Classes
DEA Class; Rx
Common Brand Names; Lopressor, Toprol XL, Kapspargo Sprinkle
- Beta-Blockers, Beta-1 Selective
Description
Competitive, beta-1-selective beta-blocker; oral and IV formulations; similar to atenolol; lacks intrinsic sympathomimetic and membrane-stabilizing activities; more lipophilic than atenolol, but less than propranolol and betaxolol.
Indications
Indicated for the treatment of angina pectoris.
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
Adverse Effects
- 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%)
- Decreased exercise tolerance
- Raynaud phenomenon
- Increased triglyceride levels and insulin resistance, decreased high-density lipoprotein (HDL) levels
Warnings
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
Pregnancy and Lactation
Untreated hypertension and heart failure during pregnancy increases maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (eg, need for cesarean section, and post-partum hemorrhage)
Limited available data from published literature report that metoprolol is present in human milk; the estimated daily infant dose of metoprolol received from breastmilk ranges from 0.05 mg to less than 1 mg; the estimated relative infant dosage was 0.5% to 2% of the mother’s weight-adjusted dosage; no adverse reactions of metoprolol on the breastfed infant have been identified; there is no information regarding the effects of metoprolol on milk production
Monitor breastfed infant for bradycardia and other symptoms of beta-blockade such as listlessness (hypoglycemia)
Maximum Dosage
400 mg/day PO for extended-release tablets or 450 mg/day PO for immediate-release tablets.
400 mg/day PO for extended-release tablets or 450 mg/day PO for immediate-release tablets.
2 mg/kg/day PO (Max: 200 mg/day) of extended-release metoprolol for hypertension. Safety and efficacy of intravenous or oral immediate-release metoprolol have not been established. However, up to 6 mg/kg/day PO (Max: 200 mg/day) of the immediate-release tablets has been used off-label for hypertension; up to 2.4 mg/kg/day PO has been used off-label for heart failure.
6 to 12 years: 2 mg/kg/day PO (Max: 200 mg/day) of extended-release metoprolol for hypertension. Safety and efficacy of intravenous or oral immediate-release metoprolol have not been established. However, up to 6 mg/kg/day PO (Max: 200 mg/day) of the immediate-release tablets has been used off-label for hypertension; up to 2.4 mg/kg/day PO has been used off-label for heart failure.
1 to 5 years: Safety and efficacy have not been established. However, up to 6 mg/kg/day PO (Max: 200 mg/day) of the immediate-release tablets has been used off-label for hypertension; up to 2.4 mg/kg/day PO has been used off-label for heart failure.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Metoprolol
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
