Zetia 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
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 'bad' cholesterol (LDL-C) in your blood. It works by blocking the absorption of cholesterol from the food you eat in your intestines. This helps reduce the amount of cholesterol that reaches your liver and then your bloodstream.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and try to take it at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling better.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method or explore local drug take-back programs.
Missing 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 scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and try to take it at the same time every day. Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling better.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method or explore local drug take-back programs.
Missing 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 scheduled dose, skip the missed dose and resume your regular dosing 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 (low in saturated fat and cholesterol) as recommended by your doctor.
- Engage in regular physical activity.
- Maintain a healthy weight.
- Avoid smoking.
- Limit alcohol intake.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
10 mg orally once daily
Dose Range:
10 - 10 mg
Condition-Specific Dosing:
primary hyperlipidemia:
10 mg orally once daily, alone or with an HMG-CoA reductase inhibitor (statin).
homozygous familial hypercholesterolemia (HoFH):
10 mg orally once daily, with an HMG-CoA reductase inhibitor.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
10 mg orally once daily for children âĨ10 years of age with heterozygous familial hypercholesterolemia (HeFH) or homozygous familial hypercholesterolemia (HoFH).
Adolescent:
10 mg orally once daily for adolescents âĨ10 years of age with heterozygous familial hypercholesterolemia (HeFH) or homozygous familial hypercholesterolemia (HoFH).
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
No dosage adjustment necessary.
Dialysis:
No dosage adjustment necessary for patients with end-stage renal disease on dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment necessary (Child-Pugh score 5-6).
Moderate:
Not recommended (Child-Pugh score 7-9) due to increased ezetimibe exposure.
Severe:
Not recommended (Child-Pugh score >9) due to increased ezetimibe exposure.
Pharmacology
Mechanism of Action
Ezetimibe 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:
Variable (not precisely quantified due to extensive first-pass metabolism)
Tmax:
4-12 hours (for total ezetimibe, which includes ezetimibe and its active glucuronide metabolite)
FoodEffect:
Food has no significant effect on the oral bioavailability of ezetimibe.
Distribution:
Vd:
Approximately 7.8 L/kg
ProteinBinding:
>90% (ezetimibe and ezetimibe-glucuronide)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 22 hours (for total ezetimibe)
Clearance:
Not precisely quantified due to enterohepatic recirculation
ExcretionRoute:
Primarily in feces (78%), with a smaller amount in urine (11%)
Unchanged:
Less than 5% of total ezetimibe excreted unchanged in urine or feces
Pharmacodynamics
OnsetOfAction:
Within 2 weeks (for maximal LDL-C reduction)
PeakEffect:
Approximately 2 weeks (for maximal LDL-C reduction)
DurationOfAction:
Sustained as long as therapy continues due to long half-life and enterohepatic recirculation
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 or eyes
Muscle pain, tenderness, or weakness, which can be a sign of a severe muscle problem (rhabdomyolysis). This is more likely to occur when taking this medication with other drugs 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Joint pain
Back pain
Pain in 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, consult 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 experience any of the following symptoms, contact your doctor or seek medical attention right away:
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 or eyes
Muscle pain, tenderness, or weakness, which can be a sign of a severe muscle problem (rhabdomyolysis). This is more likely to occur when taking this medication with other drugs 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
Joint pain
Back pain
Pain in 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, consult 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 the skin or eyes (jaundice), dark urine, or unusual fatigue (could be signs of liver problems).
- Severe abdominal pain (especially if radiating to the back, could be pancreatitis or gallbladder issues if combined with fibrates).
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 in conjunction 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 in conjunction 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 of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- In clinical studies, single doses of ezetimibe 50 mg/day for 14 days and 400 mg/day for 8 days were well tolerated. No specific symptoms of overdose have been reported.
What to Do:
In the event of an overdose, symptomatic and supportive measures should be employed. Contact a poison control center (1-800-222-1222) or seek immediate medical attention.
Drug Interactions
Major Interactions
- Cyclosporine (increased ezetimibe exposure, monitor cyclosporine levels)
- Fibrates (especially gemfibrozil - increased risk of cholelithiasis and ezetimibe exposure; co-administration with gemfibrozil is not recommended)
Moderate Interactions
- Bile Acid Sequestrants (e.g., cholestyramine - decreased ezetimibe absorption; administer ezetimibe at least 2 hours before or 4 hours after a bile acid sequestrant)
- Warfarin (monitor INR when initiating or discontinuing ezetimibe)
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, 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, as statins can cause transaminase elevations.
