Zetia is a brand-name prescription drug. It’s FDA-approved to treat certain forms of high cholesterol in adults and in children ages 10 years and older.

Specifically, Zetia is used along with a low-cholesterol diet to treat:

  • Primary hyperlipidemia. Primary hyperlipidemia is a genetic condition caused by a mutation (change) in the genes that control how cholesterol is cleared from your body.
  • Mixed hyperlipidemia. Mixed hyperlipidemia is a genetic condition caused by a mutation in the genes that control how cholesterol and triglycerides are cleared from your body.
  • Homozygous familial hypercholesterolemia (HoFH). HoFH is a rare genetic condition caused by a mutation in the genes that control how cholesterol is cleared from your body.
  • Homozygous sitosterolemia. Homozygous sitosterolemia is a genetic condition caused by a mutation in the genes that control how plant sterols are cleared from your body. (Plant sterols are a type of fat found in nuts, vegetable oils, and other plant-based foods.)

Zetia is approved to treat these conditions in certain situations. For more information about how the drug is used, see the “Zetia uses” section below.

Zetia drug class and form

Zetia contains the active drug ezetimibe. It belongs to a class of drugs called cholesterol absorption inhibitors. Drugs in this class prevent your small intestine from absorbing cholesterol. For more information, see the “How Zetia works” section below.

Zetia comes as a tablet that you swallow. You’ll likely take it once a day. You can take Zetia with or without food.

Effectiveness

For information on the effectiveness of Zetia, see the “Zetia uses” section below.

Zetia is a brand-name drug that contains the active drug ezetimibe. This active drug is also available as a generic medication. A generic drug is an exact copy of the active drug in a brand-name medication. The generic is considered to be as safe and effective as the original drug. Generics tend to cost less than brand-name drugs.

Zetia can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Zetia. These lists don’t include all possible side effects.

For more information on the possible side effects of Zetia, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome.

Note: The Food and Drug Administration (FDA) tracks side effects of drugs it has approved. If you would like to report to the FDA a side effect you’ve had with Zetia, you can do so through MedWatch.

Mild side effects

Mild side effects of Zetia can include:*

Most of these side effects may go away within a few days or a couple of weeks. But if they become more severe or don’t go away, talk with your doctor or pharmacist.

* This is a partial list of mild side effects from Zetia. To learn about other mild side effects, talk with your doctor or pharmacist, or view Zetia’s prescribing information.
† For more information on these side effects, see “Side effect details” below.

Serious side effects

Serious side effects from Zetia aren’t common, but they can occur. Call your doctor right away if you have serious side effects. Call 911 or your local emergency number if your symptoms feel life threatening or if you think you’re having a medical emergency.

Serious side effects and their symptoms can include:

  • High levels of liver transaminases.* Transaminases are a type of liver enzyme. If you have high levels of liver enzymes, your liver may not be working correctly. You may not have any symptoms of high liver enzymes unless you have more serious liver disease. Symptoms of liver disease can include:
    • abdominal (belly) pain
    • bruising more easily than usual
    • dark-colored urine
    • pale-colored stool
    • decreased appetite
    • itching
    • jaundice (yellowing of your skin or the whites of your eyes)
    • swollen ankles or legs
    • fatigue (lack of energy)
  • Allergic reaction.
  • Muscle problems.

* You may be more likely to experience this side effect if you take Zetia with a statin drug than if you take Zetia alone.
† For more information on these side effects, see “Side effect details” below.

Side effects in children

Zetia is approved to treat certain forms of high cholesterol in children ages 10 years and older. The side effects of Zetia in children are similar to the side effects in adults. See the “Mild side effects” and “Serious side effects” sections above for more information.

Side effect details

You may wonder how often certain side effects occur with this drug, or whether certain side effects pertain to it. Here’s some detail on certain side effects this drug may or may not cause.

Allergic reaction

As with most drugs, some people can have an allergic reaction after taking Zetia. It isn’t known how often this side effect occurred with Zetia in clinical studies.

Symptoms of a mild allergic reaction can include:

  • skin rash
  • itchiness
  • flushing (warmth and redness in your skin)

A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:

  • swelling under your skin, typically in your eyelids, lips, hands, or feet
  • swelling of your tongue, mouth, or throat
  • trouble breathing

Call your doctor right away if you have a severe allergic reaction to Zetia. Call 911 or your local emergency number if your symptoms feel life threatening or if you think you’re having a medical emergency.

Joint pain

Zetia may cause joint pain. Clinical studies looked at Zetia for the treatment of primary hyperlipidemia in adults and in children ages 10 years and older.

Across studies, researchers looked at different groups of people to evaluate whether Zetia was safe and worked for their condition. In these groups, joint pain occurred in:

  • 3% of people who took Zetia alone
  • 2.6% of people who took Zetia with a statin drug
  • 2.4% of people who took a statin drug alone
  • 2.2% of people who took a placebo (treatment with no active drug)

The length of time that adults and children experienced joint pain while taking Zetia in these clinical studies isn’t known. However, 0.3% of people who took Zetia alone experienced joint pain so bothersome that they had to stop treatment.

It also isn’t known how many adults and children experienced joint pain in clinical studies of Zetia used to treat other conditions.

Symptoms that occur with joint pain

If you have joint pain while taking Zetia, you may also experience swelling, redness, or weakness in your joints. Talk with your doctor right away if you have fever or chills with your joint pain. These symptoms can be signs of an infection.

If you’re concerned about joint pain while using Zetia, talk with your doctor. They can recommend treatments that may help with joint pain, or they may recommend a different treatment option for you.

Diarrhea

Diarrhea is a common side effect of Zetia. Clinical studies involved adults and children ages 10 years and older. Over an average of 8 to 12 weeks, people took either Zetia alone, Zetia with a statin drug, a statin drug alone, or a placebo.

