Ezetimibe

( Zetia )

Medically Reviewed by HaVy Ngo, Pharm.D.

Last Reviewed: Jun 07, 2022

Warnings


What are the risks of taking ezetimibe (Zetia)?



Ezetimibe can cause serious health problems in certain groups of people. You should talk to your healthcare provider if you have any concerns or other treatment options.

If you take ezetimibe with a statin or fenofibrate, you should follow your doctor’s instructions to avoid adverse effects and complications.

Other risks of ezetimibe use include:
  • Elevated liver enzymes:
    Risk factor: Taking ezetimibe and a statin together; history of liver disease.

    Clinical studies showed that taking ezetimibe and statin together can raise liver enzymes. However, those patients with elevated liver enzymes did not show any symptoms, and the liver enzymes returned to normal regardless of discontinuation of therapy. If your doctor prescribes ezetimibe and a statin for you, liver function tests are ordered before starting treatment. If your liver enzymes increase 3 folds from the normal limit, discontinuation of therapy is recommended. 

  • Myopathy/Rhabdomyolysis (the breaking down of muscle tissue):
    Risk factors: Taking ezetimibe and a statin together; taking high-dose statin; history or current kidney disease; being elderly; being a female.

  • Ezetimibe can cause the breaking down of the muscle tissue leading to kidney injury. This condition is rare but serious. The risk increases if you take a high-dose statin or have a history of renal impairment. Older age also increases the risk of this condition. Inform your healthcare professional immediately if you notice unusual muscle pain, tenderness, unexplained weakness, fever, and dark urine. 

  • Liver problems: 
    Risk factors: History of liver problems; active liver disease 
    If you have moderate to severe liver disease, ezetimibe is not a safe choice for you

Speak to your doctor or pharmacist about other treatment options if you are at high risk for the above complications.


What should I tell my doctor before starting ezetimibe (Zetia)?

You should not take ezetimibe if you have had an allergic reaction to ezetimibe to Zetia. Hypersensitivity reactions to ezetimibe can be mild to severe, including skin hives, rash, swelling of the throat, tongue, causing trouble breathing. You should seek medical help immediately if you experience any of these symptoms. 

You should not take ezetimibe if you have moderate to severe liver disease.

Ezetimibe is not indicated to be used for children under the age of 10 or girls who have not started their menstrual periods. 

Often, ezetimibe is used as a monotherapy (being used alone) or in combination with a statin such as atorvastatin, rosuvastatin, or lovastatin. You should not use this combination if you have:

  • Active liver disease
  • You are pregnant
  • You are breastfeeding 


Before taking ezetimibe, you should inform your healthcare provider of your complete medical history, especially if you have:

  • Liver disease
  • Kidney disease
  • Thyroid problems


Tell your doctor if you are pregnant. Ezetimibe is a pregnancy category C drug; there are no adequate and well-controlled studies of ezetimibe in pregnant women. Ezetimibe should be used during pregnancy only if the potential benefits justify the risk to the fetus, with your doctor’s approval. Keep in mind that all statins are contraindicated in pregnant women and nursing mothers.  

Women of childbearing age should use a reliable form of birth control if they use ezetimibe with a statin medicine.

Tell your doctor if you are breastfeeding. It is unknown whether this drug passes into human breast milk. Talk to your doctor if you are a nursing mother. You may have to decide whether to stop nursing or stop using ezetimibe. 

What precautions should I take while on ezetimibe? (Zetia)?

If you are taking colesevelam (Wellchol), cholestyramine (Questran), or colestipol (Colestid), you should take ezetimibe at least 2 hours before or 4 hours after the administration of these bile acid sequestrants. 

Ezetimibe can cause myopathy or rhabdomyolysis, which are serious muscle problems. Your healthcare provider will check your blood cholesterol and the effects of this medication at regular visits. You should keep all blood tests and doctor appointments. 

A reliable method of birth control must be used by women of childbearing age if using ezetimibe and a statin together. 

What drugs can interact with ezetimibe? (Zetia)?

Take ezetimibe 2 hours before or 4 hours after taking colesevelam (Wellchol), cholestyramine (Questran), or colestipol (Colestid). These bile acid sequestrants can decrease the amount of ezetimibe in your body, causing ezetimibe to be less effective.

Tell your doctor about other drugs you are taking, especially:

  • Cyclosporine - drug interactions between cyclosporine and ezetimibe increase the levels of both drugs in your body.
  • Fenofibric acid, gemfibrozil - these drugs may cause gallstones when taken with ezetimibe. 
  • A blood thinner such as warfarin (Coumadin, Jantoven) - ezetimibe can affect the effectiveness of warfarin. Your doctor will monitor you closely if you take a blood thinner with ezetimibe.


This is not a complete list. Other drugs, including prescription drugs, over-the-counter products, herbal supplements, and vitamins, may have possible drug interactions with ezetimibe. Not all potential drug interactions are listed in this guide. It is highly recommended to keep a list of all the drug products you are using (prescriptions, over-the-counter products, herbal supplements, natural products, and vitamins) and share it with your doctor and pharmacist.