Dosing & Uses
Dosage Forms & Strengths
tablets
- 10mg
Homozygous Familial Hypercholesterolemia
10 mg PO qDay in combination with atorvastatin or simvastatin
Homozygous Sitosterolemia
10 mg PO qDay adjunctive to diet
Primary Hyperlipidemia
10 mg PO qDay in combination with HMG-CoA reductase inhibitors adjunctive to diet
Dosing Considerations
Overdose management: Treatment should be supportive
Dosing Modifications
Renal impairment
- Monotherapy: No dosage adjustment required
- Moderate to severe: Renal impairment is a risk factor for statin-associated myopathy; caution when coadministered with doses of simvastatin exceeding 20 mg
Hepatic impairment
- Mild (Child-Pugh class A): Dose adjustment not necessary
- Moderate to severe (Child-Pugh class B or C): Not recommended
Dosage Forms & Strengths
tablets
- 10mg
Homozygous Familial Hypercholesterolemia
<10 years: Safety and efficacy not established
>10 years: 10 mg PO qDay in combination with atorvastatin or simvastatin
Homozygous Sitosterolemia
<10 years: Safety and efficacy not established
>10 years: 10 mg PO qDay adjunctive to diet
Primary Hyperlipidemia
<10 years: Safety and efficacy not established
>10 years: 10 mg PO qDay in combination with HMG-CoA reductase inhibitors adjunctive to diet
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (4)
- cyclosporine
cyclosporine, ezetimibe. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Monitor for potential adverse effects of cyclosporine and ezetimibe if coadministered, especially in patients with severe renal impairment.
- leniolisib
leniolisib will increase the level or effect of ezetimibe by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, an OATP1B1 and OATP1B3 inhibitor, may increase systemic exposure of these substrates
- trofinetide
trofinetide will increase the level or effect of ezetimibe by Other (see comment). Avoid or Use Alternate Drug. Trofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.
- zavegepant intranasal
ezetimibe will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
Monitor Closely (7)
- apalutamide
apalutamide will decrease the level or effect of ezetimibe by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and weakly induces OATP1B1 and may decrease systemic exposure of drugs that are substrates of both UGT and OATP1B1.
- cholestyramine
cholestyramine decreases levels of ezetimibe by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2-4 hours.
- encorafenib
encorafenib will increase the level or effect of ezetimibe by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a OATP1B1 inhibitor) may increase the concentration and toxicities of OATP1B1 substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.
- fostemsavir
fostemsavir will increase the level or effect of ezetimibe by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 transporter. If possible, avoid coadministration or modify dose of OATP1B1/3 substrates coadministered with fostemsavir.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of ezetimibe by Other (see comment). Use Caution/Monitor. Coadministration with glecaprevir/pibrentasvir may increase plasma concentration of drugs that are substrates of OATP1B1 or OATP1B3
- letermovir
letermovir increases levels of ezetimibe by Other (see comment). Use Caution/Monitor. Comment: Letermovir, an OATP1B1/3 inhibitor may increase plasma concentrations of coadministered OATP1B1/3 substrates.
- sofosbuvir/velpatasvir
sofosbuvir/velpatasvir increases levels of ezetimibe by Other (see comment). Use Caution/Monitor. Comment: Velpatasvir inhibits OATP1B1, OATP1B3, and OATP2B1 transporters. .
Minor (5)
- fenofibrate
fenofibrate increases levels of ezetimibe by unspecified interaction mechanism. Minor/Significance Unknown.
- fenofibrate micronized
fenofibrate micronized increases levels of ezetimibe by unspecified interaction mechanism. Minor/Significance Unknown.
- fenofibric acid
fenofibric acid increases levels of ezetimibe by unspecified interaction mechanism. Minor/Significance Unknown.
- gemfibrozil
gemfibrozil increases levels of ezetimibe by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- voclosporin
voclosporin will increase the level or effect of ezetimibe by Other (see comment). Minor/Significance Unknown. Information suggests voclosporin (an OATP1B1 inhibitor) may increase in the concentration of OATP1B1 substrates is possible. Monitor for adverse reactions of OATP1B1 substrates when coadministered with voclosporin.
