metoprolol (Rx)

Brand and Other Names:Lopressor, Toprol XL, more...Kapspargo Sprinkle
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution (Lopressor [as tartrate])

  • 1mg/mL

injectable solution (Lopressor [as tartrate])

  • 25mg
  • 50mg
  • 100mg

tablet, extended-release (Toprol XL [as succinate])

  • 25mg
  • 50mg
  • 100mg
  • 200mg

capsule, extended-release (Kapspargo Sprinkle [as succinate]))

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

Hypertension

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

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

Kapspargo Sprinkles

  • Initial dose: 25-100 mg PO qDay in a single dose; adjust dosage at weekly (or longer) intervals until optimum blood pressure reduction is achieved
  • Dosages above 400 mg/day not studied

Acute Myocardial Infarction

Early treatment

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

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

Kapspargo Sprinkle

  • Prior to initiation, stabilize dose of other heart failure drug therapy and ensure patient is not fluid overloaded
  • Initial dose: 25 mg PO qDay for 2 weeks
  • Not suitable for initial therapy in patients who are expected to require a starting dose less than 25 mg/day
  • Individualize dose and closely monitor during up-titration; double dose q2Weeks to the highest dosage level tolerated or up to 200 mg

Angina

Lopressor

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

Toprol XL

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

Kapspargo Sprinkle

  • Usual initial dose: 100 mg PO qDay, given in a single dose; gradually increase dose at weekly intervals until optimum clinical response is achieved or there is a pronounced slowing of the heart rate
  • Dosages above 400 mg/day have not been studied
  • If treatment is to be discontinued, gradually reduce dose over a period of 1-2 weeks

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

Dosing Modifications

Lopressor

  • Renal impairment: No dosage adjustment necessary; systemic availability and half-life in patients with renal failure do not differ to a clinically significant degree from those in normal subjects
  • Hepatic impairment: Since drug is primarily eliminated by hepatic metabolism, hepatic impairment may impact the pharmacokinetics of metoprolol; elimination half-life of metoprolol is considerably prolonged, depending on severity (up to 7.2 h)

Kapspargo Sprinkle

  • If a patient experiences symptomatic bradycardia, reduce dose
  • If transient worsening of heart failure occurs, consider treating with increased doses of diuretics, lower dose or temporarily discontinuing treatment
  • Do not increase until symptoms of worsening heart failure have been stabilized
  • Initial difficulty with titration should not preclude later attempts to introduce Kapspargo Sprinkle
  • or patients who are taking metoprolol succinate ER tablets at a dose of 25-200 mg PO qDay, substitute ER capsules for ER tablets, using the same total daily dose of metoprolol succinate

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

Dosage Forms & Strengths

injectable solution (Lopressor [as tartrate])

  • 1mg/mL

injectable solution (Lopressor [as tartrate])

  • 25mg
  • 50mg
  • 100mg

tablet, extended-release (Toprol XL [as succinate])

  • 25mg
  • 50mg
  • 100mg
  • 200mg

capsule, extended-release (Kapspargo Sprinkle [as succinate]))

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

Hypertension

Lopressor

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

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

Kapspargo Sprinkle

  • <6 years: Safety and efficacy not established
  • ≥6 years: 1 mg/kg PO qDay, do not exceed 50 mg PO qDay; adjust dosage according to blood pressure response
  • Doses >2 mg/kg (or >200 mg) qDay not studied

Use lower dosage in management of hypertension

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Interactions

Interaction Checker

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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

            Lopressor and Toprol XL only

            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

            Lopressor

            • 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

            Toprol XL

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

            Kapspargo Sprinkle

            • Severe bradycardia, second or third degree heart block, cardiogenic shock, decompensated heart failure, sick sinus syndrome (unless a permanent pacemaker is in place), and in patients who are hypersensitive to any component of this product

            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

            Worsening cardiac failure may occur during up-titration of metoprolol succinate; if such symptoms occur, increase diuretics and restore clinical stability before advancing the dose of metoprolol succinate; it may be necessary to lower the dose of metoprolol succinate or temporarily discontinue it

            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

            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

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

            Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease

            Drug interactions overview

            • Catecholamine depleting drugs (eg, reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents; monitor when coadministration with catecholamine depleting drugs for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension
            • While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction
            • Drugs that are strong inhibitors of CYP2D6, such as quinidine, fluoxetine, paroxetine, and propafenone, were shown to double metoprolol concentrations; no information about moderate or weak inhibitors, but are likely to increase metoprolol concentration; closely monitor patients when the combination cannot be avoided
            • Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate
            • Concomitant administration of hydralazine may inhibit presystemic metabolism of metoprolol leading to increased concentrations of metoprolol
            • Concomitant use with beta blockers can increase the risk of bradycardia; if clonidine and a beta blocker, such as metoprolol are coadministered, withdraw the beta-blocker several days before the gradual withdrawal of clonidine because beta-blockers may exacerbate the rebound hypertension that can follow the withdrawal of clonidine
            • If replacing clonidine by beta-blocker therapy, delay introduction of beta-blockers for several days after clonidine administration has stopped
            • Metoprolol succinate is released faster from Kapspargo Sprinkle in the presence of alcohol; may increase the risk for adverse events associated with Kapspargo Sprinkle
            • Avoid alcohol consumption
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies in pregnant women

            The amount of data on the use of metoprolol in pregnant women is limited

            Risk to the fetus/mother is unknown; because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed

            Animal data

            • Lopressor has been shown to increase postimplantation loss and decrease neonatal survival in rats at doses up to 11 times the maximum daily human dose of 450 mg, when based on surface area
            • Distribution studies in mice confirm exposure of the fetus when Lopressor is administered to the pregnant animal
            • These limited animal studies do not indicate direct or indirect harmful effects with respect to teratogenicity

            Fertility

            • The drug effects on the fertility of human have not been studied
            • Lopressor showed effects on spermatogenesis in male rats at a therapeutic dose level, but had no effect on rates of conception at higher doses in animal fertility studies

            Lactation

            Lopressor is excreted in breast milk in a very small quantity

            An infant consuming 1 liter of breast milk daily would receive a dose of less than 1 mg of the drug

            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.

            more...
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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

            IV Administration

            Give undiluted by direct injection

            Oral Administration

            Kapspargo Sprinkle

            • Swallow whole
            • For patients unable to swallow an intact capsule, alternative administration options are available
            • Directions for use with soft food (applesauce, pudding, or yogurt)
              • Open capsule and sprinkle contents soft food
              • Contents of the capsules should be swallowed along with a small amount (teaspoonful) of soft food (such as applesauce, pudding, or yogurt)
              • Drug/food mixture should be swallowed within 60 minutes and not stored for future use

            Nasogastric tube administration

            Kapspargo Sprinkle

            • Open and add contents of capsule to an all plastic oral tip syringe and add 15 mL of water
            • Gently shake the syringe for ~10 seconds
            • Promptly deliver through a 12 French or larger nasogastric tube
            • Ensure no granules are left in the syringe
            • Rinse with additional water if needed

            Storage

            Do not freeze

            Lopressor

            • Tablets: Store at room temperature
            • Unused vials: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F); protect from light and heat

            Kapspargo Sprinkle

            • Store at 20- 25°C (68-77°F)
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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            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.