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What is ezetimibe?

Ezetimibe (uh · zeh · tuh · mibe) is a cholesterol-lowering medication. Ezetimibe is the generic drug name for the brand Zetia.

Ezetimibe’s drug classification is a cholesterol absorption inhibitor. Doctors prescribe ezetimibe to lower total cholesterol levels and low-density lipoprotein (LDL) cholesterol.

LDL is known informally as “bad cholesterol” because it’s responsible for blood vessel plaque and narrowing of the arteries. The other type of cholesterol is high-density lipoprotein (HDL) — also dubbed “good cholesterol.” HDL brings cholesterol to the liver, rids it from the body, and prevents it from building up as plaque.

Ezetimibe may be used alone or with other prescribed medications to improve cholesterol levels. Ezetimibe-statin combination therapy is a standard treatment. (Statins are also used for lowering and managing cholesterol).

Ezetimibe is only part of the overall strategy for maintaining healthy cholesterol levels. A proper diet and exercise are also vital to managing your cholesterol levels effectively.

What is ezetimibe used to treat?

Doctors prescribe ezetimibe to lower overall cholesterol levels. It works by promoting proper blood flow and oxygen supply throughout the body, especially in the brain and heart. Doctors prescribe ezetimibe to treat:

  • Primary hyperlipidemia A genetic condition that affects how the body eliminates cholesterol.

  • Mixed hyperlipidemia A genetic disorder that affects how the body eliminates cholesterol and triglycerides.

  • Homozygous familial hypercholesterolemia A rare genetic disorder that makes it difficult for the body to clear LDL cholesterol.

  • Homozygous sitosterolemia A rare genetic condition caused by a genetic mutation that affects how plant sterols are cleared from the body. Plant sterols are a specific type of fat usually found in nuts and other plant-based foods.

Ezetimibe prevents or significantly reduces the risk of diseases and medical emergencies like: 

  • Stroke

  • Heart attack

  • Angina

  • Atherosclerosis (hardening of the arteries)

How do you take ezetimibe?

 Ezetimibe is only available as a 10mg oral tablet.

Here is a typical dosage of ezetimibe for anyone over the age of ten:

  • For hyperlipidemia 10mg, taken orally, once daily

  • For homozygous familial hypercholesterolemia 10mg, taken orally, once daily

  • For sitosterolemia 10mg, taken orally, once daily

Children under age ten should not take ezetimibe.

Seeing results 

Your doctor will check your cholesterol levels frequently to verify that ezetimibe is working as expected. Improvement may not be noticeable when you first begin taking ezetimibe, but it may start to lower your cholesterol levels in as little as two weeks.

Potential side effects of ezetimibe

Common side effects of ezetimibe are generally mild and include cold and flu-like symptoms such as: 

  • Diarrhea 

  • Joint pain 

  • Sinus infection symptoms

  • Pain in limbs or extremities 

  • Fatigue

Other side effects might also include: 

When ezetimibe is taken with a statin (a lipid-lowering medication) it may increase the risk of  side effects, including:

  • Muscle pains

  • Headaches

  • Increased liver enzymes

There are some risks associated with taking ezetimibe. It is rare, but possible to develop kidney or liver damage. Those who have liver-related health problems should not take ezetimibe.

Long-term use of ezetimibe

Doctors may prescribe ezetimibe for short-term, long-term, or lifetime use. It must be taken as prescribed to avoid associated risks and side effects.

Missed doses

If you miss a dose of ezetimibe, take it as soon as you remember. However, do not take it within six hours of your next scheduled dose. If you are too close to the timing of the next dose, skip it and take the next dose as planned. Try to take your medication on a regular schedule and avoid missed doses.


If you suspect or know that you’ve taken too much ezetimibe, call 911 or seek immediate medical attention.

What to discuss with your doctor before taking ezetimibe

 Here are some of the things you must discuss with your doctor before taking ezetimibe: 

  • All the medications you’re currently taking (prescribed or non-prescribed). 

  • All the vitamins and supplements you are taking or planning to take.

  • Allergies to specific medications (especially ezetimibe). 

  • Liver problems or a history of liver problems. 

