Ezetimibe
Familial Combined Hyperlipidemia, Hypercholesterolemia ... show more
Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
YES
Known Teratogen
NO
Pharmaceutical Class
Dietary Cholesterol Absorption Inhibitor
Controlled Drug Substance
NO

Ezetimibe
Summary
Ezetimibe is primarily used to treat high cholesterol, also known as hypercholesterolemia. It can lower bad cholesterol (LDL) and total cholesterol levels. It's also used to treat a condition called homozygous familial hypercholesterolemia and to reduce cholesterol in patients with atherosclerosis, which can help reduce the risk of heart attack, stroke, and other cardiovascular conditions.
Ezetimibe works by blocking the absorption of cholesterol in your small intestine. It specifically targets a protein responsible for transporting cholesterol into your bloodstream. By blocking this protein, Ezetimibe reduces the amount of cholesterol that enters your body, which can lower your total and LDL cholesterol levels.
The usual dosage of Ezetimibe for adults is 10 mg once daily. It can be taken with or without food and at any time of the day. If you're taking it with a statin, both medications can typically be taken together. Always follow your healthcare provider's instructions.
Common side effects of Ezetimibe include headache, diarrhea, abdominal pain, and muscle pain. More serious adverse effects are rare but may include liver problems and allergic reactions, such as rash or swelling. In some cases, Ezetimibe can cause muscle weakness or inflammation, and very rarely severe muscle breakdown.
Ezetimibe should be used with caution in patients with liver disease, as it may increase the risk of liver problems. It is not recommended for patients with a known hypersensitivity to Ezetimibe or any of its components. Patients who are pregnant or breastfeeding should avoid using Ezetimibe unless specifically advised by a healthcare provider, as its safety during these times is not well established.
Indications and Purpose
How does Ezetimibe work?
Ezetimibe works by inhibiting the absorption of cholesterol in the small intestine. It specifically targets the Niemann-Pick C1-like 1 (NPC1L1) protein, which is responsible for transporting cholesterol from the intestine into the bloodstream. By blocking this protein, Ezetimibe reduces the amount of cholesterol that enters the body, leading to lower levels of total cholesterol and LDL ("bad" cholesterol). This helps reduce the risk of heart disease and other cardiovascular conditions.
Is Ezetimibe effective?
Clinical studies have demonstrated that Ezetimibe effectively lowers LDL ("bad" cholesterol) levels. In trials like the IMPROVE-IT study, Ezetimibe, when combined with statins, significantly reduced cardiovascular events such as heart attacks and strokes compared to statin therapy alone. Additionally, studies have shown that Ezetimibe lowers total cholesterol levels and improves the lipid profile, making it a valuable treatment for managing high cholesterol and reducing the risk of cardiovascular disease.
What is Ezetimibe?
Ezetimibe is commonly used to lower cholesterol levels in the blood, particularly when combined with statins. It works by inhibiting the absorption of cholesterol in the small intestine, which reduces the amount of cholesterol that enters the bloodstream. This helps lower total cholesterol and LDL ("bad" cholesterol) levels, reducing the risk of heart disease and stroke. Ezetimibe is often prescribed alongside diet changes and exercise for more effective cholesterol management.
Directions for Use
For how long do I take Ezetimibe?
Ezetimibe is typically used for life to manage cholesterol levels. It is important to continue taking it as prescribed by your doctor to maintain its effectiveness.
How do I dispose of Ezetimibe?
If you can, bring unused medicines to a drug take-back program or collection site at a pharmacy or hospital. They will dispose of this medicine properly so they don't harm people or the environment. If you can't find a take-back program, you can throw most medicines in the trash at home. But first, take them out of their original containers, mix them with something undesirable like used coffee grounds, seal the mixture in a plastic bag and throw it away.
How do I take Ezetimibe?
Ezetimibe can be taken with or without food, and there are no specific food restrictions while using this medication. It's important to take it at the same time each day for consistency. If you're taking Ezetimibe in combination with a statin or other cholesterol-lowering medications, follow your healthcare provider’s instructions closely. Always avoid taking large amounts of grapefruit or grapefruit juice as it may interact with certain cholesterol medications, although this is more of a concern with statins than Ezetimibe.
How long does it take for Ezetimibe to start working?
Ezetimibe usually starts working within 2 weeks of starting the medication. However, the maximum effect is typically achieved within 4 weeks and maintained with ongoing therapy.
How should I store Ezetimibe?
Keep the ezetimibe tablets in their original container, tightly closed, and out of reach of children. Store them at room temperature, away from heat and moisture (not in the bathroom).
What is the usual dose of Ezetimibe?
The usual daily dose of Ezetimibe for both adults and children aged 10 years and older is one 10 mg tablet taken once a day.
Warnings and Precautions
Can Ezetimibe be taken safely while breastfeeding?