Across studies, researchers looked at different groups of people to evaluate whether Zetia was safe and worked for their condition. In these groups, joint pain occurred in:

  • 4.1% of people who took Zetia alone
  • 2.5% of people who took Zetia with a statin drug
  • 2.2% of people who took a statin drug alone
  • 3.7% of people who took a placebo

It isn’t known how long adults and children experienced diarrhea while taking Zetia in these clinical studies. It also isn’t known what percentage of adults and children experienced diarrhea in clinical studies of other conditions treated with Zetia.

Talk with your doctor if you experience diarrhea while taking this medication. They can suggest ways to help relieve this side effect.

Muscle problems

You may experience muscle problems as a side effect of Zetia. These problems can include muscle pain and muscle weakness, and rarely, muscle breakdown. You may also have muscle cramps, spasms, or stiffness.

Muscle problems were reported in clinical studies of adults and children who took Zetia with statin drugs. However, you may still experience muscle problems if you use Zetia alone.

Muscle pain

In clinical studies of Zetia used with statin drugs to treat primary hyperlipidemia in adults and in children ages 10 years and older:

  • 3.2% of adults and children who took Zetia with a statin drug experienced muscle pain
  • 2.7% of adults and children who took a statin drug alone experienced muscle pain

It isn’t known how long adults and children experienced muscle pain while taking Zetia with statin drugs in these clinical studies. However, 0.5% of adults and children who took Zetia with a statin drug experienced muscle pain so bothersome that they had to stop treatment.

It’s not known how many adults and children experienced muscle pain in clinical studies of other conditions treated with Zetia and statin drugs. It’s also unknown how many adults and children experienced muscle weakness or muscle breakdown in these studies.

Muscle breakdown

While taking Zetia, tell your doctor right away if you experience extreme muscle pain, muscle tenderness, or dark-colored urine. These can be signs of rhabdomyolysis (muscle breakdown), which is a serious medical condition. If left untreated, it can cause your kidneys to stop working properly.

Rhabdomyolysis can also occur with statin drugs, and you may need to take Zetia with a statin.

Depending on your age or other medical conditions you may have, you may be at higher risk of developing rhabdomyolysis while taking Zetia. People who may be at higher risk of this side effect include those who:

  • are older than age 65 years
  • are taking a statin, especially a high-dose statin
  • have low levels of thyroid hormones (hypothyroidism)
  • have kidney disease
  • are taking other drugs that increase the risk of rhabdomyolysis

Tell your doctor if any of the above apply to you before starting Zetia treatment. These conditions can raise your risk of muscle problems while taking Zetia.

Memory loss (not a side effect)

Memory loss isn’t a side effect of Zetia. However, some people have reported experiencing memory loss when taking statin drugs. Statins are cholesterol drugs that may be taken with Zetia.

Talk with your doctor if you’re concerned about your risk of memory loss while using Zetia alone or with a statin drug.

Weight gain (not a side effect)

Weight gain isn’t a side effect reported in clinical studies of Zetia. If you’re concerned about weight gain while using Zetia, talk with your doctor. They may suggest foods that can help lower your cholesterol and reduce your risk of weight gain.

Your doctor will likely start you on the typical dosage approved to treat your condition. Then they’ll monitor whether the drug is working for you and whether you experience any side effects. Your doctor may stop your Zetia treatment if it isn’t safe or effective for you. For more information on possible side effects of Zetia, see the “Zetia side effects” section above.

The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to fit your needs.

Drug forms and strengths

Zetia comes as a tablet that you swallow. It’s available in a strength of 10 mg.

Dosage for high cholesterol

Zetia is approved to treat certain forms of high cholesterol in adults when used with a low-cholesterol diet. For this purpose, Zetia may be used:

The only FDA-approved dosage of Zetia is 10 mg once a day. The dosage is the same for all approved uses. You can take Zetia with or without food.

Pediatric dosage

Zetia is approved to treat certain forms of high cholesterol in children ages 10 years and older when used with a low-cholesterol diet.

The dose of Zetia used for children is the same as the adult dose. The only FDA-approved dosage of Zetia for children is 10 mg once a day. Your child can take Zetia with or without food.

What if I miss a dose?

If you miss a dose of Zetia, you can take your missed dose as soon as you remember. However, skip your missed dose if it’s almost time for your next dose. Don’t take an extra dose to make up for your missed dose. Doing this can raise your risk of side effects. (For information on side effects, see the “Zetia side effects” section above.)

To help make sure you don’t miss a dose, try setting a reminder on your phone. A medication timer may be useful, too.

Will I need to use this drug long term?

Zetia is meant to be used as a long-term treatment. If you and your doctor determine that Zetia is safe and effective for you, you’ll likely take it long term.

The Food and Drug Administration (FDA) approves prescription drugs such as Zetia to treat certain conditions. Zetia may also be used off-label for other conditions. Off-label use is when a drug that’s approved to treat one condition is used to treat a different condition.

Zetia is FDA-approved to treat certain forms of high cholesterol in adults and children. Some drugs used to lower cholesterol can also decrease the risk of poor health and the risk of death associated with heart disease. However, it isn’t known how Zetia may affect these risks.

Note: Zetia isn’t approved to lower these types of cholesterol:

  • Chylomicrons, also known as ultra low-density lipoprotein or ULDL cholesterol. Chylomicrons help your body digest fat.
  • Very low-density lipoprotein (VLDL) cholesterol. VLDL cholesterol helps move triglycerides throughout your body.

About cholesterol

Cholesterol is measured in several ways. “Total cholesterol” is the overall amount of cholesterol found in your blood. Total cholesterol consists of:

  • low-density lipoproteins (LDL), sometimes referred to as “bad cholesterol”
  • high-density lipoproteins (HDL), sometimes referred to as “good cholesterol”
  • triglycerides, which are a type of fat that are “building blocks” of cholesterol

High cholesterol occurs when you have more cholesterol in your blood than your body needs. High cholesterol may be caused by genetics, smoking, low amounts of physical activity, or eating too many high-cholesterol foods.

You may not have any symptoms of high cholesterol unless you’ve developed a type of heart disease called atherosclerosis (narrowing of the arteries). Symptoms of atherosclerosis may include confusion, fatigue (lack of energy), trouble breathing, or pain in your chest, arms, or legs.

