1. Introduction
Ezetimibe is a cholesterol absorption inhibitor used to lower blood cholesterol levels. It works by selectively inhibiting the absorption of cholesterol at the brush border of the small intestine, reducing the amount of cholesterol delivered to the liver. Ezetimibe is often used in combination with statins or as monotherapy for patients who cannot tolerate statins.
2. Indications
- Approved Indications:
- Primary hypercholesterolaemia (alone or in combination with a statin).
- Homozygous familial hypercholesterolaemia (in combination with a statin).
- Homozygous sitosterolaemia (phytosterolaemia).
- Off-Label Uses:
- Mixed dyslipidaemia (in combination with fenofibrate).
- Secondary prevention of cardiovascular events (as part of combination therapy).
3. Dosage
- Adults:
- 10 mg orally once daily, with or without food.
- Elderly:
- No dose adjustment required.
- Children (≥10 years):
- 10 mg orally once daily.
4. Administration
- Take orally once daily, at the same time each day, with or without food.
- Can be taken alongside statins or fenofibrate for enhanced lipid-lowering effects.
5. Forms Available
- Tablets: 10 mg.
6. Side Effects
6.1. Common Side Effects
- Diarrhoea.
- Abdominal pain.
- Fatigue.
- Headache.
6.2. Less Common Side Effects
- Flatulence.
- Back pain.
- Muscle aches (especially when combined with statins).
6.3. Rare but Serious Side Effects
- Myopathy or rhabdomyolysis (more common with statin combination).
- Elevated liver enzymes (particularly with statins).
- Severe allergic reactions (e.g., angioedema).
7. Warnings
- Myopathy/Rhabdomyolysis: Risk increases when used with statins or fibrates. Monitor for muscle pain or weakness.
- Liver Dysfunction: Elevated liver enzymes can occur, especially when combined with statins. Regular liver function tests are recommended.
- Gallstones: Increased risk when combined with fibrates due to altered bile composition.
8. Precautions
- Use cautiously in patients with moderate to severe hepatic impairment.
- Avoid use in patients with known hypersensitivity to ezetimibe or its components.
- Regular lipid profiles and liver function tests are recommended during therapy.
9. Interactions
- Drug-Drug Interactions:
- Statins: Increased risk of liver enzyme elevations and myopathy.
- Fibrates: Increased risk of gallstones and myopathy.
- Cyclosporine: Increased ezetimibe levels; monitor for toxicity.
- Bile acid sequestrants (e.g., cholestyramine): May reduce ezetimibe absorption; take ezetimibe 2 hours before or 4 hours after bile acid sequestrants.
10. Monitoring Parameters
- Lipid profile (LDL-C, HDL-C, triglycerides) to assess therapeutic response.
- Liver function tests, especially when used with statins or fibrates.
- Symptoms of myopathy or rhabdomyolysis (e.g., muscle pain, dark urine).
11. Use in Children
- Approved for children ≥10 years for primary hypercholesterolaemia or familial hypercholesterolaemia. Monitor lipid levels and side effects closely.
12. Use in Pregnancy
- Category C: Use only if the potential benefit outweighs the risk. Combination therapy with statins is contraindicated during pregnancy.
13. Use in Elderly
- Safe for use in elderly patients; no dose adjustment is required.
14. Use in Kidney Disease
- No dose adjustment is required in renal impairment. Use cautiously in severe renal dysfunction, especially in combination with statins.
15. Use in Liver Disease
- Avoid use in patients with moderate to severe hepatic impairment due to limited safety data.
16. Patient Counselling Points
- Take ezetimibe exactly as prescribed, even if you feel well.
- Inform your doctor if you experience unexplained muscle pain, tenderness, or weakness, especially when combined with statins.
- Take ezetimibe at the same time every day for best results.
- If taking bile acid sequestrants (e.g., cholestyramine), ensure proper spacing between doses to maintain effectiveness.
- Maintain a healthy diet and exercise routine to optimise cholesterol control.
17. Table of Brand Names, Manufacturers, and Prices
Brand Name | Manufacturer | Price (USD) |
---|---|---|
Zetia | Merck & Co. | $300–400 (30 tablets, 10 mg) |
Ezetrol | Merck Sharp & Dohme | $250–350 (30 tablets, 10 mg) |
Generic Ezetimibe | Various | $50–150 (30 tablets, 10 mg) |
18. FAQs (15 Questions)
- What is ezetimibe used for?
It is used to lower cholesterol levels, especially LDL cholesterol, and to treat conditions like familial hypercholesterolaemia. - How does ezetimibe work?
It inhibits cholesterol absorption in the small intestine, reducing the amount of cholesterol delivered to the liver. - How long does it take for ezetimibe to work?
Effects can be seen within 2 weeks, with full benefits typically observed within 4–6 weeks. - What are the common side effects of ezetimibe?
Common side effects include diarrhoea, abdominal pain, and headache. - Can ezetimibe cause muscle pain?
Yes, it can cause muscle pain, especially when combined with statins. - Is ezetimibe safe during pregnancy?
It should only be used if the benefits outweigh the risks. Combination therapy with statins is contraindicated during pregnancy. - Can ezetimibe be taken with food?
Yes, ezetimibe can be taken with or without food. - Does ezetimibe interact with other medications?
Yes, it interacts with statins, fibrates, cyclosporine, and bile acid sequestrants. - How should I take ezetimibe if I’m on bile acid sequestrants?
Take ezetimibe 2 hours before or 4 hours after the bile acid sequestrant. - Can children take ezetimibe?
Yes, it is approved for use in children aged 10 years and older for certain conditions. - Does ezetimibe cause liver damage?
It can cause liver enzyme elevations, especially when combined with statins. Liver function tests are recommended. - Can I stop taking ezetimibe once my cholesterol improves?
No, cholesterol levels may rise again. Continue therapy as directed by your doctor. - Is ezetimibe safe for elderly patients?
Yes, it is safe for elderly patients without the need for dose adjustments. - How should ezetimibe be stored?
Store at room temperature, away from light and moisture. - What should I do if I miss a dose of ezetimibe?
Take it as soon as you remember, but skip it if it’s close to the next dose. Do not double up.