Ezetimibe is a medication that may be taken while breastfeeding, but it's always best to talk to your doctor or pharmacist first. Only a small amount of Ezetimibe passes into breast milk, so it's unlikely to harm your baby. However, its safety for breastfeeding infants hasn't been fully studied. So it's important to weigh the benefits of taking the medication against any potential risks to your baby before deciding.
Can Ezetimibe be taken safely while pregnant?
Ezetimibe is not commonly recommended during pregnancy due to limited safety data. If you have high cholesterol and are pregnant, your doctor may prescribe it under special circumstances.
Can I take Ezetimibe with other prescription drugs?
- Statins (e.g., atorvastatin, simvastatin) – Combining Ezetimibe with statins can increase the risk of muscle-related side effects, such as myopathy or rhabdomyolysis, and liver damage.
- Fibrates (e.g., gemfibrozil) – When used together, they may increase the risk of muscle pain or damage.
- Cyclosporine – This combination can increase the levels of Ezetimibe in the blood, potentially increasing the risk of side effects.
Does Ezetimibe have adverse effects?
Adverse effects are unwanted or harmful effects that can occur with medication use. For Ezetimibe, some concerning adverse effects include muscle pain, liver problems, allergic reactions, and fatigue. These effects are not very common, but they can occur. Serious adverse effects, though rare, may include severe muscle pain or weakness, which could indicate a condition called rhabdomyolysis, or liver damage, which may present as yellowing of the skin or eyes. It's important to report any new or unusual symptoms to a healthcare provider and to consult them before stopping the medication.
Does Ezetimibe have any safety warnings?
Ezetimibe comes with safety warnings, particularly regarding liver function and muscle problems. It can affect liver enzymes, so regular monitoring of liver function tests is advised. Symptoms like yellowing of the skin or eyes may indicate liver issues. Ezetimibe can also cause muscle pain or weakness, which could be a sign of a serious condition called rhabdomyolysis. If you experience unexplained muscle pain, tenderness, or weakness, contact your healthcare provider immediately. Always follow your doctor's advice and report any unusual symptoms.
Is Ezetimibe addictive?
Ezetimibe has no known potential for dependence or addiction. It is not habit-forming, and there are no behaviors or warning signs associated with physical or psychological dependence on this medicine. You can take Ezetimibe as prescribed by your healthcare provider without concern for addiction. Always follow your doctor's instructions and discuss any concerns you may have about your medication.
Is Ezetimibe safe for the elderly?
Ezetimibe is generally safe for elderly patients, with no significant differences in safety or effectiveness compared to younger adults. However, elderly patients should be monitored closely for any side effects, and dosage adjustments may be necessary based on individual health conditions.
Is it safe to drink alcohol while taking Ezetimibe?
Most people tolerate Ezetimibe well, and occasional alcoholic drinks should not affect the way this medicine works. There are no well-established interactions between Ezetimibe and alcohol that would interfere with the medicine's effectiveness. However, excessive alcohol consumption can affect liver function, and since Ezetimibe is processed by the liver, it's best to drink alcohol in moderation. If you have any concerns or experience unusual symptoms, consult your healthcare provider.
Is it safe to exercise while taking Ezetimibe?
Most people tolerate Ezetimibe well, and it should not limit your ability to exercise. There are no known symptoms caused by Ezetimibe that would affect exercise capacity, physical strength, or endurance. You can continue your regular exercise routine while taking this medicine. If you experience any unusual symptoms during physical activity, such as muscle pain or weakness, consult your healthcare provider for advice.
Is it safe to stop Ezetimibe?
Ezetimibe is typically used for the long-term management of high cholesterol, which is an asymptomatic chronic condition. Stopping Ezetimibe suddenly may lead to an increase in cholesterol levels, which can raise the risk of heart disease or stroke over time. There are no known withdrawal symptoms, but the benefits of cholesterol management will be lost. It's crucial to consult with a doctor before stopping Ezetimibe to discuss any potential risks and to explore alternative treatments if necessary.
What are the most common side effects of Ezetimibe?
A side effect is an unwanted or unexpected reaction to a medicine. Common side effects of Ezetimibe include headache, diarrhea, muscle pain, fatigue, and upper respiratory tract infection. These side effects are not very common and may be mild and temporary. It's important to remember that new symptoms can occur when starting any new medicine, and they may not always be related to the medicine itself. Always speak to a healthcare provider before stopping any medication to ensure it's safe to do so.
Who should avoid taking Ezetimibe?
Ezetimibe should be used with caution in patients with liver disease, especially if combined with statins, as it may increase the risk of liver problems. It is contraindicated in patients with a known hypersensitivity to Ezetimibe or any of its components. Additionally, patients who are pregnant or breastfeeding should avoid using Ezetimibe unless specifically advised by a healthcare provider, as its safety during pregnancy and lactation is not well established. Regular liver function tests are recommended during treatment.