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Ezetimibe: 7 things you should know

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on Aug 8, 2022.

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.
  • Exetimibe targets the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols.
  • Ezetimibe is a prescription medicine that reduces your total and LDL (bad) cholesterol levels in the blood. Your total cholesterol is made up of LDL and HDL cholesterol.
  • 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 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 sequesterants that also help to lower lipids. These medicines work in a different way and have a complementary effect to ezetimibe.
  • 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.
  • 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.
  • No dosage adjustments are recommended for people with kidney disease, mild liver disease or due to advanced age; however, ezetimibe is not recommended in people with moderate to severe liver disease. Studies have not shown an increase in liver enzymes when ezetimibe is used alone (without a statin). A greater sensitivity of some older individuals cannot be ruled out
  • Ezetimibe has not been shown to result in changes in blood pressure.
  • Ezetimibe can also be found in combination products that may be more convenient. For example, Vytorin (ezetimibe and simvastatin) and Roszet (ezetimibe and rosuvastatin) are brand name products that contain both ezetimibe and a statin. These brands are also available as lower cost generics.
  • 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.

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 and feeling tired when ezetimibe if used alone. When ezetimibe is used with a statin, side effects may include common cold symptoms, muscle aches, upper respiratory tract infection, joint pain and diarrhea.
  • 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.
  • Ezetimibe has not been shown to prevent heart disease or heart attacks.
  • Rarely, severe muscle pain may occur, if ezetimibe is used alone or combined with a statin. This may include cases of myopathy and rhabdomyolysis. Contact your doctor right away if you have severe muscle pain, tenderness, or weakness, which may lead to muscle breakdown and kidney damage.
  • If you have active liver disease, you may not be able to use ezetimibe alone. Your doctor will monitor your liver function.
  • 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.
  • Serious allergic reactions can happen in some people. Signs of an allergic reaction may include: rash or hives; swelling of the face, lips, tongue, and/or throat that may cause trouble breathing or swallowing; joint pain and muscle aches; changes in laboratory tests; liver problems; stomach pain; inflammation of the pancreas; nausea; dizziness; tingling sensation; depression; headache; gallstones; inflammation of the gallbladder.
  • If you have active liver disease, are pregnant or plan to become pregnant or are breastfeeding, you cannot use ezetimibe with a statin. Talk to your doctor about whether ezetimibe is right for you.
  • It is unknown if Zetia is effective for Fredrickson Type I, III, IV, and V dyslipidemias.
  • Zetia has not been studied in children under the age of 10.

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 a statin or fenofibrate in some patients to further reduce lipids. Ezetimibe is usually well-tolerated, but its use may be limited by 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.
  • Take your medicine exactly as directed by your doctor. Do not change your dose or stop treatment unless recommended by your doctor.
  • 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.
  • 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.
  • 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.
  • 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 stop using any medications without first talking to your doctor.

6. Response and effectiveness

Ezetimibe (Zetia) 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).

  • 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%.
  • In a clinical study, when ezetimibe was used with atorvastatin (a statin) at the beginning of treatment, LDL cholesterol levels were reduced by 54%.
  • When ezetimibe was combined with fenofibrate in patients mixed hyperlipidemia in a 12-week study, LDL-C was significantly reduced by 20%, compared to a 6% reduction when taking fenofibrate alone, a 13% reduction when taking ezetimibe alone, or 0% when taking a placebo.
  • Ezetimibe has also been shown to significantly lower LDL-C levels in patients with Homozygous Familial Hypercholesterolemia (HoFH) also taking a statin.
  • In patients with Homozygous Sitosterolemia (Phytosterolemia) and continuing their current therapeutic regimen (which may include diet, bile-acid-binding resins, statins, ileal bypass surgery and/or LDL apheresis), ezetimibe significantly lowered plasma sitosterol and campesterol, by 21% and 24% from baseline, respectively. However, patients who received placebo 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. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor or pharmacist about how drug interactions should be managed.

  • Bile acid sequestrants: Take ezetimibe either 2 hours before or 4 hours after taking a bile acid sequestrant (such as cholestyramine). Taking these medicines at the same time may reduce the absorption and effectiveness of ezetimibe.
  • Cyclosporine: Combining ezetimibe with cyclosporine may increase the blood levels of both ezetimibe and cyclosporine and worsen side effects for one or both drugs. Speak to your doctor before you combine these two medicines. Your blood levels of cyclosporine may need to be monitored. Fenofibrate: Combined use may lead to increased blood levels of ezetimibe. Both medicines can be harmful to the gallbladder, and these effects are increased when the medications are used together. Fibrates may increase cholesterol excretion into the bile, leading to cholesterol gallstones. Symptoms of gallbladder side effects include severe stomach pain, nausea, vomiting, unusual weakness, or fever. Contact your doctor if you experience these side effects. You may need a special gallbladder study and / or a change in medicine.
  • Fibrates: Coadministration of ezetimibe with fibrates other than fenofibrate is not recommended until further studies are completed.
  • Statins: Additional serious interactions, including liver disease and severe muscle problems (rhabdomyolysis) may occur if ezetimibe is combined with other medicines like a statin.
  • Warfarin: If you take the blood thinner warfarin and ezetimibe, your doctor will monitor your INR closely.

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.

References

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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