Ezetimibe 10mg Tablets
It is used to lower cholesterol.This drug may be used with other drugs to treat your health condition. If you are also taking other drugs, talk with your doctor about the risks and side effects that may happen.
Drug Class
Antilipemic agent
Pharmacologic Class
Selective cholesterol absorption inhibitor
Pregnancy Category
Category C
FDA Approved
Oct 2002
DEA Schedule
Not Controlled
Overview
What is this medicine?
Ezetimibe is a medication that helps lower your 'bad' cholesterol (LDL-C) by blocking its absorption from the food you eat in your intestines. It works differently from statins, which block cholesterol production in the liver. It can be used alone or with a statin to further reduce cholesterol levels.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day.
Continuing Your Medication
Even if you start to feel well, continue taking your medication as directed by your doctor or healthcare provider. Do not stop taking it without consulting your doctor first.
Storing and Disposing of Your Medication
To keep your medication safe and effective, store it at room temperature in a dry place, away from the bathroom. Keep all medications out of the reach of children and pets. When you're finished with your medication or it expires, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you're unsure about how to dispose of your medication, ask your pharmacist for guidance. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day.
Continuing Your Medication
Even if you start to feel well, continue taking your medication as directed by your doctor or healthcare provider. Do not stop taking it without consulting your doctor first.
Storing and Disposing of Your Medication
To keep your medication safe and effective, store it at room temperature in a dry place, away from the bathroom. Keep all medications out of the reach of children and pets. When you're finished with your medication or it expires, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you're unsure about how to dispose of your medication, ask your pharmacist for guidance. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next dose, skip the missed dose and return to your regular schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Continue to follow a cholesterol-lowering diet as recommended by your doctor or dietitian.
- Engage in regular physical activity.
- Maintain a healthy weight.
- Avoid smoking and limit alcohol intake.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg orally once daily
Dose Range:
10 - 10 mg
Condition-Specific Dosing:
primaryHyperlipidemia:
10 mg orally once daily, alone or with an HMG-CoA reductase inhibitor (statin).
homozygousFamilialHypercholesterolemia (HoFH):
10 mg orally once daily, with atorvastatin or simvastatin.
homozygousSitosterolemia:
10 mg orally once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
10 mg orally once daily for children 10 years and older with primary hyperlipidemia or homozygous familial hypercholesterolemia.
Adolescent:
10 mg orally once daily for adolescents 10 years and older with primary hyperlipidemia or homozygous familial hypercholesterolemia.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment needed.
Moderate:
No dosage adjustment needed.
Severe:
No dosage adjustment needed.
Dialysis:
No dosage adjustment needed for patients on dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment needed.
Moderate:
Not recommended (due to increased ezetimibe exposure).
Severe:
Not recommended (due to increased ezetimibe exposure).
Pharmacology
Mechanism of Action
Ezetimibe selectively inhibits the absorption of cholesterol and related phytosterols by the small intestine. It localizes at the brush border of the small intestine and inhibits the Niemann-Pick C1-Like 1 (NPC1L1) protein, which is involved in intestinal uptake of cholesterol. This leads to a decrease in the delivery of intestinal cholesterol to the liver, which in turn reduces hepatic cholesterol stores and increases clearance of cholesterol from the blood.
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely determined due to extensive first-pass metabolism, but well absorbed.
Tmax:
Ezetimibe: 4-12 hours; Ezetimibe-glucuronide: 1-2 hours.
FoodEffect:
Food has no effect on the oral bioavailability of ezetimibe.
Distribution:
Vd:
Not widely reported, but extensive tissue distribution.
ProteinBinding:
>90% (ezetimibe and ezetimibe-glucuronide) to human plasma proteins.
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 22 hours (for both ezetimibe and ezetimibe-glucuronide).
Clearance:
Not precisely quantified, but primarily through biliary and renal excretion.
ExcretionRoute:
Approximately 78% in feces and 11% in urine (as total ezetimibe).
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 2 weeks (significant LDL-C reduction).
PeakEffect:
Within 2 weeks (maximal LDL-C reduction).
DurationOfAction:
Sustained with daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Dizziness or fainting
Rapid heartbeat
Flu-like symptoms, including:
+ Fever
+ Sore throat
+ Cough
+ Fatigue
+ Joint pain
Dark urine or yellowing of the skin and eyes
Muscle pain, tenderness, or weakness, which can be a sign of a severe muscle problem (rhabdomyolysis), especially if you are taking other medications that increase the risk of muscle problems. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention.
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Joint pain
Back pain
Pain in the arms or legs
Diarrhea
Feeling tired or weak
Nose or throat irritation
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Dizziness or fainting
Rapid heartbeat
Flu-like symptoms, including:
+ Fever
+ Sore throat
+ Cough
+ Fatigue
+ Joint pain
Dark urine or yellowing of the skin and eyes
Muscle pain, tenderness, or weakness, which can be a sign of a severe muscle problem (rhabdomyolysis), especially if you are taking other medications that increase the risk of muscle problems. If you experience abnormal muscle pain, tenderness, or weakness (with or without fever or feeling unwell), contact your doctor immediately. If muscle problems persist after stopping the medication, seek medical attention.
Other Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Joint pain
Back pain
Pain in the arms or legs
Diarrhea
Feeling tired or weak
Nose or throat irritation
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (could be a sign of muscle damage).
