Cholesterol absorption inhibitors for high cholesterol


Generic Name Brand Name
ezetimibe Zetia
ezetimibe and simvastatin Vytorin

How It Works

Cholesterol absorption inhibitors lower the amount of cholesterol that your body absorbs. So your blood has lower total cholesterol and lower LDL (bad) cholesterol.

Why It Is Used

Cholesterol absorption inhibitors are used to treat high cholesterol. This medicine lowers total cholesterol and LDL (bad) cholesterol.

This medicine is used along with lifestyle changes including diet and exercise to lower cholesterol. It can be used alone or taken with a statin or other cholesterol-lowering medicines. One medicine, Vytorin, is a combination of a cholesterol absorption inhibitor and a statin.

How Well It Works

Ezetimibe (Zetia) lowers total cholesterol and LDL cholesterol levels in people with high cholesterol.

A drug that combines ezetimibe and simvastatin (Vytorin) lowers total cholesterol and LDL levels. But a recent study showed that taking Vytorin may not limit hardening of the arteries (atherosclerosis) any better than the statin medicine alone, based on one way to measure atherosclerosis. But the combination of ezetimibe and simvastatin can lower LDL levels more than simvastatin alone.1 If you are taking Vytorin, or you are taking Zetia and a statin as separate pills, you may want to talk to your doctor before your next refill about switching to simvastatin alone. Because you can buy a generic version of simvastatin or other statin medicines, taking the statin alone can save you money.

Side Effects

Side effects of cholesterol absorption inhibitors may include:

  • Stomach ache.
  • Tiredness.
  • Allergic reactions.
  • Cold symptoms, such as a sore throat or runny nose.
  • Dizziness.
  • Headache.
  • Joint pain.

Serious, but uncommon side effects, include:

  • Muscle pain or weakness.
  • Chest pain.
  • Severe stomach pain or nausea.
  • Fever.
  • Dark urine.
  • Loss of appetite.
  • Yellowing of the skin.

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

If you have liver disease, do not take a cholesterol absorption inhibitor with a statin.

If you also take bile acid sequestrants (cholestyramine, colestipol, and colesevelam) for high cholesterol, do not take them at the same time as a cholesterol absorption inhibitor. Instead, take your cholesterol absorption inhibitor either 2 hours before or 4 hours after the bile acid sequestrant.

If you also take a statin, you can take a cholesterol absorption inhibitor at the same time as the statin.

Before taking this medicine, tell your doctor all of the medicines you are taking, including nonprescription medicines. Be sure to mention any of the following: anticoagulants (such as warfarin), cyclosporine, or a fibric acid derivative (fenofibrate or gemfibrozil).

Do not take this medicine if you are pregnant or breast-feeding.

You can take this medicine with or without food.

You will have regular doctor visits and tests to check for side effects, including side effects to your liver.

Complete the new medication information form (PDF)(What is a PDF document?) to help you understand this medication.



  1. Kastelein JJP, et al. (2008). Simvastatin with or without ezetimibe in familial hypercholesterolemia. New England Journal of Medicine, 358(14): 1431–1443.

Last Updated: July 11, 2008

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