  • Whether or not you consume alcohol, how much, and how frequently. Alcohol may increase the possibility of liver damage. In addition, ezetimibe with a statin drug may significantly increase the risk of side effects.

  • Whether you are pregnant or trying to get pregnant. 

  • Whether you are currently breastfeeding or planning to breastfeed. 

  • Your age. Ezetimibe is metabolized differently depending on your stage of life. Ezetimibe is not suitable for those under age ten. 

  • Suitable dietary and exercise regimens while using ezetimibe to lower cholesterol.

Stopping ezetimibe

Do not stop taking ezetimibe without talking to your doctor first. Suddenly stopping ezetimibe without consultation might increase your cholesterol levels, putting you at risk for health complications.

Ezetimibe and pregnancy

Ezetimibe belongs to the US FDA Pregnancy Category C. You should not take ezetimibe during pregnancy unless advised to do so by your doctor.

Whether ezetimibe could pass into the child from the mother through breast milk is unknown. Therefore, breastfeeding mothers are advised not to use ezetimibe unless their healthcare provider determines that the potential benefits outweigh the risks.

Ezetimibe and interactions with other drugs

Drugs that may interact with ezetimibe and cause unwanted side effects include:

  • Other cholesterol-lowering drugs Taking cholestyramine (Prevalite), colestipol (Colestid), or colesevelam (Welchol) may decrease the efficiency of ezetimibe.

  • Fibrates Taking fenofibrate (Tricor, Fenobrat) or gemfibrozil (Lopid) with ezetimibe may cause gallstones.

  • Warfarin Taking ezetimibe with the blood thinner warfarin (Coumadin) might decrease the blood thinner’s effectiveness. You should have your warfarin level monitored closely while taking ezetimibe.

  • Cyclosporine Taking ezetimibe with cyclosporine (Gengraf, Neoral, SandIMMUNE, Apo-cycloSPORINE)may increase levels of both drugs and therefore increase the risk of side effects.

 Allergy information

Ezetimibe may cause a severe allergic reaction. Symptoms of a severe allergic reaction may include:

  • Trouble breathing

  • Trouble swallowing

  • Hives

  • Rash

  • Swelling in the face, lips, tongue, lips, or throat

If you ever develop these symptoms upon taking ezetimibe, seek immediate medical attention. Call 911 or go to the nearest emergency room.

Clinical trial history

During Phase II and Phase III clinical trial development, ezetimibe proved to be an effective and safe option for treating high cholesterol even in difficult-to-treat cases, such as homozygous and heterozygous familial hypercholesterolemia and sitosterolemia. Ezetimibe was FDA-approved in 2002.

Tips and advice for taking ezetimibe

Here are some tips and advice when taking ezetimibe:

  • You can take ezetimibe with or without food.

  • Take ezetimibe at the same time every day.

  • If you take other cholesterol-lowering medications (other than a statin), take ezetimibe two hours before the other medication or four hours after.

  • Follow your doctor's instructions and regularly check your blood cholesterol levels to ensure ezetimibe is working.

  • Get your liver function checked periodically, especially if you receive ezetimibe-statin combination therapy.

  • Self-monitor for side effects, especially if you take ezetimibe with other cholesterol-lowering drugs or statins. 

  • To effectively manage your cholesterol levels while taking ezetimibe, eating a healthy diet and exercising are essential.

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Here at HealthMatch, we’ve done our best to ensure that the information provided in this article is helpful, up to date, and, most importantly, accurate.

However, we can’t replace the one-to-one advice of a qualified medical practitioner or outline all of the possible risks associated with this particular drug and your circumstances.

It is therefore important for you to note that the information contained in this article does not constitute professional medical or healthcare advice, diagnosis or recommendation of treatment and is not intended to, nor should be used to, replace professional medical advice. This article may not always be up to date and is not exhaustive of all of the risks and considerations relevant to this particular drug. In no circumstances should this article be relied upon without independent consideration and confirmation by a qualified medical practitioner.

Your doctor will be able to explain all possible uses, dosages, precautions, interactions with other drugs, and other potential adverse effects, and you should always talk to them about any kind of medication you are taking, thinking about taking or wanting to stop taking.

Curious about clinical trials?

Access the latest treatments and medications. unavailable elsewhere - entirely free of charge. We make it easy to take part.