Ezetimibe

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Generic Name of Ezetimibe - Learn More

Ezetimibe

Ezetimibe Precaution - What You Need to Know

- Pregnancy and Breastfeeding: Ezetimibe is classified as Pregnancy Category C by the FDA, which means that its safety during pregnancy has not been well-established. It should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. It is not known whether ezetimibe passes into breast milk, so it should be used cautiously in breastfeeding women. The decision to use this drug should be based on a careful risk-benefit analysis.
- Hepatic Impairment: In patients with moderate to severe hepatic impairment, ezetimibe should be used cautiously. It is primarily metabolized in the liver, and impaired liver function can lead to increased drug levels and a heightened risk of side effects. Regular monitoring of liver function tests is recommended.
- Renal Impairment: Ezetimibe can generally be used in patients with mild to moderate renal impairment without dose adjustments. However, in patients with severe renal impairment, caution is advised due to the potential for altered drug metabolism and accumulation, although significant dose adjustments are typically not necessary.
- Musculoskeletal Concerns: Ezetimibe can, in rare cases, cause muscle-related side effects like myopathy or rhabdomyolysis, particularly when used in combination with statins. It is important to monitor for symptoms such as muscle pain, weakness, or tenderness, especially if the patient has renal impairment or is taking other cholesterol-lowering drugs.
- Monitoring: During therapy, liver function tests and muscle-related symptoms (especially in combination with statins) should be monitored regularly to detect any adverse effects early.

Ezetimibe Indication - Uses and Benefits

- Hypercholesterolemia: Ezetimibe is primarily indicated for the treatment of primary hypercholesterolemia (both heterozygous familial and non-familial), either as monotherapy or in combination with statins (HMG-CoA reductase inhibitors) to lower total cholesterol, LDL cholesterol, and apolipoprotein B levels. It works by inhibiting the absorption of cholesterol from the small intestine.
- Homozygous Familial Hypercholesterolemia (HoFH): Ezetimibe is also used in combination with other lipid-lowering treatments (such as statins or LDL apheresis) in patients with homozygous familial hypercholesterolemia, a genetic condition leading to very high levels of cholesterol.
- Mixed Dyslipidemia: It is often prescribed in combination with other cholesterol-lowering agents to manage mixed dyslipidemia, a condition where patients have both high cholesterol and elevated triglycerides.
- Off-label Uses: Ezetimibe may also be considered in the management of sitosterolemia, a rare inherited condition characterized by excessive plant sterol absorption, where ezetimibe has shown benefit in lowering plant sterol levels.
- Evidence-Based Context: Ezetimibe has been shown to be effective in reducing atherosclerotic cardiovascular disease (ASCVD) risk when used in combination with statins, especially in patients who are at high risk of heart attacks or stroke. Clinical trials have demonstrated that ezetimibe can significantly reduce LDL cholesterol levels and improve cardiovascular outcomes, particularly in high-risk patients.

Ezetimibe Contraindications - Important Warnings

- Active Liver Disease: Ezetimibe is contraindicated in patients with active liver disease or unexplained persistent elevations in liver enzymes. This includes conditions like hepatitis and cirrhosis, as the drug is metabolized by the liver, and hepatic dysfunction could worsen or be exacerbated by its use.
- Hypersensitivity: Ezetimibe is contraindicated in patients who have shown hypersensitivity or allergic reactions to the drug or any of its components, including angioedema, rash, or hives.
- Pregnancy and Breastfeeding: As mentioned, ezetimibe is not recommended during pregnancy and breastfeeding, unless deemed absolutely necessary, due to a lack of sufficient safety data for these populations.
- Concomitant Use with Certain Lipid-Lowering Agents: Ezetimibe should not be used in combination with gemfibrozil (a fibrate), as this combination can increase the risk of muscle-related side effects (e.g., myopathy or rhabdomyolysis). If combined with statins, the patient must be monitored carefully for muscle toxicity, particularly in those with renal impairment or other risk factors.
- Children: Ezetimibe is not approved for use in children younger than 10 years for primary hypercholesterolemia, although it can be used in pediatric patients with HoFH under the guidance of a healthcare provider.

