ezetimibe (Rx)

Brand and Other Names:Zetia
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and ezetimibe

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

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            Warnings

            Contraindications

            Hypersensitivity

            Coadministration with a statin in the presence of active liver disease or persistent, unexplained elevations of hepatic transaminase levels

            Cautions

            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)

            Myopathy, including rhabdomyolysis reported with monotherapy (rare); risk increased with concomitant use of statin or fibrate immediately if myopathy suspected or confirmed (symptomatic patient with CPK >10 X ULN)

            Hepatic impairment may increase systemic exposure; use with caution in patient swith 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

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            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.

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            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%)

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.