| Fact Table | |
|---|---|
| Formula | C24H21F2NO3 |
| License | FDA approved (Initial U.S. Approval: 2002) |
| Bioavailability | Approximately 35% to 65% |
| Legal status | Prescription only (Rx) |
| Chemical Name | (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one |
| Elimination half-life | Approximately 22 hours |
| Dosage (Strength) | 10 mg oral tablet once daily, with or without food |
| Pregnancy | Use during pregnancy only if clearly needed; current labeling should be consulted for patient-specific risk assessment |
| Brands | Zetia |
| Protein binding | Highly protein bound (>90%) |
| PubChem CID | 150311 |
| MedlinePlus | a603015 |
| ChEBI | 49040 |
| ATC code | C10AX09 |
| DrugBank | DB00973 |
| KEGG | D01966 |
| Routes of administration | By mouth (oral) |
Zetia (ezetimibe) is a cholesterol-lowering medication that works differently than statins by blocking cholesterol absorption in the small intestine. This helps reduce LDL cholesterol levels in the blood. Zetia can be used alone or combined with statins and dietary changes to treat various types of high cholesterol, including inherited forms like familial hypercholesterolemia and familial sitosterolemia.
Ezetimibe is taken by mouth once daily, with or without food, at a standard dose of 10 mg for adults and children 10 years and older. It should be taken at the same time each day. If taking ezetimibe with a statin, both can be taken together, but if taking a bile acid sequestrant (like cholestyramine or colestipol), ezetimibe should be taken at least 2 hours before or at least 4 hours after the bile acid sequestrant.
Do not stop taking ezetimibe without consulting a healthcare provider. The medication may be used alone or combined with other cholesterol-lowering medicines. Follow a healthcare provider's instructions for dosage.
The active ingredient in Zetia is ezetimibe.
Before using this medication, you may want to consult a healthcare provider about the following:
Zetia is sometimes taken with other cholesterol-lowering medications such as statins or fibrates. When used together, the risks and side effects of those medications may also apply.
Liver enzyme levels may increase. Some people taking Zetia may develop elevated liver enzymes, which can signal liver irritation. Your healthcare provider may order blood tests to monitor liver function, especially if you take Zetia with a statin.
Muscle problems can occur in rare cases. Zetia may cause muscle pain, weakness, or a serious muscle condition called rhabdomyolysis, particularly when combined with statins or fibrates.
Avoid taking or using this medication if any of the following apply:
Common side effects of Zetia include:
Some people may also experience upper respiratory infections, sinus inflammation, flu-like symptoms, or a runny nose and sore throat. These side effects are usually mild and may happen whether Zetia is taken alone or with a statin. Let your healthcare provider know if symptoms persist or become bothersome.
More serious side effects are less common but possible. Zetia can cause increased liver enzymes, especially when taken with statins, which may require blood tests to monitor liver function. Muscle pain, tenderness, or weakness can also occur and may rarely lead to muscle breakdown (rhabdomyolysis). Contact a healthcare provider if you develop unexplained muscle pain, severe weakness, fever, or unusual fatigue.
What is Zetia (ezetimibe) used for?
Zetia is a cholesterol-lowering medicine used to reduce LDL cholesterol. It may be used by itself or together with a statin when more LDL lowering is needed. It is also used in certain inherited lipid disorders, including homozygous familial hypercholesterolemia and homozygous familial sitosterolemia.
How does Zetia work?
Zetia works differently from statins. Instead of mainly reducing cholesterol production in the liver, it decreases the absorption of cholesterol in the small intestine, which helps lower the amount of cholesterol circulating in the blood.
How is Zetia taken?
The usual dose is 10 mg by mouth once daily. It can be taken with or without food, and it may be taken alone or with other cholesterol medicines if prescribed.
What should I do if I miss a dose?
If you miss a dose, take it as soon as you remember. Do not take two doses at the same time or double the next dose.
Can Zetia be taken with a statin?
Yes. Zetia is commonly combined with a statin when cholesterol goals are not met with one medicine alone. When it is used with a statin, the warnings and precautions for the statin also matter, including pregnancy-related precautions and possible liver or muscle-related side effects.
What are the common side effects of Zetia?
Common side effects can include upper respiratory symptoms, diarrhea, joint pain, sinus-related symptoms, and pain in the arms or legs. When used with a statin, some side effects may overlap with the statin's side effect profile.
What serious side effects should people know about?
Serious but less common concerns include allergic reactions, liver enzyme elevations, muscle problems such as myopathy or rhabdomyolysis, and postmarketing reports of more severe skin reactions. Newer labeling updates have also noted liver transaminase information in postmarketing safety review.
Are there important drug interactions?
Yes. If Zetia is taken with a bile acid sequestrant, it should be taken at least 2 hours before or 4 hours after that medicine. Additional interaction precautions may apply with certain other lipid-lowering drugs, especially when combination therapy is used.
How soon does Zetia start showing results?
Cholesterol levels are usually reassessed after starting treatment, and LDL can be checked as early as 4 weeks after beginning ezetimibe. That helps determine how well the medicine is working and whether treatment needs adjustment.
Who should speak with a clinician before taking Zetia?
Anyone with active liver problems, unexplained muscle symptoms, pregnancy concerns, breastfeeding questions, or multiple cholesterol medicines should review use carefully with a clinician. This is especially important if Zetia is being combined with a statin, since the statin's safety guidance also applies.
A generic drug is a copy of the brand-name drug with the same dosage, safety, strength, quality, consumption method, performance, and intended use. Before generics become available on the market, the generic company must prove it has the same active ingredients as the brand-name drug and works in the same way and in the same amount of time in the body.
The only differences between generics and their brand-name counterparts is that generics are less expensive and may look slightly different (e.g., different shape or color), as trademark laws prevent a generic from looking exactly like the brand-name drug.
Generics are less expensive because generic manufacturers don't have to invest large sums of money to develop a drug. When the brand-name patent expires, generic companies can manufacture a copy of the brand-name and sell it at a substantial discount.