased cholesterol absorption leads to an increase in LDL-cholesterol uptake into cells, thus decreasing levels in the blood plasma.
Pharmacokinets of Ezetimibe
Absorption- Poorly absorbed after oral administration
Distribution- Widely distributed in the body as plasma protein binding form (>90%)
Metabolism- Metabolized in the liver and intestinal wall
Excretion- Excreted through urine and feces

Onset of Action for Ezetimibe
Duration of Action for Ezetimibe
Half Life of Ezetimibe
19-30 hours
Side Effects of Ezetimibe
1. Difficulty breathing
2. Closing of the throat
3. Swelling of the lips, tongue, or face
4. Abdominal pain
5. Diarrhea
6. Tiredness
7. Headache
8. Dizziness
9. Sore throat
10. Runny nose
11. Sneezing
12. Joint pain
13. Rash
14. Itching.
15. Hoarseness
16. Upset stomach
17. Unusual bleeding or bruising
18. Loss of appetite
19. Pain in the upper right part of the stomach
20. Yellowing of the skin or eyes
21. flu-like symptoms
22. Muscle pain or weakness
23. Fever
24. Chills
25. Pale or fatty stools
26. Chest pain
Contra-indications of Ezetimibe
Contraindicated in patients with hypersensitivity to the drug or any components of it
Special Precautions while taking Ezetimibe
1. Liver disease
2. Liver enzymes, persistently high levels
3. Major surgery or serious illness
4. Diabetes mellitus
5. Kidney disease
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Use with caution
Indications for Ezetimibe
1. Adjunct to dietary measures and statin in primary and homozygous familial hypercholesterolaemia
2. Adjunct to dietary measures in homozygous familial sitosterolaemia
Interactions for Ezetimibe
Cyclosporin: Plasma concentraction of ezetimibe increased. Lipid-regulating drugs: Avoid concomitant use with fibrates.
Typical Dosage for Ezetimibe
Adult -10 mg/day
Schedule of Ezetimibe
Storage Requirements for Ezetimibe
Stored at room temperature (15-30 degree C).
Effects of Missed Dosage of Ezetimibe
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Ezetimibe
Give symptomatic and supportive treatment

Home Delivery for Ezetimibe in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including ezetimibe.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for ezetimibe and other medicines and health products. Home delivery services for ezetimibe may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take ezetimibe only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for ezetimibe before they complete the sale. You can get this information while placing the order for ezetimibe with the pharmacy.

Ezetimibe is a generic medicine name and there are several brands available for it. Some of the brands for ezetimibe might be better known than ezetimibe itself. If the pharmacy that's willing to deliver medicines to your home doesn't have ezetimibe in stock, you can ask for one of the branded alternatives for ezetimibe.