Timing: Prior to initiation of therapy.
Routine Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Frequency: Periodically, typically 4-12 weeks after initiation or dose adjustment, then every 6-12 months.
Target: LDL-C reduction goals vary based on patient risk (e.g., <100 mg/dL, <70 mg/dL, or <55 mg/dL).
Action Threshold: If lipid goals are not met, consider dose adjustment of concomitant statin, addition of other lipid-lowering agents, or re-evaluation of therapy.
Liver Function Tests (ALT, AST)
Frequency: As clinically indicated, especially if co-administered with a statin. Routine monitoring of LFTs is generally not required for ezetimibe monotherapy.
Target: Within normal limits.
Action Threshold: If persistent elevations >3 times the upper limit of normal (ULN) occur, consider discontinuing ezetimibe or concomitant statin.
Creatine Kinase (CK)
Frequency: As clinically indicated (e.g., if muscle pain, tenderness, or weakness occurs).
Target: Within normal limits.
Action Threshold: If CK levels are significantly elevated (>10 times ULN) or if myopathy/rhabdomyolysis is suspected, discontinue ezetimibe and any concomitant statin.
Symptom Monitoring
- Unexplained muscle pain, tenderness, or weakness (myopathy/rhabdomyolysis)
- Dark urine
- Yellowing of skin or eyes (jaundice)
- Unusual fatigue or weakness
- Abdominal pain (especially if severe and persistent, could indicate cholelithiasis/cholecystitis if co-administered with fibrates)
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. If ezetimibe is administered with a statin, refer to the statin's prescribing information for pregnancy considerations, as statins are generally contraindicated in pregnancy.
Trimester-Specific Risks:
First Trimester:
Risk cannot be ruled out. Animal studies have shown adverse effects at maternally toxic doses.
Second Trimester:
Risk cannot be ruled out.
Third Trimester:
Risk cannot be ruled out.
Lactation
It is not known whether ezetimibe is excreted in human milk. Caution should be exercised when ezetimibe is administered to a nursing woman. If ezetimibe is administered with a statin, refer to the statin's prescribing information for lactation considerations, as statins are generally contraindicated during breastfeeding.
Infant Risk:
Risk cannot be ruled out. Potential for serious adverse reactions in the breastfed infant.
Pediatric Use
Approved for children âĨ10 years of age with heterozygous familial hypercholesterolemia (HeFH) or homozygous familial hypercholesterolemia (HoFH). Safety and effectiveness in children younger than 10 years have not been established.
Geriatric Use
No dosage adjustment is necessary for elderly patients. Efficacy and safety were similar in patients âĨ65 years of age compared to younger patients.
Clinical Information
Clinical Pearls
- Ezetimibe is a good option for patients who cannot tolerate statins or who need additional LDL-C lowering beyond what statins alone can achieve.
- It can be used as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin).
- Unlike statins, ezetimibe has minimal systemic exposure and is not metabolized by CYP450 enzymes, leading to fewer drug-drug interactions related to CYP inhibition.
- When co-administered with a bile acid sequestrant, ezetimibe should be taken at least 2 hours before or 4 hours after the sequestrant to avoid reduced absorption.
- While generally well-tolerated, monitor for muscle symptoms (myalgia, weakness) and liver enzyme elevations, especially when combined with a statin.
Alternative Therapies
- HMG-CoA Reductase Inhibitors (Statins): atorvastatin, rosuvastatin, simvastatin, pravastatin, lovastatin, fluvastatin, pitavastatin
- PCSK9 Inhibitors: alirocumab, evolocumab
- Bile Acid Sequestrants: cholestyramine, colestipol, colesevelam
- Fibrates: gemfibrozil, fenofibrate
- Niacin (Nicotinic Acid)
- Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors: bempedoic acid
- Selective Adenosine Triphosphate-Citrate Lyase (ACL) Inhibitors: bempedoic acid/ezetimibe (Nexlizet)
Cost & Coverage
Average Cost:
$10 - $30 per 30 tablets (generic ezetimibe 10mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic ezetimibe) on most commercial and Medicare Part D plans.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, 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. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.