Cholesterol Absorption Inhibitors for High Cholesterol

Example(s): Zetia (ezetimibe)

Cholesterol Absorption Inhibitors for High Cholesterol


Generic Name Brand Name
ezetimibe Zetia

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 in people who cannot take a statin. This medicine lowers total cholesterol and LDL
(bad) cholesterol.

This medicine is used along with lifestyle
changes including diet and exercise to lower cholesterol.

How Well It Works

Ezetimibe (Zetia) lowers total
cholesterol and LDL cholesterol levels in people who have high cholesterol. This medicine can improve cholesterol levels, but it has not been proved to lower the risk of a heart attack or a stroke.

A drug that combines ezetimibe and simvastatin (Vytorin) lowers total
cholesterol and LDL levels. But taking Vytorin may
not limit hardening of the arteries (atherosclerosis) any better than the statin medicine
alone. But the combination of
ezetimibe and simvastatin can lower LDL levels more than simvastatin
alone.footnote 1

Side Effects

All medicines have side effects. But many people don’t feel the side effects, or they are able to deal with them. Ask your pharmacist about the side effects of each medicine you take. Side effects are also listed in the information that comes with your medicine.

Here are some important things to think about:

  • Usually the benefits of the medicine are more important than any minor side effects.
  • Side effects may go away after you take the medicine for a while.
  • If side effects still bother you and you wonder if you should keep taking the medicine, call your doctor. He or she may be able to lower your dose or change your medicine. Do not suddenly quit taking your medicine unless your doctor tells you to.

Call 911 or other emergency services right away if you have:

  • Trouble breathing.
  • Swelling of your face, lips, tongue, or throat.

Call your doctor right away if you have:

  • Hives.
  • Unexplained muscle pain, tenderness, or weakness.
  • Dark-colored urine.

Common side effects of this medicine include:

  • Stomach ache.
  • Diarrhea.
  • Tiredness.
  • Headache.

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

What To Think About

Before taking this medicine, tell your doctor all of
the medicines you are taking, including
over-the-counter medicines, vitamins, or supplements.

A heart-healthy lifestyle is important for lowering your risk whether you take medicine or not. This includes eating healthy foods, being active, staying at a healthy weight, and not smoking.

Taking medicine

Medicine is one of the many tools your doctor has to treat a health problem. Taking medicine as your doctor suggests will improve your health and may prevent future problems. If you don’t take your medicines properly, you may be putting your health (and perhaps your life) at risk.

Advice for women

Do not use this medicine if you are pregnant or planning to get pregnant. If you need to take this medicine, talk to your doctor about how you can prevent pregnancy.

If you are breastfeeding, talk to your doctor before using ezetimibe. Do not use ezetimibe and a statin if you are breastfeeding.


You will have regular doctor
visits and tests to check your cholesterol level and to check for side effects.

Follow-up care is a key part of your treatment and safety. Be sure to make and go to all appointments, and call your doctor if you are having problems. It’s also a good idea to know your test results and keep a list of the medicines you take.

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.


ByHealthwise StaffPrimary Medical Reviewer Kathleen Romito, MD – Family Medicine Martin J. Gabica, MD – Family Medicine Specialist Medical Reviewer Adam Husney, MD – Family Medicine

Current as ofOctober 5, 2017