Zetia is approved to treat different types of high cholesterol. Each type is described below in more detail. To determine whether you have high cholesterol, your doctor will do a blood test called a lipid panel.

Zetia for primary high cholesterol

Primary hyperlipidemia is a genetic condition caused by a mutation (change) in the genes that control how cholesterol is cleared from your body. (Primary hyperlipidemia is also called primary high cholesterol.) People with this condition have high levels of LDL (“bad”) cholesterol.

For primary high cholesterol, Zetia is FDA-approved for use in adults and children to decrease levels of:

  • total cholesterol
  • LDL cholesterol
  • Apo B (high levels of this protein are a sign of high cholesterol)
  • non-HDL cholesterol (calculated by subtracting your HDL cholesterol level from your total cholesterol)

For this purpose, Zetia is used with a low-cholesterol diet. Zetia can also be used with statin drugs in adults. Statins are another type of medication used to lower cholesterol.

Effectiveness for primary high cholesterol

Clinical studies have shown Zetia to be effective for treating primary high cholesterol when used alone or with statin drugs.

Zetia compared with a placebo

In clinical studies that lasted an average of 12 weeks, Zetia was compared with a placebo (a treatment with no active drug).

In the studies, total cholesterol levels:

  • were reduced by an average of 13% to 14% in people who used Zetia
  • ranged from not changing to being reduced by an average of 1% in people who used a placebo

LDL (“bad”) cholesterol levels:

  • were reduced by an average of 18% in people who used Zetia
  • increased by an average of 1% in people who used a placebo

To learn how Zetia and the placebo affected people’s levels of HDL (“good”) cholesterol, triglycerides, non-HDL cholesterol, and Apo B, see the prescribing information.

Zetia used with statin drugs

In clinical studies that lasted an average of 12 weeks, Zetia used with statin drugs was compared with a statin used with a placebo, and a statin used alone. Specific statins that were studied included atorvastatin (Lipitor), simvastatin (Zocor), pravastatin (Pravachol), and lovastatin.

In the studies, total cholesterol levels:

  • decreased by an average of 13% to 14% in people who used Zetia alone
  • decreased by an average of 15% to 40% in people who used a statin alone, depending on the statin used
  • decreased by an average of 24% to 46% in people who used Zetia and a statin, depending on the statin used
  • ranged from decreasing by an average to 1% to increasing by an average of 4% in people who took a placebo

And, LDL (“bad”) cholesterol levels:

  • decreased by an average of 19% to 20% in people who used Zetia alone
  • decreased by an average of 20% to 54% in people who used a statin alone, depending on the statin used
  • decreased by an average of 34% to 61% in people who used Zetia and a statin, depending on the statin used
  • ranged from decreasing by an average to 1% to increasing by an average of 4% in people who took a placebo

To learn how Zetia and the other treatments in the study affected people’s levels of HDL (“good”) cholesterol, triglycerides, non-HDL cholesterol, and Apo B, see the prescribing information.

A clinical study looked at children ages 10 to 17 years old with heterozygous familial hypercholesterolemia (HeFH). The children took Zetia and simvastatin or simvastatin alone. At the end of the study, researchers found that:

  • Total cholesterol was reduced by 12% more in children who took Zetia and simvastatin than children who took simvastatin alone.
  • LDL cholesterol was reduced by 15% more in children who took Zetia and simvastatin than in children who took simvastatin alone.

Zetia for mixed high cholesterol

Mixed hyperlipidemia is a genetic condition caused by a mutation (change) in the genes that control how cholesterol and fats are cleared from your body. (Mixed hyperlipidemia is also known as mixed high cholesterol.)

People with this condition have high levels of LDL (“bad”) cholesterol, high levels of triglycerides, and low levels of HDL (“good”) cholesterol.

For mixed high cholesterol, Zetia is FDA-approved to decrease levels of:

  • total cholesterol
  • LDL cholesterol
  • Apo B (high levels of this protein are a sign of high cholesterol)
  • non-HDL cholesterol (calculated by subtracting your HDL cholesterol level from your total cholesterol)

For this purpose, Zetia is used with a low-cholesterol diet and is taken with other drugs. It can be taken with or without fenofibrate in adults. (Fenofibrate is a drug used to lower your triglyceride levels.)

Effectiveness for mixed high cholesterol

In clinical studies, Zetia has been found to be effective for treating mixed high cholesterol when used with fenofibrate.

In these studies, 12 weeks of treatment with Zetia and fenofibrate was compared with Zetia taken alone, fenofibrate taken alone, or a placebo (a treatment with no active drug).

Total cholesterol levels were reduced by an average of:

  • 22% in people who used Zetia with fenofibrate
  • 12% in people who used Zetia alone
  • 11% in people who used fenofibrate alone
  • 0% in people who used a placebo

LDL (“bad”) cholesterol levels were reduced by an average of:

  • 20% in people who used Zetia with fenofibrate
  • 13% in people who used Zetia alone
  • 6% in people who used fenofibrate alone
  • 0% in people who used a placebo

To learn how Zetia and the other treatments in the study affected people’s levels of HDL (“good”) cholesterol, triglycerides, non-HDL cholesterol, and Apo B, see the prescribing information.

Zetia for homozygous familial hypercholesterolemia

Homozygous familial hypercholesterolemia (HoFH) is a rare genetic condition caused by a mutation (change) in the genes that control how cholesterol is cleared from your body. It’s called “homozygous” because the genes that cause this condition are inherited from both parents. People with HoFH have high levels of LDL (“bad”) cholesterol.

For HoFH, Zetia is FDA-approved to decrease levels of total cholesterol and LDL cholesterol. For this purpose, Zetia is used with a low-cholesterol diet and is taken with atorvastatin (Lipitor) or simvastatin (Zocor) in adults and in children ages 10 years and older.

Effectiveness for homozygous familial hypercholesterolemia

Clinical studies have shown Zetia to be effective for treating homozygous familial hypercholesterolemia when used with atorvastatin or simvastatin.

