Ezetimibe Patient Tips

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on Oct 23, 2023.

1. How it works

• Ezetimibe (brand name: Zetia) works by reducing cholesterol absorption from the small intestine. This means less cholesterol is delivered and stored in your liver. More cholesterol is then cleared from the blood and helps to lower your cholesterol levels. It is in the class of drugs known as cholesterol absorption inhibitors.
• More specifically, ezetimibe worls by targeting the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols.
• Ezetimibe is used to treat high cholesterol in people who cannot control their cholesterol levels by diet and exercise alone. You should also adhere to a cholesterol-lowering diet and an exercise plan while taking this medication.
• Your doctor may need to prescribe other cholesterol-lowering medications, like statins, to increase the effect of ezetimibe.

2. Upsides

• Ezetimibe can be taken with or without other cholesterol-lowering medications like statins, fenofibrate or bile-acid sequestrants that also help to lower lipids. These medicines work in a different way and have a complementary effect to ezetimibe.
• Ezetimibe is only taken once a day as an oral tablet you swallow, with or without food. The usual dosage is 10 mg per day.
• Ezetimibe can also be found in combination products that may be more convenient. For example, Vytorin (ezetimibe and simvastatin) contains both ezetimibe and a statin. Ezetimibe is also available combined with bempedoic acid (brand name: Nexlizet), a non-statin cholesterol-lowering medicine. Bempedoic acid works by lowering the amount of cholesterol made in the liver.
• Ezetimibe can be used in children at certain ages and with certain types of cholesterol problems as recommended by your doctor.
• Ezetimibe is available as a generic product in a 10 mg tablet and is very affordable in the US. It is also available as a brand name drug called Zetia, made by Organon.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Diarrhea, upper respiratory tract infection, joint pain, sinusitis, flu-like symptoms and feeling tired when ezetimibe if used alone. When ezetimibe is used with a statin, side effects may include common cold symptoms, feeling tired, diarrhea, muscle aches, pain in arms or legs, back pain, upper respiratory tract infection, flu-like symptoms, joint pain and diarrhea.
• Rarely, increased liver enzymes and severe muscle pain may occur, if ezetimibe is used alone or combined with a statin or fibrate. This may include cases of myopathy and rhabdomyolysis. Contact your doctor right away if you have severe muscle pain, tenderness, or weakness, feel more tired than usual, or have a fever. These may be symptoms of myopathy or rhabdomyolysis, which may lead to muscle breakdown and kidney damage.
• Statins have been associated with memory loss, forgetfulness, and confusion in rare instances. This may also occur if statins are used with ezetimibe. These symptoms typically reverse if the statin is discontinued by your doctor.
• Ezetimibe has not been shown to prevent heart disease or heart attacks. Although ezetimibe has been shown to lower cholesterol levels, it will not help you lose weight. Continue a diet and exercise program as recommended by your doctor.
• Stop using this medicine and get medical help right away if you have symptoms of a serious allergic reaction (for example, swelling in your face, tongue or throat; trouble breathing or swallowing; fainting; feeling dizzy; fast heartbeat; severe skin rash, hives, and itching; flu-like symptoms including fever, sore throat, cough, tiredness, and joint pain.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Ezetimibe is effective at lowering cholesterol levels when taken on a regular basis and can be combined with certain other cholesterol treatments in some patients to further reduce blood lipids (fats). Most people tolerate ezetimibe well, but some may have side effects like muscle pain or liver toxicity, especially if used with a statin. Ezetimibe has not been shown to reduce the risk for heart disease or a heart attack.

5. Tips

• Take once daily, with or without food. May be taken at any time of the day (morning or night); however, it is best to be consistent with the time you take your tablets. If you miss a dose, take it as soon as possible, but do not double your next dose.
• Take your medicine exactly as directed by your doctor. Do not change your dose or stop treatment unless recommended by your doctor.
• Tell your doctor if you take other medicines to help control your cholesterol or other lipid levels, like statins, bile-acid sequestrants or fibrates.
• If you are taking another medicine to help control your cholesterol, ask your doctor if you can take it at the same time as you take ezetimibe.
• Take ezetimibe either 2 hours before or 4 hours after taking a bile acid sequestrant (such as cholestyramine, colestipol or colesevelam). Taking these medicines at the same time may reduce the absorption and effectiveness of ezetimibe
• You will need to follow a cholesterol-lowering diet and exercise plan while on this medicine. Ask your doctor if you need diet information. If you smoke, ask your doctor how you can quit.
• Tell your doctor if you have liver problems. Contact your doctor right away if you notice any yellowing of your skin or eyes, shortness of breath, unexplained cough, severe muscle pain, tenderness, or weakness. Ask your doctor how to recognize liver problems.
• If you are a female of childbearing age you should use an effective method of birth control to prevent pregnancy while using ezetimibe added to a statin therapy. Let your doctor know if you are breastfeeding.

6. Response and effectiveness

Ezetimibe has been shown in studies to lower total cholesterol levels, low-density lipoprotein cholesterol (LDL-C or “bad” cholesterol), apolipoprotein B (Apo B) levels, non-high density lipoprotein cholesterol (non-HDL-C), triglycerides (TG) and increase high density lipoprotein cholesterol (HDL-C or “good”) levels, compared to a placebo (an inactive product), when used with diet.

• A maximum effect is generally achieved within 2 weeks and maintained during ongoing therapy. When used alone and compared to a placebo in two studies, ezetimibe reduced LDL cholesterol levels by 18%. Higher levels may be achieved when used with other cholesterol-lowering agents, like statins or fenofibrate. Ezetimibe has also been shown to lower elevated sitosterol and campesterol (plant sterols) levels in adults and children 9 year of age and younger with Homozygous Familial Sitosterolemia, when used with diet. Sitosterolemia is a rare genetic condition in which fatty substances (lipids) from vegetable oils, nuts, and other plant-based foods build up in the blood and tissues.
• In studies, ezetimibe significantly lowered plasma sitosterol by 21% and campesterol by 24% compared to when they first started the study. However, patients who received the placebo (inactive) treatment had increases in sitosterol and campesterol of 4% and 3%, respectively.

7. Interactions

• Medicines that interact with ezetimibe may either decrease its effect, increase its side effects, or change how other medicines work. Speak to your doctor or pharmacist about how drug interactions should be managed.
• It is important to tell your doctor and pharmacist about all other medications you use, including prescription drugs, over-the-counter (OTC medicines) vitamins, herbs and dietary supplements. Do not start using any medications without first talking to your healthcare provider.

Tell your healthcare provider if you take:

• Bile acid sequestrants (a medicine to lower LDL)
• Cyclosporine (an immune system medicine)
• Fibrates (medicines to lower cholesterol)
• Flax or Flaxseed oil
• Statins (for example: atorvastatin or simvastatin)
• Some prostate cancer medicines (for example: apalutamide or darolutamide)
• Red Yeast Rice
• Warfarin

Note that this list is not all-inclusive and includes only common medications that may interact with ezetimibe. Refer to the prescribing information for ezetimibe for a complete list of interactions.

Related/similar drugs

Frequently asked questions

• Does Zetia (ezetimibe) cause memory loss?
• Can Zetia (ezetimibe) cause liver damage?
• How does Zetia (ezetimibe) work to lower cholesterol?
• Does Zetia (ezetimibe) cause weight gain/loss or muscle aches/pains?
• What happens if you stop taking Ezetimibe?
• When should you take ezetimibe?
• Is ezetimibe a statin drug?
• When is the best time to take ezetimibe?
• Does ezetimibe lower triglycerides?

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Ezetimibe only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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