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metoprolol (Rx)Brand and Other Names:Lopressor, Toprol XL

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution (as tartrate)

  • 1mg/mL

tablet (as tartrate)

  • 25mg
  • 50mg
  • 100mg

tablet, extended-release (as succinate)

  • 25mg
  • 50mg
  • 100mg
  • 200mg
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Acute Myocardial Infarction

Early treatment

metoprolol tartrate (Lopressor)

  • 5 mg rapid IV q2min, up to 3 doses; then, 15 minutes after last IV, 50 mg PO q6hr for 48 hours; then 50-100 mg PO q12hr
  • If full IV dose not tolerated: 25-50 mg PO q6hr after last IV  

Congestive Heart Failure

metoprolol succinate (Toprol XL)

  • 25 mg PO qDay initially; increased every 2 weeks PRN; target dosage, 200 mg/day
  • New York Heart Association (NYHA) class ≥II: Reduce dosage 12.5 mg/day

Hypertension

metoprolol tartrate (Lopressor)

  • 100 mg/day PO initially in single dose or divided q12hr; may be increased at intervals of 1 week or longer; not to exceed 450 mg/day

metoprolol succinate (Toprol XL)

  • 25-100 mg PO qDay initially; may be increased at intervals of 1 week or longer; usual range, 50-100 mg/day; not to exceed 400 mg/day

Angina

metoprolol tartrate (Lopressor)

  • 100 mg/day PO initially divided q12hr; may be increased at intervals of 1 week or longer; not to exceed 400 mg/day

metoprolol succinate (Toprol XL)

  • 100 mg/day PO initially; may be increased at intervals of 1 week or longer; not to exceed 400 mg/day

Hyperthyroidism

25-50 mg PO q6hr

Acute Tachyarrhythmia (Off-label)

5 mg IV over 1-2 minutes q5min; total dose not to exceed 15 mg

Migraine (Off-label)

Prophylaxis

Metoprolol tartrate: 50-100 mg PO q12hr

Atrial Fibrillation/Flutter or Supraventricular Tachycardia (Off-label)

2.5-5 mg IV q2-5min; not to exceed 15 mg over 10-15 minutes; maintenance: 25-100 mg PO q12hr

Hepatic impairment

Consider initiating extended release tablet at doses lower than those recommended; gradually increase dosage to optimize therapy, while monitoring closely for adverse events

Dosing Considerations

In switching from immediate-release to extended-release, same total daily dose of metoprolol should be used

In switching between oral and IV dosage forms, equivalent beta-blocking effect is achieved in 2.5:1 (oral-to-IV) ratio

Take with or immediately following meals metoprolol tartrate: Take with or immediately after meals

Metoprolol succinate: Tablet should not be chewed or crushed

Dosing Modifications

Renal impairment: Dosage adjustment is not necessary

Hepatic impairment: Not studied; lower dosage may be necessary

Dosage Forms & Strengths

injectable solution (as tartrate)

  • 1mg/mL

tablet, immediate-release (as tartrate)

  • 25mg
  • 50mg
  • 100mg

tablet, extended-release (as succinate)

  • 25mg
  • 50mg
  • 100mg
  • 200mg
more...

Hypertension

metoprolol tartrate (Lopressor)

  • 1-17 years: 1-2 mg/kg/day PO divided BID; not to exceed 6 mg/kg/day or ≤200 mg/day 

metoprolol succinate (Toprol XL)

  • ≥6 years: 1 mg/kg PO qDay; not to exceed 50 mg/day initially; adjusted on basis of patient response; not to exceed 2 mg/kg/day or ≤200 mg/day

Use lower dosage in management of hypertension

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Interactions

Interaction Checker

metoprolol and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Dizziness (10%)

            Headache (10%)

            Tiredness (10%)

            Depression (5%)

            Diarrhea (5%)

            Pruritus (5%)

            Bradycardia (9%)

            Rash (5%)

            Dyspnea (1-3%)

            Cold extremities (1%)

            Constipation (1%)

            Dyspepsia (1%)

            Heart failure (1%)

            Hypotension (1%)

            Nausea (1%)

            Flatulence (1%)

            Heartburn (1%)

            Xerostomia (1%)

            Wheezing (1%)

            Bronchospasm (1%)

            Frequency Not Defined

            Decreased exercise tolerance

            Raynaud phenomenon

            Increased triglyceride levels and insulin resistance, decreased high-density lipoprotein (HDL) levels

            Postmarketing reports

            Anxiety/nervousness

            Hallusinations

            Paresthesia

            Hepatitis

            Vomiting

            Arthralgia

            Male impotence

            Reversible alopecia

            Agranulocytosis

            Dry eyes

            Worsening of psoriasis

            Pyronie’s disease

            Sweating

            Photosensitivity

            Taste disturbance

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            Warnings

            Black Box Warnings

            Ischemic heart disease may be exacerbated after abrupt withdrawal

            Hypersensitivity to catecholamines has been observed during withdrawal

            Exacerbation of angina and, in some cases, myocardial infarction (MI) may occur after abrupt discontinuance