Twelve weeks of treatment with Zetia and atorvastatin or simvastatin was compared with atorvastatin or simvastatin used alone.

In the study:

  • people who used Zetia with atorvastatin or simvastatin had their LDL levels reduced by an average of 21% to 27% (the percentage varied depending on the dosage used)
  • people who used atorvastatin or simvastatin alone had their LDL levels reduced by an average of 7%

The effect of Zetia, atorvastatin, or simvastatin on other types of cholesterol levels in this study isn’t known.

Zetia for homozygous sitosterolemia

Homozygous sitosterolemia is a genetic condition caused by a mutation (change) in the genes that control how plant sterols are cleared from your body. Plant sterols are similar to cholesterol. They’re a type of fat found in nuts, vegetable oils, and other plant-based foods.

People with this condition have high levels of plant sterols. Over time, plant sterols can build up in your blood vessels and raise your risk of heart disease.

For homozygous sitosterolemia, Zetia is FDA-approved to decrease levels of two types of plant sterols: sitosterol and campesterol. For this purpose, Zetia is used with a low-cholesterol diet (but with no other drugs) in adults and in children ages 10 years and older.

Effectiveness for homozygous sitosterolemia

Clinical studies have shown Zetia to be effective for treating homozygous sitosterolemia when used alone.

In clinical studies that lasted 8 weeks, Zetia was compared with a placebo (a treatment with no active drug). In the studies:

  • people who used Zetia had their sitosterol levels decreased by an average of 21% and their campstrol levels decreased by an average of 24%
  • people who used a placebo had their sitosterol levels decreased by an average of 4% and their campstrol levels decreased by an average of 3%

Zetia and children

Zetia is approved to treat the following conditions in children ages 10 years and older when used with a low-cholesterol diet:

  • primary hyperlipidemia, used alone or with a statin
  • mixed hyperlipidemia, used with fenofibrate
  • homozygous familial hypercholesterolemia, used with atorvastatin or simvastatin
  • homozygous sitosterolemia

To learn more about how Zetia is used for these conditions, see the sections above.

Here are answers to some frequently asked questions about Zetia.

Is Zetia a statin?

No, Zetia isn’t a statin drug. Zetia belongs to a class of drugs called cholesterol absorption inhibitors. (A class of drugs is a group of medications that work in a similar way.) Drugs in this class prevent your small intestine from absorbing cholesterol. For more information, see the “How Zetia works” section below.

Medications in the statin drug class work differently than cholesterol absorption inhibitors like Zetia. Statins lower cholesterol by preventing your liver from making new cholesterol.

Your doctor may prescribe Zetia with a statin drug. If you have questions about the differences between Zetia and statin drugs, talk with your doctor.

Are there any foods I should avoid while taking Zetia?

Yes, there are a few. Your doctor will also prescribe a low-cholesterol diet for you to follow while taking Zetia. This means you should avoid foods that are high in cholesterol and other types of fat.

In addition, you may need to watch out for grapefruit. Zetia isn’t known to interact with grapefruit or any other foods. However, you may need to avoid grapefruit if you take Zetia with a statin, another type of cholesterol medication.

This is because it isn’t safe to eat grapefruit or drink grapefruit juice while using a statin. Grapefruit can prevent the breakdown of statins in your body, which can raise your levels of these drugs and increase your risk of side effects.

So if you’re taking Zetia with a statin drug, you may need to avoid eating grapefruit or drinking grapefruit juice during your treatment. Learn more about how grapefruit may interact with medications.

If you have any questions about eating certain foods while taking Zetia, talk with your doctor.

Does Zetia cause hair loss?

No, hair loss isn’t a known side effect of Zetia.

In fact, researchers have looked into using Zetia to treat hair loss due to a condition called alopecia areata.

If you’re experiencing hair loss while using Zetia, talk with your doctor. They may be able to help determine what’s causing your hair loss.

Will Zetia lower my triglycerides?

Yes, treatment with Zetia should lower your triglycerides. Zetia is FDA-approved to lower your total cholesterol level, and triglycerides are one part of your total cholesterol level. For this purpose, Zetia may be used alone or with fenofibrate. For more information about the effectiveness of Zetia for lowering your triglycerides, see the “Zetia uses” section above.

Talk with your doctor if you have questions about using Zetia to lower your triglyceride levels.

Does Zetia affect my blood pressure or blood sugar levels?

No, clinical studies haven’t shown Zetia to affect blood pressure. And Zetia hasn’t been shown to affect blood sugar levels in clinical studies of people with diabetes and people without diabetes.

If you have high cholesterol with hypertension (high blood pressure) or diabetes, you’ll likely have to take other drugs with Zetia to treat these conditions. Talk with your doctor if you have questions about managing your blood pressure or blood sugar while using Zetia.

Does stopping Zetia cause side effects?

No, stopping Zetia shouldn’t cause any side effects. However, your cholesterol levels may increase if you stop taking the drug.

Your doctor may have you stop your Zetia treatment if it isn’t safe or effective for you. However, you shouldn’t stop taking Zetia without first talking with your doctor.

There are no known interactions between Zetia and alcohol.

However, excessive alcohol use can damage your liver over time. If you have a history of heavy alcohol use and are taking Zetia with a statin drug, you may have a higher risk of side effects. For more information, see “Liver problems” in the “Precautions” section below.

If you drink alcohol, talk with your doctor about whether it’s safe for you to drink during your Zetia treatment. Also, if you have a history of heavy drinking or liver damage, be sure to tell your doctor before you begin taking Zetia.

Zetia can interact with several other medications. It can also interact with certain supplements as well as certain foods.

Different interactions can cause different effects. For instance, some interactions can interfere with how well a drug works. Other interactions can increase side effects or make them more severe.

Zetia and other medications

Below are medications that can interact with Zetia. This section doesn’t contain all drugs that may interact with Zetia.

