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Ezetimibe

Familial Combined Hyperlipidemia, Hypercholesterolemia ... show more

DRUG STATUS

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Government Approvals

US(FDA), UK(BNF)

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WHO Essential Medicine

YES

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Known Teratogen

No

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Pharmaceutical Class

Dietary Cholesterol Absorption Inhibitor

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Drug Ingredient

Ezetimibe

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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

What is Ezetimibe used for?

Ezetimibe is primarily indicated for the treatment of high cholesterol (hypercholesterolemia). It is used to lower LDL ("bad" cholesterol) and total cholesterol levels in patients with primary hypercholesterolemia, either alone or in combination with statins. Ezetimibe is also used to treat homozygous familial hypercholesterolemia and is prescribed to reduce cholesterol in patients with atherosclerosis to reduce the risk of heart attack, stroke, and other cardiovascular conditions.

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.

How does one know if Ezetimibe is working?

The benefit of Ezetimibe is evaluated through regular blood tests to monitor cholesterol levels, particularly LDL ("bad" cholesterol) and total cholesterol. The effectiveness of the medication can also be assessed by tracking improvements in overall cardiovascular health, such as reduced risk of heart attacks and strokes. Your healthcare provider may also evaluate your progress by assessing changes in your diet, exercise habits, and other lipid markers.

Directions for Use

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.

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.

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 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).

Warnings and Precautions

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.

Can I take Ezetimibe with other prescription drugs?

  1. 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.
  2. Fibrates (e.g., gemfibrozil) – When used together, they may increase the risk of muscle pain or damage.
  3. Cyclosporine – This combination can increase the levels of Ezetimibe in the blood, potentially increasing the risk of side effects.

Can I take Ezetimibe with vitamins or supplements?

Ezetimibe has minimal interactions with vitamins or supplements. However, patients should be cautious when taking niacin (vitamin B3) as it may increase the risk of muscle-related side effects when combined with Ezetimibe, especially when taken with statins. There are no significant interactions with other common vitamins or minerals, but it's always best to consult a healthcare provider before starting any new supplements while on Ezetimibe.

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 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.

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 exercise while taking Ezetimibe?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.

Is it safe to drink alcohol while taking Ezetimibe?

From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.