pharmacopeia
GET
/api/v1/drug/ezetimibe
2D structure
(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
SMILES C1=CC(=CC=C1[C@@H]2[C@H](C(=O)N2C3=CC=C(C=C3)F)CC[C@@H](C4=CC=C(C=C4)F)O)O
InChIKey OLNTVTPDXPETLC-XPWALMASSA-N

Mechanism of action

Sourced from openFDA

Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols.

Indications

Sourced from openFDA
  • Ezetimibe tablets are indicated: • In combination with a statin, or alone when additional low-density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). • In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH.ICD-10: E78.00, E78.5

Contraindications

Sourced from openFDA
  • Ezetimibe tablets are contraindicated in patients with a known hypersensitivity to ezetimibe or any of the excipients in ezetimibe tablets. Hypersensitivity reactions including anaphylaxis, angioedema, rash, and urticaria have been reported [see Adverse Reactions (6.2) ].contraindicated

Dosage & administration

Sourced from openFDA

• The recommended dose of ezetimibe tablets is 10 mg orally once daily, administered with or without food. • If as dose is missed, take the missed dose as soon as possible. Do not double the next dose. • Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablets. • Administer ezetimibe tablets at least 2 hours before or 4 hours after administration of a bile acid sequestrant [see Drug Interactions (7) ]. • 10 mg orally once daily, with or without food ( 2 ) • Administer ezetimibe tablets either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant. ( 2 ) • Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablets. ( 2 )

Warnings & precautions

Sourced from openFDA

• Risks Associated with Combination Treatment 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. ( 5.1 ) • Liver Enzyme Abnormalities and Monitoring : Increases in serum transaminases have been reported with use of ezetimibe. Perform liver enzyme testing as clinically indicated and consider withdrawal of ezetimibe if increases in ALT or AST ≥3 X ULN persist. ( 5.2 ) • Skeletal Muscle Effects (e.g., Myopathy and Rhabdomyolysis) : Ezetimibe may cause myopathy 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 ezetimibe and other concomitant medications, as appropriate. ( 5.3 ) 5.1 Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies If ezetimibe 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 [see Contraindications (4) ]. 5.2 Liver Enzymes Increases in serum transaminases have been reported with use of ezetimibe [see Adverse Reactions (6.1) ].

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed in greater detail in other sections of the label: • Liver enzyme abnormalities [see Warnings and Precautions (5.2) ] • Rhabdomyolysis and myopathy [see Warnings and Precautions (5.3) ] • Common adverse reactions in clinical trials: o Ezetimibe administered alone (incidence ≥2% and greater than placebo): upper respiratory tract infection, diarrhea, arthralgia, sinusitis, pain in extremity, fatigue, and influenza. ( 6.1 ) o Ezetimibe coadministered with a statin (incidence ≥2% and greater than statin alone): nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, diarrhea, back pain, influenza, pain in extremity, and fatigue. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in clinical practice. Monotherapy In 10 double-blind, placebo-controlled clinical trials, 2,396 patients with primary hyperlipidemia (age range 9 to 86 years; 50% female, 90% White, 5% Black or African American, 2% Asian, 3% other races; 3% identified as Hispanic or Latino ethnicity) and elevated LDL-C were treated with ezetimibe 10 mg daily for a median treatment duration of 12 weeks (range 0 to 39 weeks).

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary There are insufficient data on ezetimibe use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed in pregnant rats and rabbits orally administered ezetimibe during the period of organogenesis at doses that resulted in up to 10 and 150 times, respectively, the human exposure at the MRHD, based on AUC (see Data) . Ezetimibe should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. When ezetimibe is administered with a statin, refer to the Prescribing Information for the statin. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In oral (gavage) embryo-fetal development studies of ezetimibe conducted in rats (gestation days 6-15) and rabbits (gestation days 7-19), there was no evidence of maternal toxicity or embryolethal effects at the doses tested (250, 500, 1,000 mg/kg/day).

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide (ezetimibe-glucuronide). After a single 10 mg dose of ezetimibe to fasted adults, mean ezetimibe peak plasma concentrations (C max) of 3.4 to 5.5 ng/mL were attained within 4 to 12 hours (T max ).

Overdosage

Sourced from openFDA

In the event of overdose, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.

Approval history

Sourced from openFDA
  • Oct 25, 2002NDANDA021445Organon
  • Jul 23, 2004NDANDA021687Organon
  • Jun 26, 2015ANDAANDA078560Glenmark Pharms Ltd
  • Apr 26, 2017ANDAANDA200909Dr Reddys Labs Sa
  • Jun 12, 2017ANDAANDA203931Sandoz
  • Jun 12, 2017ANDAANDA204331Zydus Pharms
  • Jun 12, 2017ANDAANDA200831Watson Labs Inc
  • Feb 26, 2020NDANDA211617Esperion Theraps Inc

FDA shortages

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Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Ezetimibe, Tablet, 10 mg (NDC 0591-3713-05)To be discontinued
    Sponsor: Actavis Pharma, Inc.
    Updated
  • Ezetimibe, Tablet, 10 mg (NDC 0591-3713-19)To be discontinued
    Sponsor: Actavis Pharma, Inc.
    Updated
  • Ezetimibe, Tablet, 10 mg (NDC 0591-3713-30)To be discontinued
    Sponsor: Actavis Pharma, Inc.
    Updated

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
87,705 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue5,5686.3%
  2. 2Nausea5,3096.1%
  3. 3Myalgia5,0725.8%
  4. 4Drug Ineffective4,4275.0%
  5. 5Diarrhoea4,4195.0%
  6. 6Dizziness4,1874.8%
  7. 7Dyspnoea4,0014.6%
  8. 8Headache3,8394.4%
  9. 9Arthralgia3,5154.0%
  10. 10Pain3,5144.0%
  11. 11Asthenia3,4403.9%
  12. 12Pain In Extremity2,9493.4%
  13. 13Fall2,8353.2%
  14. 14Vomiting2,7853.2%
  15. 15Malaise2,6043.0%

Literature

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Recent PubMed references pinned to Ezetimibe as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 480 ClinicalTrials.gov registrations naming Ezetimibe as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Ezetimibe work?
Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols.
What is Ezetimibe used for?
According to FDA labeling, Ezetimibe carries indications including: Ezetimibe tablets are indicated: • In combination with a statin, or alone when additional low-density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). • In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Ezetimibe?
Ezetimibe is classified as Other lipid modifying agents, Dietary Cholesterol Absorption Inhibitor, Mechanism of Action, Decreased Cholesterol Absorption.
What are the brand names for Ezetimibe?
Ezetimibe is marketed under brand names including Nexlizet, Roszet, Vytorin, Zetia.
What are the contraindications for Ezetimibe?
Ezetimibe labeling lists contraindications including: Ezetimibe tablets are contraindicated in patients with a known hypersensitivity to ezetimibe or any of the excipients in ezetimibe tablets. Hypersensitivity reactions including anaphylaxis, angioedema, rash, and urticaria have been reported [see Adverse Reactions (6.2) ].. Always consult the full prescribing information and a clinician.
Note. Data for ezetimibe is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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