Before taking Zetia, talk with your doctor and pharmacist. Tell them about all prescription, over-the-counter, and other drugs you take. Also tell them about any vitamins, herbs, and supplements you use. Sharing this information can help you avoid potential interactions.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Zetia and cyclosporine

Taking Zetia with cyclosporine (a drug that suppresses your immune system) can raise the levels of both medications in your body. This can increase your risk of side effects from either medication. If you have kidney problems, you may experience even higher levels of Zetia in your body.

If you’re currently taking cyclosporine, talk with your doctor about whether it’s safe for you to take Zetia.

Zetia and cholestyramine

Cholestyramine (Prevalite) is a drug used to treat high cholesterol. Taking Zetia with cholestyramine can decrease the amount of Zetia in your body. This can cause Zetia to be less effective. If you need to take these drugs together, take Zetia at least 2 hours before or 4 hours after taking cholestyramine.

If you have questions about using Zetia and cholestyramine together, talk with your doctor.

Zetia and the fibrate drug class

Medications in the fibrate drug class are used to treat high cholesterol. (A drug class is a group of medications that work in a similar way.) Fenofibrate belongs to the fibrate drug class. Zetia is FDA-approved to treat mixed high cholesterol when used with fenofibrate.

However, Zetia shouldn’t be used with fibrate drugs other than fenofibrate. This is because fenofibrate is the only fibrate Zetia was studied with, so it isn’t known whether Zetia and other fibrate drugs are safe to use together.

Medications in the fibrate drug class may increase the amount of cholesterol that’s stored in your gallbladder. This can cause gallstones (hardened stones in your gallbladder). Zetia may also increase the amount of cholesterol that’s stored in your gallbladder. Using Zetia with medications in the fibrate drug class raises your risk of gallstones even more.

You may not have any symptoms of gallstones unless they cause your gallbladder to swell. Symptoms of a swollen gallbladder may include:

  • back or shoulder pain
  • pain on the right side of your body, below your ribs
  • nausea and vomiting
  • sweating
  • restlessness

Tell your doctor if you experience gallstones while using Zetia with fenofibrate. They may want to select a different treatment option for you.

Zetia and warfarin

Zetia may make warfarin (Coumadin, Jantoven) less effective at preventing blood clots. If you use Zetia and warfarin together, your doctor may want to monitor you more closely during your treatment. Talk with your doctor about the risks of taking Zetia with warfarin.

Zetia and herbs and supplements

There aren’t any herbs or supplements that have been specifically reported to interact with Zetia. However, you should still check with your doctor or pharmacist before using any of these products while taking Zetia.

Zetia and foods

There aren’t any foods that have been specifically reported to interact with Zetia. This includes grapefruit and grapefruit juice. However, if you’re taking Zetia with a statin drug, you’ll need to avoid eating grapefruit or drinking grapefruit juice.

It isn’t safe to eat grapefruit or drink grapefruit juice while using statins. Grapefruit can prevent the breakdown of these drugs in your body. This can raise your levels of these drugs and increase your risk of side effects. Examples of statin drugs include:

Learn more about how grapefruit may interact with medications. And talk with your doctor if you have any questions about eating certain foods with Zetia.

Other drugs are available that can treat your conditions. Some may be a better fit for you than others. If you’re interested in finding an alternative to Zetia, talk with your doctor. They can tell you about other medications that may work well for you.

Note: Some of the drugs listed here are used off-label to treat these specific conditions. Off-label use is when a drug that’s approved to treat one condition is used to treat a different condition.

Alternatives for primary high cholesterol

Examples of other drugs that may be used to treat primary high cholesterol include:

  • alirocumab (Praluent)
  • evolocumab (Repatha)
  • statin drugs, such as atorvastatin (Lipitor), rosuvastatin (Crestor), and simvastatin (Zocor)
  • bile acid sequestrants, such as cholestyramine (Prevalite, Questran), colesevelam (Welchol), and colestipol (Colestid)

Alternatives for mixed high cholesterol

Examples of other drugs that may be used to treat mixed high cholesterol include:

  • fibrates, such as fenofibrate
  • gemfibrozil
  • statins, such as atorvastatin (Lipitor), rosuvastatin (Crestor), and simvastatin (Zocor)

Alternatives for homozygous familial hypercholesterolemia

Examples of other drugs that may be used to treat homozygous familial hypercholesterolemia include:

  • bile acid sequestrants, such as cholestyramine (Prevalite, Questran), colesevelam (Welchol), and colestipol (Colestid)
  • statins, such as atorvastatin (Lipitor), rosuvastatin (Crestor), and simvastatin (Zocor)
  • alirocumab (Praluent)
  • evolocumab (Repatha)

Alternatives for homozygous sitosterolemia

Examples of other drugs that may be used to treat homozygous sitosterolemia include:

  • bile acid sequestrants, such as cholestyramine (Prevalite, Questran), colesevelam (Welchol), and colestipol (Colestid)

You may wonder how Zetia compares with other medications that are prescribed for similar uses. Here we look at how Zetia and Lipitor are alike and different.

Ingredients

Zetia contains the active drug ezetimibe. Lipitor contains the active drug atorvastatin.

Zetia belongs to a class of drugs called cholesterol absorption inhibitors. (A class of drugs is a group of medications that work in a similar way.) Medications in this class prevent your small intestine from absorbing cholesterol.

Lipitor is part of the statin drug class. Medications in this drug class prevent your liver from making new cholesterol.

Uses

Here is a list of conditions that the Food and Drug Administration (FDA) has approved Zetia and Lipitor to treat.

  • Both Zetia and Lipitor are FDA-approved to treat the following conditions* in adults when used with a low-cholesterol diet:
  • Zetia is also FDA-approved to treat the following conditions when used with a low-cholesterol diet:
    • homozygous sitosterolemia in adults and in children ages 10 years and older
  • Lipitor is also FDA-approved for the following conditions when used with a low-cholesterol diet:
    • heart disease in adults with certain conditions (for this purpose, Lipitor is used to prevent heart disease)
    • primary dysbetalipoproteinemia in adults (a genetic condition that causes high total cholesterol, high triglycerides, and low HDL levels)

* Zetia is also approved to treat these conditions in children ages 10 years and older.