            When long-term beta blocker therapy (particularly with ischemic heart disease) is discontinued, dosage should be gradually reduced over 1-2 weeks with careful monitoring

            If angina worsens markedly or acute coronary insufficiency develops, beta-blocker administration should be promptly reinitiated, at least temporarily (in addition to other measures appropriate for unstable angina)

            Patients should be warned against interruption or discontinuance of beta-blocker therapy without physician advice

            Because coronary artery disease (CAD) is common and may be unrecognized, beta-blocker therapy must be discontinued slowly, even in patients treated only for hypertension

            Contraindications

            Hypersensitivity

            Immediate release formulation

            • Hypertension and angina: Sinus bradycardia, 2°/3° heart block, cardiogenic shock, sick sinus syndrome (unless permanent pacemaker in place), severe peripheral vascular disease, pheochromocytoma
            • Myocardial infarction: Severe sinus bradycardia, heart rate <45 beats/min, systolic BP <100 mmHg, significant first-degree heart block ((PR interval at least 0.24 seconds), 2°/3° heart block, moderate-to-severe cardiac failure

            Extended release tablet

            • Second- and third-degree heart block, deompensated heart failure, sick sinus syndrome (except in patients with functioning artificial pacemaker), severe bradycardia, cardiogenic shock

            Cautions

            Use with caution in cerebrovascular insufficiency, CHF, cardiomegaly, myasthenia gravis, hyperthyroidism or thyrotoxicosis (may mask signs or symptoms), liver disease, renal impairment, peripheral vascular disease, psoriasis (may cause exacerbation of psoriasis)

            May exacerbate bronchospastic disease; monitor closely

            Beta blockers can cause myocardial depression and may precipitate heart failure and cardiogenic shock

            Sudden discontinuance can exacerbate angina and lead to MI and ventricular arrhythmias in patients with CAD

            Bradycardia, including sinus pause, heart block, and cardiac arrest, has been reported; patients with 1° atrioventricular block, sinus node dysfunction, or conduction disorders may be at increased risk

            Increased risk of stroke after surgery

            May potentiate hypoglycemia in patients with diabetes mellitus and may mask signs and symptoms

            Avoid starting high-dose regimen of extended-release metoprolol in patients undergoing noncardiac surgery; use in patients with cardiovascular risk factors is associated with bradycardia, hypotension, stroke, and death

            Long-term beta blockers should not be routinely withdrawn before major surgery; however, impaired ability of the heart to respond to reflex adrenergic stimuli may augment risks of general anesthesia and surgical procedures

            Metoprolol loses beta-receptor selectivity at high doses and in poor metabolizers

            If drug is administered for tachycardia secondary to pheochromocytoma, it should be given in combination with an alpha blocker (which should be started before metoprolol is started)

            While taking beta blockers, patients with history of severe anaphylactic reaction to variety of allergens may be more reactive to repeated challenge

            Worsening cardiac failure may occur during up-titration of beta-blockers; if such symptoms occur, increase diuretics and restore clinical stability

            Extended release tablet should not be withdrawn routinely prior to major surgery

            Hydrochlorothiazide, can cause an idiosyncratic reaction, resulting in acute transient myopia and acute angle-closure glaucoma, which can lead to permanent vision loss if not treated; discontinue hydrochlorothiazide as rapidly as possible if symptoms occur; prompt medical or surgical treatments may need to be considered if intraocular pressure remains uncontrolled; risk factors for developing acute angle-closure glaucoma may include history of sulfonamide or penicillin allergy

            Concomitant use of beta-blockers with digitalis glycosides, diltiazem, verapamil and clonidine can increase risk of bradycardia

            Caution in patients with history of psychiatric illness; may cause or exacerbate CNS depression

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Drug is concentrated in breast milk; use with caution (American Academy of Pediatrics states that drug is compatible with nursing)

            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

            Blocks response to beta-adrenergic stimulation; cardioselective for beta1 receptors at low doses, with little or no effect on beta2 receptors

            Absorption

            Bioavailability: Immediate release, 40-50%; extended release, 65-77% relative to immediate release

            Onset: 20 min (IV), when infused over 10 min; onset may be immediate, depending on clinical setting; 1-2 hr (PO)

            Duration: 3-6 hr (PO); duration is dose-related; 24 hr (ER); 5-8 hr (IV)

            Peak plasma time: Immediate release, 1.5-2 hr; extended release, 3.3 hr

            Therapeutic range: 35-212 ng/mL

            Distribution

            Protein bound: 10%

            Vd: 3.2-5.6 L/kg

            Metabolism

            Metabolized in liver by CYP2D6

            Metabolites: Inactive

            Elimination

            Half-life: 3-4 hr (average); 7.5 hr (poor metabolizers); 2.8 hr (extensive metabolizers)

            Excretion: Urine (95%)

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            Administration

            IV Compatibilities

            Solution: D5W, NS

            Y-site: Abciximab, alteplase, argatroban, meperidine, morphine sulfate

            IV Incompatibilities

            Y-site: Amphotericin B cholesteryl sulfate

            Storage

            Do not freeze

            Store at room temperature, and protect from light

            Discard solution if it is discolored or contains particles

            IV Administration

            Give undiluted by direct injection

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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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