- Yellowing of your skin or the whites of your eyes (jaundice), unusual tiredness, loss of appetite, or pain in your upper right stomach area (could be signs of liver problems).
- Severe stomach pain that may spread to your back (could be a sign of gallstones or pancreatitis).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease or elevated liver enzymes.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood work and laboratory tests should be conducted as directed by your doctor to monitor your condition. Adhere to the diet and exercise plan recommended by your doctor to ensure optimal results. When taking this drug, avoid concurrent use of colestipol or cholestyramine within a 4-hour window before or 2-hour window after administration. If you are pregnant, planning to become pregnant, or are breast-feeding, consult your doctor to discuss the potential benefits and risks associated with this medication for both you and your baby.
Overdose Information
Overdose Symptoms:
- In clinical studies, single doses of ezetimibe up to 50 mg/day for 14 days and 40 mg/day for 28 days were generally well tolerated. Overdose symptoms are generally mild and non-specific.
What to Do:
In the event of an overdose, symptomatic and supportive measures should be instituted. Call your local poison control center (e.g., 1-800-222-1222 in the US) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Cyclosporine: Co-administration with cyclosporine significantly increases ezetimibe exposure. Monitor cyclosporine levels and ezetimibe exposure carefully.
- Fibrates (especially Gemfibrozil): Co-administration with gemfibrozil is not recommended due to increased risk of cholelithiasis and myopathy. Other fibrates (e.g., fenofibrate) may be used with caution, but monitor for adverse effects.
Moderate Interactions
- Bile Acid Sequestrants (e.g., Cholestyramine): May decrease the absorption of ezetimibe. Administer ezetimibe at least 2 hours before or 4 hours after a bile acid sequestrant.
- Warfarin: Co-administration may increase INR. Monitor INR closely when initiating or discontinuing ezetimibe.
Monitoring
Baseline Monitoring
Lipid Panel (LDL-C, HDL-C, Total Cholesterol, Triglycerides)
Rationale: To establish baseline lipid levels and assess the need for therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST)
Rationale: To establish baseline liver enzyme levels, especially if co-administered with a statin.
Timing: Prior to initiation of therapy.
Routine Monitoring
Lipid Panel (LDL-C, HDL-C, Total Cholesterol, Triglycerides)
Frequency: 4-12 weeks after initiation or dose adjustment, then periodically (e.g., every 6-12 months) as clinically indicated.
Target: Individualized based on patient risk factors and treatment goals (e.g., LDL-C reduction targets).
Action Threshold: Failure to meet lipid goals, or unexpected increase in lipid levels.
Liver Function Tests (ALT, AST)
Frequency: Periodically, especially if co-administered with a statin, or if symptoms of liver dysfunction develop.
Target: Within normal limits (typically <3 times upper limit of normal).
Action Threshold: Persistent elevations >3 times upper limit of normal; consider dose reduction or discontinuation.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (potential myopathy/rhabdomyolysis)
- Dark urine (potential rhabdomyolysis)
- Yellowing of skin or eyes (jaundice), unexplained fatigue, loss of appetite, upper right abdominal pain (potential liver dysfunction)
- Severe abdominal pain (potential cholelithiasis/pancreatitis)
Special Patient Groups
Pregnancy
Pregnancy Category C. There are no adequate and well-controlled studies of ezetimibe in pregnant women. Ezetimibe should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential risk to fetus not fully established; use only if clearly needed.
Second Trimester:
Potential risk to fetus not fully established; use only if clearly needed.
Third Trimester:
Potential risk to fetus not fully established; use only if clearly needed.
Lactation
It is not known whether ezetimibe is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk level L3 (Moderate concern) due to unknown excretion into human milk and potential for adverse effects.
Pediatric Use
Safety and effectiveness in pediatric patients younger than 10 years of age have not been established. For patients 10 years and older, the recommended dose is 10 mg once daily.
Geriatric Use
No dosage adjustment is required for elderly patients. Efficacy and safety profiles are similar to those observed in younger patients.
Clinical Information
Clinical Pearls
- Ezetimibe can be taken at any time of day, with or without food.
- When co-administered with a statin, ezetimibe can be taken at the same time as the statin.
- If co-administered with a bile acid sequestrant (e.g., cholestyramine), ezetimibe should be taken at least 2 hours before or 4 hours after the bile acid sequestrant.
- Ezetimibe is particularly useful for patients who cannot tolerate higher doses of statins or who need additional LDL-C lowering beyond what statins alone can achieve.
- It is generally well-tolerated, with a low incidence of side effects.
Alternative Therapies
- HMG-CoA Reductase Inhibitors (Statins) (e.g., Atorvastatin, Rosuvastatin, Simvastatin)
- PCSK9 Inhibitors (e.g., Alirocumab, Evolocumab)
- Bile Acid Sequestrants (e.g., Cholestyramine, Colesevelam)
- Fibrates (e.g., Fenofibrate, Gemfibrozil)
- Niacin (Nicotinic Acid)
- Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors (e.g., Bempedoic Acid)
- Microsomal Triglyceride Transfer Protein (MTP) Inhibitors (e.g., Lomitapide - for HoFH)
- Apolipoprotein B-100 Synthesis Inhibitors (e.g., Mipomersen - for HoFH)
Cost & Coverage
Average Cost:
$15 - $50 per 30 tablets (generic)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.