Drug forms and administration

Both Zetia and Lipitor come as tablets that are swallowed. Both drugs are typically taken once each day. They can both be taken with or without food.

Side effects and risks

Zetia and Lipitor have some similar side effects and others that vary. Below are examples of these side effects.

Mild side effects

These lists contain up to 10 of the most common mild side effects that can occur with Zetia, with Lipitor, or with both drugs (when taken individually).

Serious side effects

These lists contain examples of serious side effects that can occur with Lipitor or with both drugs (when taken individually).

Effectiveness

These drugs haven’t been directly compared in clinical studies. However, studies have found both Zetia and Lipitor to be effective for lowering cholesterol.

Costs

Zetia and Lipitor are both brand-name drugs. Zetia is also available in a generic form called ezetimibe. Lipitor is available in a generic form called atorvastatin. Brand-name medications usually cost more than generics.

According to estimates on GoodRx.com, Zetia generally costs less than Lipitor. The generic form of Zetia costs about the same as the generic form of Lipitor. The actual price you’ll pay for any of these drugs depends on your treatment plan, your insurance plan, your location, and the pharmacy you use.

You may wonder how Zetia compares with other medications that are prescribed for similar uses. Here we look at how Zetia and Crestor are alike and different.

Ingredients

Zetia contains the active drug ezetimibe. Crestor contains the active drug rosuvastatin.

Zetia belongs to a class of drugs called cholesterol absorption inhibitors. (A class of drugs is a group of medications that work in a similar way.) Medications in this class prevent your small intestine from absorbing cholesterol.

Crestor is part of the statin drug class. Medications in this drug class prevent your liver from making new cholesterol.

Uses

Here is a list of conditions that the Food and Drug Administration (FDA) has approved Zetia and Crestor to treat.

  • Both Zetia and Crestor are FDA-approved to treat the following conditions* when used with a low-cholesterol diet:
  • Zetia is also FDA-approved to treat the following conditions when used with a low-cholesterol diet:
    • homozygous sitosterolemia in adults and in children ages 10 years and older
  • Crestor is also FDA-approved for the following conditions in adults when used with a low-cholesterol diet:
    • heart disease, when certain conditions are met (for this purpose, Crestor is used to prevent heart disease)
    • primary dysbetalipoproteinemia (a genetic condition that causes high total cholesterol, high triglycerides, and low HDL levels)
    • atherosclerosis (for this purpose, Crestor is used to slow the progression of atherosclerosis)

* For these purposes, Zetia and Crestor are used to treat people of different ages. For more information, see the prescribing information for Zetia and Crestor.

Drug forms and administration

Both Zetia and Crestor come as tablets that are swallowed. Both drugs are typically taken once each day. They can both be taken with or without food.

Side effects and risks

Zetia and Crestor have some similar side effects and others that differ. Below are examples of these side effects.

Mild side effects

These lists contain up to 10 of the most common mild side effects that can occur with Zetia, with Crestor, or with both drugs (when taken individually).

Serious side effects

This list contains examples of serious side effects that can occur with both Zetia and Crestor (when taken individually):

Effectiveness

These drugs haven’t been directly compared in clinical studies. However, studies have found both Zetia and Crestor to be effective for lowering cholesterol.

Costs

Zetia and Crestor are both brand-name drugs. Zetia is also available in a generic form called ezetimibe. Crestor is available in a generic form called rosuvastatin. Brand-name medications usually cost more than generics.

According to estimates on GoodRx.com, Zetia generally costs more than Crestor. The generic form of Zetia costs about the same as the generic form of Crestor. The actual price you’ll pay for any of these drug depends on your insurance plan, your location, and the pharmacy you use.

You should take Zetia according to your doctor’s or healthcare provider’s instructions.

Zetia comes as a tablet that you swallow.

When to take

You’ll likely take Zetia once a day. You can take Zetia at any time during the day, but try to take your dose around the same time each day.

To help make sure you don’t miss a dose, try setting a reminder on your phone. A medication timer may be useful, too.

Taking Zetia with food

You can take Zetia with or without food.

Can Zetia be crushed, split, or chewed?

The manufacturer of Zetia hasn’t stated whether the tablets can be crushed, split, or chewed. Talk with your doctor or pharmacist if you have trouble swallowing Zetia tablets.

Zetia is FDA-approved to treat certain types of high cholesterol in adults and in children when used with a low-cholesterol diet. (For more information on the specific conditions Zetia can treat, see the “Zetia uses” section.)

What happens with high cholesterol

Cholesterol is a fatty substance found in the cells of your body. Cholesterol is made naturally in your liver. Cholesterol itself isn’t a harmful substance. Your body uses cholesterol to make some vitamins, hormones, and fluids that help you digest food. Cholesterol can also be found in foods such as eggs, cheese, and meat.

High cholesterol occurs when you have more cholesterol in your blood than your body needs. This may be caused by genetics, smoking, not getting enough physical activity, or eating too many foods that are high in cholesterol. High cholesterol can raise your risk of heart disease.

What Zetia does

Zetia contains the active drug ezetimibe. It belongs to a class of drugs called cholesterol absorption inhibitors. (A class of drugs is a group of medications that work in a similar way.) Cholesterol absorption inhibitors prevent your small intestine from absorbing cholesterol. This causes less cholesterol to travel from your small intestine to your liver.

Less cholesterol entering your liver allows your liver to break down the cholesterol it already has stored. When this happens, more cholesterol can then be cleared from your blood by your liver.

Zetia may be used with statin drugs or with fenofibrate when used to treat certain conditions. Examples of statin drugs include atorvastatin (Lipitor) and simvastatin (Zocor). Ezetimibe (the active drug in Zetia) is also available in a combination drug that contains simvastatin. The brand name for this drug combination is Vytorin.

How long does it take to work?