Ezetimibe Side Effects - What to Expect

- Common Side Effects:
- Gastrointestinal symptoms: These include diarrhea, abdominal pain, and nausea, which tend to be mild and resolve with continued use.
- Headache: A common side effect, especially when first starting therapy.
- Fatigue: Some patients may report feelings of tiredness or fatigue, though this is usually mild.
- Serious Side Effects:
- Muscle-Related Issues: Myopathy and rhabdomyolysis are rare but serious side effects, especially in patients using statins or those with renal dysfunction. Patients should be monitored for muscle pain, weakness, and tenderness.
- Liver Enzyme Elevations: Although rare, elevations in liver enzymes (ALT, AST) have been observed, and periodic liver function tests are recommended during therapy.
- Angioedema and Rash: Severe allergic reactions, including angioedema and rash, though rare, require immediate discontinuation of the drug.
- Pancreatitis: Some patients have reported pancreatitis, though this is not common.
- Liver Dysfunction: In combination with other lipid-lowering agents, ezetimibe may contribute to liver dysfunction or exacerbate preexisting conditions, necessitating regular monitoring.

Ezetimibe Pregnancy Category ID - Safety Information

3

Ezetimibe Mode of Action - How It Works

Ezetimibe works by inhibiting the Niemann-Pick C1-like 1 (NPC1L1) protein, which plays a key role in the absorption of cholesterol from the small intestine. By blocking this transporter, ezetimibe reduces the amount of cholesterol entering the bloodstream. This results in a reduction of total cholesterol and LDL cholesterol, both of which are significant contributors to atherosclerotic cardiovascular disease (ASCVD).
- Pharmacodynamics: Ezetimibe is absorbed in the small intestine and extensively metabolized in the liver. The active metabolite, ezetimibe glucuronide, is responsible for its cholesterol-lowering effect.
- Pharmacokinetics: Ezetimibe reaches peak plasma concentrations within 1 to 2 hours of oral administration. It has a half-life of 22 hours, allowing for once-daily dosing. The drug is primarily excreted via the feces (90% of the dose), with a small amount eliminated through the urine.

Ezetimibe Drug Interactions - What to Avoid

- Statins: When used in combination with statins, ezetimibe may enhance the cholesterol-lowering effects. However, this combination increases the risk of myopathy and rhabdomyolysis. Patients should be monitored for muscle pain, weakness, or tenderness, particularly during the first few months of therapy or when doses are increased.
- Fibrates: Combining ezetimibe with gemfibrozil (a fibrate) is not recommended due to the increased risk of muscle toxicity. If a fibrate is used, fenofibrate is considered a safer alternative in combination with ezetimibe.
- Cyclosporine: Cyclosporine, an immunosuppressant, can increase the blood levels of ezetimibe, potentially leading to an increased risk of side effects. Dose adjustments of either drug may be necessary, and close monitoring is recommended.
- Cholestyramine: Cholestyramine, a bile acid sequestrant, may decrease the absorption and effectiveness of ezetimibe. It is advised to take ezetimibe at least 2 hours before or 4 hours after cholestyramine to avoid interaction.
- Antacids: Antacids containing aluminum or magnesium may reduce the absorption of ezetimibe. Therefore, if antacids are necessary, they should be taken at least 2 hours apart from ezetimibe.

Ezetimibe Adult Dose - Recommended Dosage

- Monotherapy: The usual recommended dose of ezetimibe is 10 mg once daily.
- Combination Therapy: When used in combination with statins or other lipid-lowering agents, the typical dose remains 10 mg once daily.
- Renal Impairment: No dosage adjustment is necessary for patients with mild to moderate renal impairment. In patients with severe renal impairment, monitoring is recommended, though dose adjustment is typically not required.
- Hepatic Impairment: In patients with moderate to severe hepatic impairment, ezetimibe should be used with caution, and dose adjustments may be required based on clinical judgment.

Ezetimibe Child Dose - Dosage for Children

- Pediatrics: Ezetimibe is approved for use in children aged 10 years and older for the treatment of heterozygous familial hypercholesterolemia in combination with statins. The usual dose for children is 10 mg once daily. Ezetimibe should be used with caution in pediatric patients, and regular monitoring for side effects is recommended. The safety and efficacy in younger children have not been established.

Ezetimibe Renal Dose - Dosage for Kidney Conditions

- Renal Impairment: No dose adjustments are necessary for mild to moderate renal impairment. However, patients with severe renal impairment should be monitored closely, though no specific recommendations are available for dosage adjustments in this population.