Adverse Effects
1-10%
Diarrhea (4%)
Upper respiratory tract symptoms (2-4%)
Cough (2-4%)
Pain in extremity (3%)
Sinusitis (3%)
Arthralgia (2-3%)
Fatigue (2%)
Influenza (2%)
Increased liver transaminases (with HMG-CoA reductase inhibitors; ≥3 x ULN; 1%)
Postmarketing Reports
Hepatitis/liver function test abnormalities (LFTs elevated slightly higher in combination with statin than with statin alone)
Hypersensitivity reactions (including anaphylaxis, angioedema, rash, urticaria)
Erythema multiforme
Elevated creatine phosphokinase
Myopathy/rhabdomyolysis
Thrombocytopenia
Back pain
Abdominal pain
Pancreatitis
Nausea
Dizziness
Paresthesia
Depression
Headache
Cholelithiasis and cholecystitis
Warnings
Contraindications
Hypersensitivity
Coadministration with a statin in the presence of active liver disease or persistent, unexplained elevations of hepatic transaminase levels
Patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated
Cautions
If this drug is administered with a statin, fenofibrate, or other LDL-C lowering therapies, refer to the prescribing information of these products for a description of their risks including, but not limited to, the warnings and precautions
Elevated hepatic transaminases (≥3 X ULN) reported with concomitant use of statins compared to statin monotherapy; consider discontinuation of therapy (ezetimibe and/or statin) for persistently elevated transaminases (ALT or AST (≥3 X ULN); perform liver enzyme testing as clinically indicated
Therapy may cause myopathy [muscle pain, tenderness, or weakness associated with elevated creatine kinase (CK)] and rhabdomyolysis; in post-marketing reports, most patients who developed rhabdomyolysis were taking a statin or other agents known to be associated with an increased risk of rhabdomyolysis, such as fibrates; if myopathy is suspected, discontinue therapy and other concomitant medications, as appropriate
Hepatic impairment may increase systemic exposure; use with caution in patients with mild hepatic impairment (Child-Pugh class A); use not recommended in patients with moderate to severe hepatic impairment (Child-Pugh classes B and C)
Use with caution in patients with severe renal impairment (CrCl ≤30 mL/min/1.73 m²); if using concurrent simvastatin in patients with moderate to severe renal impairment (CrCl<60 mL/min/1.73 m²) use caution with simvastatin doses exceeding 20 mg; monitor for adverse events
Cholelithiasis reported (when coadministered with fibric acid derivatives)
Rule out secondary causes of hyperlipidemia prior to therapy
Pregnancy & Lactation
Pregnancy category: C
Lactation: Excretion in milk unknown; use with caution
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits sterol transporter at brush border and, consequently, intestinal absorption of cholesterol, which in turn decreases delivery of cholesterol to the liver and reduces hepatic cholesterol stores
Absorption
Bioavailability: Variable
Peak plasma time: 4-12 hr (parent drug); 1-2 hr (metabolite)
Peak plasma concentration: 3.4-5.5 ng/mL (parent drug); 45-71 ng/mL (metabolite)
Distribution
Protein bound: >90%
Metabolism
Metabolized by glucuronide conjugation
Metabolites: Ezetimibe-glucuronide (80-90%)
Elimination
Half-life: 22 hr
Excretion: Bile (78%), urine (11%)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| ezetimibe oral - | 10 mg tablet |  | |
| Zetia oral - | 10 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
ezetimibe oral
EZETIMIBE - ORAL
(eh-ZET-ih-mibe)
COMMON BRAND NAME(S): Zetia
USES: Ezetimibe is used along with a low cholesterol/low fat diet and exercise to help lower cholesterol in the blood. Ezetimibe may be used alone or with other drugs (such as "statins" or fibrates). Ezetimibe works by reducing the amount of cholesterol your body absorbs from your diet. Reducing cholesterol may help prevent strokes and heart attacks.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking ezetimibe and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually once daily with or without food.The dosage is based on your medical condition and response to treatment.If taking a bile acid sequestrant (such as cholestyramine, colestipol), take ezetimibe at least 2 hours before or 4 hours after taking the bile acid sequestrant. These products may bind to ezetimibe, preventing your body from fully absorbing the drug.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Keep taking this medication even if you feel well. Most people with high cholesterol do not feel sick. It may take up to 2 weeks before you get the full benefit of this drug.
SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This drug may increase the risk of liver damage (when taken with a "statin") or muscle damage when taken with a fibrate or "statin". Tell your doctor right away if you experience any of the following symptoms: signs of liver problems (such as nausea/vomiting that doesn't stop, severe stomach/abdominal pain, yellowing eyes/skin, dark urine), muscle pain/tenderness/weakness (especially with fever or unusual tiredness).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking ezetimibe, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as cholesterol levels, liver function) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised July 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
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Adding plans allows you to:
- View the formulary and any restrictions for each plan.
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- Compare formulary status to other drugs in the same class.
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