It may take about 2 weeks for your cholesterol levels to improve after you start taking Zetia. You likely won’t notice Zetia working in your body. However, your doctor will check your cholesterol levels about 4 weeks after you start treatment. If your cholesterol levels haven’t started to improve, they may recommend a different treatment for you.

How long will Zetia stay in my system?

Zetia may stay in your system for several days after you stop taking it. However, it’s important that you don’t stop taking Zetia without first talking with your doctor. Tell your doctor if you’re experiencing bothersome side effects from Zetia. They can suggest ways to help relieve your side effects, or they may recommend a different treatment option for you.

Zetia may be used with statin drugs to treat the following conditions in adults:

Statins are another class of medications used to lower cholesterol. (A class of medications is a group of drugs that work in a similar way.) Your doctor may do liver function tests before you start treatment and regularly during your Zetia treatment. If your liver function tests show increased liver enzymes called transaminases while you’re using Zetia with a statin drug, your doctor may stop your treatment. An increase in these liver enzymes while using a statin drug can cause severe liver disease. For more information, see the “Precautions” section below.

In addition, Zetia may be used with fenofibrate to treat mixed hyperlipidemia. Fenofibrate is a drug used to lower your triglyceride levels.

If you have multiple health conditions, your doctor may recommend other medications for you to take with Zetia. Talk with your doctor to learn more about which medications are right for you.

As with all medications, the cost of Zetia can vary. To find current prices for Zetia tablets in your area, check out GoodRx.

The cost you find on GoodRx.com is what you may pay without insurance. The actual price you’ll pay depends on your insurance plan, your location, and the pharmacy you use.

Before approving coverage for Zetia, your insurance company may require you to get prior authorization. This means that your doctor and insurance company will need to communicate about your prescription before the insurance company will cover the drug. The insurance company will review the prior authorization request and decide if the drug will be covered.

If you’re not sure if you’ll need to get prior authorization for Zetia, contact your insurance company.

Financial and insurance assistance

If you need financial support to pay for Zetia, or if you need help understanding your insurance coverage, help is available.

Merck, the manufacturer of Zetia, offers a Patient Assistance Program. For more information and to find out if you’re eligible for support, call 800-727-5400 or visit the program website.

Generic version

Zetia is available in a generic form called ezetimibe. A generic drug is an exact copy of the active drug in a brand-name medication. The generic is considered to be as safe and effective as the original drug. And generics tend to cost less than brand-name drugs. To find out how the cost of ezetimibe compares to the cost of Zetia, visit GoodRx.com.

If your doctor has prescribed Zetia and you’re interested in using ezetimibe instead, talk with your doctor. They may have a preference for one version or the other. You’ll also need to check your insurance plan, as it may only cover one or the other.

It’s not known if Zetia is safe to take during pregnancy. Based on animal studies, Zetia may cause harm to the fetus when taken by a pregnant woman. However, animal studies don’t always predict what will happen in humans. Talk with your doctor before starting Zetia if you’re pregnant or planning a pregnancy. Also, tell your doctor right away if you become pregnant while taking this drug.

Zetia is sometimes used with medications in the statin drug class. Statins shouldn’t be used during pregnancy. Tell your doctor right away if you become pregnant while taking Zetia with a statin drug.

It’s not known if Zetia is safe to take during pregnancy. This drug has not been studied in pregnant women.

Zetia is sometimes used with medications in the statin drug class. Statin drugs aren’t safe to use during pregnancy. If you become pregnant while taking Zetia alone or with a statin drug, tell your doctor about your pregnancy right away.

If you’re sexually active and you or your partner can become pregnant, talk with your doctor about your birth control needs while you’re using Zetia.

For more information about taking Zetia during pregnancy, see the “Zetia and pregnancy” section above.

For women using Zetia

Women who could become pregnant should use birth control while taking Zetia with a statin drug. Talk with your doctor about birth control options that may be best for you.

For men using Zetia

The manufacturer of Zetia hasn’t given birth control recommendations for men using the drug. If you’re using Zetia while sexually active with a female who could become pregnant, talk with your doctor about your birth control needs.

It’s not known if it’s safe to take Zetia while breastfeeding or if the drug passes into breast milk. Zetia has been found in breast milk during animal studies. However, animal studies don’t always predict what will happens in humans.

Zetia is sometimes used with medications in the statin drug class. Statin drugs may pass into breast milk. Side effects could occur in children who are breastfed while the mother is using a statin drug. Therefore, you shouldn’t breastfeed if you’re taking Zetia with a statin drug.

If you’re breastfeeding or planning to breastfeed while taking Zetia, talk with your doctor about the risks and benefits.

Before taking Zetia, talk with your doctor about your health history. Zetia may not be right for you if you have certain medical conditions or other factors affecting your health. These include:

  • Underactive thyroid. There aren’t any known problems with taking Zetia alone if you have underactive thyroid. However, if you have underactive thyroid and are using Zetia with a statin drug, this can raise your risk of muscle problems as a side effect. Examples of these muscle problems include muscle pain, muscle weakness, or rhabdomyolysis (muscle breakdown). For more information about this side effect, see the “Zetia side effects” section. Before you start using Zetia with a statin drug, your doctor may do thyroid function tests. If your thyroid is underactive, your doctor may treat your thyroid condition before adding a statin drug. They may also select a different treatment option that’s a better fit for you. If you have thyroid problems, talk with your doctor about whether it’s safe for you to take a statin drug with Zetia.
  • Kidney problems. There aren’t any known problems with taking Zetia alone if you have kidney problems. However, if you have kidney problems and are using Zetia with a statin drug, this can raise your risk of muscle problems, such as muscle pain or weakness, or muscle breakdown. For more information about this side effect, see the “Zetia side effects” section. Your doctor may do kidney function tests before you start using Zetia with a statin drug. If you have kidney problems, your doctor may prescribe a lower statin dose. They may also choose a different treatment option that’s a better fit for you. If you have questions about using Zetia with a statin drug while you have kidney problems, talk with your doctor.
  • Liver problems. You shouldn’t use Zetia alone or with a statin drug if you have liver problems. Zetia is broken down by your liver, but it may not break down Zetia as effectively if you have liver problems. This can cause increased levels of Zetia in your body. Higher Zetia blood levels can raise your risk of side effects. Your doctor may do liver function tests before you start treatment and regularly during your Zetia treatment. If your liver function tests show increased liver enzymes called transaminases while you’re using Zetia with a statin drug, your doctor may stop your treatment. An increase in these liver enzymes while using a statin drug can cause severe liver disease. For more information about liver problems and other side effects of Zetia, see the “Zetia side effects” section. If you have liver problems, talk with your doctor about whether it’s safe for you to use Zetia alone or with a statin drug.
  • Allergic reaction. If you’ve had an allergic reaction to Zetia or any of its ingredients, you shouldn’t take Zetia. Ask your doctor about other medications that may be a better option for you.
  • Pregnancy. It isn’t known if Zeta is safe to use during pregnancy. For more information, see the “Zetia and pregnancy” section above.
  • Breastfeeding. It’s not known if Zetia can pass into the breast milk during breastfeeding. For more information, see the “Zetia and breastfeeding” section above.

