Dosing & Uses
Dosage Forms & Strengths
injectable solution (as tartrate)
- 1mg/mL
tablet (as tartrate)
- 25mg (generic)
- 50mg (generic, Lopressor)
- 100mg (generic, Lopressor)
tablet, extended-release (Toprol XL [as succinate])
- 25mg
- 50mg
- 100mg
- 200mg
capsule, extended-release (Kapspargo Sprinkle [as succinate])
- 25mg
- 50mg
- 100mg
- 200mg
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 hr)
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
Switching from immediate-release to extended-release: Use same total daily dose of metoprolol
Switching between oral and IV dosage forms: Equivalent beta-blocking effect is achieved in 2.5:1 (oral-to-IV) ratio
Dosage Forms & Strengths
injectable solution (as tartrate)
- 1mg/mL
tablet (as tartrate)
- 25mg (generic)
- 50mg (generic, Lopressor)
- 100mg (generic, Lopressor)
tablet, extended-release (Toprol XL [as succinate])
- 25mg
- 50mg
- 100mg
- 200mg
capsule, extended-release (Kapspargo Sprinkle [as succinate])
- 25mg
- 50mg
- 100mg
- 200mg
Hypertension
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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
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
Pregnancy & Lactation
Pregnancy
There are no adequate and well-controlled studies in pregnant women
Limited data on the use of metoprolol in pregnant women
Risk to fetus/mother is unknown; because animal reproduction studies are not always predictive of human response, use 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
- 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.
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: 40-50% (immediate-release) ; 65-77% (extended-release) 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: 1.5-2 hr (immediate-release); 3.3 hr (extended-release)
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%)
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
Metoprolol tartrate: Take with or immediately after meals
Metoprolol succinate: Tablet should not be chewed or crushed
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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Patient Handout
Formulary
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