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Zetia

Generic name: ezetimibeez-ET-i-mibe ]
Drug class: Cholesterol absorption inhibitors

Medically reviewed by Melisa Puckey, BPharm. Last updated on Mar 1, 2024.

What is Zetia?

Zetia reduces the level of total cholesterol and LDL (bad) cholesterol in the blood. Zetia is used to treat high cholesterol in people who cannot control their cholesterol levels by diet and exercise alone.

Zetia works to reduce the amount of cholesterol your body absorbs. You should stay on a cholesterol-lowering diet while taking this medicine.

Zetia is sometimes given together with other cholesterol-lowering medications, including fenofibrate, or a statin medication such as atorvastatin, lovastatin, simvastatin, pravastatin, or fluvastatin. You should not use Zetia with a "statin" cholesterol medicine if you have active liver disease or if you are pregnant or breastfeeding a baby.

Warnings

Zetia is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

Some cholesterol medications should not be taken at the same time. If you take Zetia with another cholesterol medicine, follow your doctor's dosing instructions very carefully.

You should not use Zetia if you have moderate to severe liver disease. You should not use Zetia together with a "statin" cholesterol medicine if you have active liver disease or if you are pregnant or breast-feeding a baby.

Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Before taking this medicine

You should not use Zetia if you are allergic to ezetimibe, or if you have:

Zetia is not approved for use by anyone younger than 10 years old.

You should not use Zetia with a "statin" cholesterol medicine (Zocor, Lipitor, Crestor, and others) if:

Statin cholesterol medications can cause the breakdown of muscle tissue, which can lead to kidney failure. This happens more often in women, in older adults, or people who have kidney disease or poorly controlled hypothyroidism (underactive thyroid).

To make sure Zetia is safe for you, tell your doctor if you have:

Tell your doctor if you are pregnant or breastfeeding.

Use effective birth control to prevent pregnancy while you are using Zetia with a statin medicine. Tell your doctor if you plan to become pregnant.

Do not breastfeed if you take Zetia with a statin medicine.

How should I take Zetia?

Take Zetia exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Zetia is usually taken once daily at the same time each day.

You may take Zetia with or without food.

Zetia may be taken at the same time with fenofibrate, or with a statin medication such as atorvastatin, lovastatin, simvastatin, pravastatin, or fluvastatin.  You should not take Zetia together with a statin medicine if you have active liver disease or if you are pregnant or breastfeeding a baby.

Your treatment may also include diet, exercise, weight control, and blood tests.

You may need frequent medical tests, even if you have no symptoms.

Your cholesterol levels may not improve for up to 2 weeks.

Store at room temperature away from moisture and heat.

Dosing information

Usual Adult Dose of Zetia for Hyperlipidemia:

10 mg orally once a day

Uses:
-For use as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin) as an adjunct to diet to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin to reduce elevated total-C and LDL-C levels in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

Usual Adult Dose of Zetia for Homozygous Familial Hypercholesterolemia:

10 mg orally once a day

Uses:
-For use as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin) as an adjunct to diet to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin to reduce elevated total-C and LDL-C levels in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

Usual Adult Dose of Zetia for Sitosterolemia:

10 mg orally once a day

Uses:
-For use as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin) as an adjunct to diet to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin to reduce elevated total-C and LDL-C levels in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

Usual Pediatric Dose for Hyperlipidemia:

10 years or older: 10 mg orally once a day

Uses:
-For use as monotherapy or in combination with a statin as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with a fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin for the reduction of elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

Usual Pediatric Dose for Homozygous Familial Hypercholesterolemia:

10 years or older: 10 mg orally once a day

Uses:
-For use as monotherapy or in combination with a statin as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with a fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin for the reduction of elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

Usual Pediatric Dose for Sitosterolemia:

10 years or older: 10 mg orally once a day

Uses:
-For use as monotherapy or in combination with a statin as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary (heterozygous familial and non-familial) hyperlipidemia
-For use as combination therapy with a fenofibrate as an adjunct to diet to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia
-As an adjunct to diet to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia
-For use as combination therapy with atorvastatin or simvastatin for the reduction of elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Zetia?

Avoid eating foods high in fat or cholesterol, or Zetia will not be as effective.

Zetia side effects

Get emergency medical help if you have signs of an allergic reaction to Zetia: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Zetia can cause the breakdown of muscle tissue, which can lead to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, or dark urine.

Side effects may be more likely in older adults.

Common side effects of Zetia may include:

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Zetia?

If you also take other cholesterol medication: Take Zetia 2 hours before or 4 hours after taking cholestyramine, colestipol, or colesevelam.

Tell your doctor about all your other medicines, especially:

This list is not complete. Other drugs may interact with ezetimibe, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Popular FAQ

No, Zetia is not a statin drug. Zetia reduces blood cholesterol in a different way to statin medications. Zetia lowers cholesterol levels by decreasing the amount of cholesterol that is absorbed from the small intestine, so that there is less intestinal cholesterol delivered to the liver. Continue reading

Memory loss is not a side effect of Zetia (ezetimibe) when it is used alone to treat high cholesterol. Zetia is often used with diet and other cholesterol lowering medications like statins which have been linked with cognitive impairment (memory loss, forgetfulness, or confusion). Continue reading

Yes, Zetia (ezetimibe) can cause liver damage, although it is very rare. Monitor liver enzymes for the development of serious toxic hepatitis and consider ezetimibe discontinuation if it develops. Perform liver tests during ezetimibe initiation and regularly thereafter and consider withdrawal of ezetimibe and/or the statin (if coadministered) should an increase in ALT or AST ≥3 X upper limit of normal (ULN) persist. Continue reading

It reduces cholesterol absorption from the small intestine so there is less cholesterol delivered to the liver. This means there is a lower amount of cholesterol stored in the liver, which leads to more cholesterol being cleared from the blood. Continue reading

More FAQ

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Further information

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

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