Note: For more information about the potential negative effects of Zetia, see the “Zetia side effects” section above.

Do not use more Zetia than your doctor recommends. For some drugs, doing so may lead to unwanted side effects or overdose.

What to do in case you take too much Zetia

If you think you’ve taken too much of this drug, call your doctor. You can also call the American Association of Poison Control Centers at 800-222-1222 or use their online tool. But if your symptoms are severe, call 911 or your local emergency number, or go to the nearest emergency room right away.

When you get Zetia from the pharmacy, the pharmacist will add an expiration date to the label on the bottle. This date is typically 1 year from the date they dispensed the medication.

The expiration date helps guarantee that the medication is effective during this time. The current stance of the Food and Drug Administration (FDA) is to avoid using expired medications. If you have unused medication that has gone past the expiration date, talk to your pharmacist about whether you might still be able to use it.

Storage

How long a medication remains good can depend on many factors, including how and where you store the medication.

You should store Zetia tablets at a room temperature of 77°F (25°C) in a tightly sealed container away from light. In certain conditions (such as when traveling), you may temporarily store Zetia at temperatures of 59°F to 86°F (15°C to 30°C). Avoid storing this medication in areas where it could get damp or wet, such as bathrooms.

Disposal

If you no longer need to take Zetia and have leftover medication, it’s important to dispose of it safely. This helps prevent others, including children and pets, from taking the drug by accident. It also helps keep the drug from harming the environment.

This article provides several useful tips on medication disposal. You can also ask your pharmacist for information on how to dispose of your medication.

The following information is provided for clinicians and other healthcare professionals.

Indications

Zetia is indicated as an adjunct to a low-cholesterol diet for treatment of the following types of hyperlipidemia:

  • Primary hyperlipidemia. For this condition, Zetia is used:
    • in adults as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin drug)
    • in children ages 10 years and older

For treatment of primary hyperlipidemia, Zetia is indicated to reduce total cholesterol, low-density lipoprotein (LDL) cholesterol, non-high-density lipoprotein (non-HDL) cholesterol, and apiloprotein B (ApoB).

  • Mixed hyperlipidemia. For this purpose, Zetia is used:
    • in adults in combination with a fenofibrate
    • in children ages 10 years and older

For treatment of mixed hyperlipidemia, Zetia is indicated to reduce total cholesterol, LDL cholesterol, non-HDL cholesterol, and ApoB.

  • Homozygous familial hypercholesterolemia (HoFH). For this purpose, Zetia is used in combination with atorvastatin or simvastatin in adults. Zetia is also approved for use in children ages 10 years and older with this condition. For treatment of HoFH, Zetia is indicated to reduce total cholesterol and LDL cholesterol.
  • Homozygous sitosterolemia. For this condition, Zetia is used as monotherapy in adults and in children ages 10 years and older. For treatment of homozygous sitosterolemia, Zetia is indicated to reduce levels of sitosterol and campesterol.

Zetia’s effect on cardiovascular morbidity and mortality isn’t known. Zetia hasn’t been studied in certain types of dyslipidemia, including Frederickson types I, III, IV, and V.

Administration

Zetia is taken orally with or without food. When taken together, it should be administered at least 2 hours before or 4 hours after a bile acid sequestrant. Examples of bile acid sequestrants include:

  • cholestyramine (Prevalite, Questran)
  • colesevelam (Welchol)
  • colestipol (Colestid)

Mechanism of action

Zetia inhibits the intestinal absorption of cholesterol and phytosterols, resulting in a decrease in the transport of intestinal cholesterol to the liver. Its intestinal molecular target is the Niemann-Pick C1-Like 1 (NPC1L1) sterol transporter. A decrease in the transport of intestinal cholesterol to the liver reduces stores of hepatic cholesterol. This in turn increases clearance of cholesterol from the blood. Zetia’s mechanism of action is considered complementary to that of statins and fenofibrate.

Pharmacokinetics and metabolism

Within 4 to 12 hours of oral administration, a single 10-mg dose of Zetia reaches peak plasma concentrations of 3.4 to 5.5 ng/mL. Absorption isn’t affected by food. Zetia is metabolized in the small intestine and liver. Its primary metabolic pathway is via hepatic glucuronic conjunction. Zetia is primarily cleared from the body through fecal excretion.

Contraindications

Zetia is contraindicated under the following conditions:

  • in combination with statins, in people with hepatic disease
  • in combination with statins, in people with elevated hepatic transaminases
  • in combination with statins, during pregnancy or in someone planning to become pregnant
  • in combination with statins, while breastfeeding
  • in people who have a known allergy to Zetia

Storage

Zetia tablets should be stored at a room temperature of 77°F (25°C) in a tightly sealed container away from light. Temporary excursions of 59°F to 86°F (15°C to 30°C) are allowed. Zetia should be protected from moisture and shouldn’t be stored in areas where it could get damp or wet, such as bathrooms.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up to date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.