Class: Beta-adrenergic blocking agent
- Tablets 50 mg
- Tablets 100 mg
- Injection 1 mg/mL
- Tablets 25 mg
- Tablets, ER 25 mg (metoprolol succinate 23.75 mg equivalent to metoprolol tartrate 25 mg)
- Tablets, ER 50 mg (metoprolol succinate 47.5 mg equivalent to metoprolol tartrate 50 mg)
- Tablets, ER 100 mg (metoprolol succinate 95 mg equivalent to metoprolol tartrate 100 mg)
- Tablets, ER 200 mg (metoprolol succinate 190 mg equivalent to metoprolol tartrate 200 mg)
Apo-Metoprolol SR (Canada)
Betaloc Durules (Canada)
Gen-Metoprolol (Type L) (Canada)
Sandoz Metoprolol (Type L) (Canada)
Blocks beta receptors, primarily affecting CV system (decreases heart rate, contractility, and BP) and lungs (promotes bronchospasm).
95% is absorbed; oral bioavailability is 40% to 50%.
12% is protein bound; rapidly enters the CNS, and has moderate lipid solubility.
Metabolized hepatically (primarily by CYP2D6).
Elimination is mainly by biotransformation in the liver. Approximately 95% excreted renally and less than 5% unchanged in urine. The half-life is 3 to 7 h.
Times to peak are 1 to 2 h (oral, regular), 6 to 12 h (oral, long-acting), and 20 min (IV).
Indications and Usage
Used alone or in combination with other antihypertensive agents for management of hypertension; long-term management of angina pectoris; MI (immediate-release tablets and injection); treatment of stable, symptomatic (New York Heart Association [NYHA] class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin ( Toprol XL only).
Acute coronary syndrome (ST-elevation MI, non–ST-elevation MI, and unstable angina); atrial fibrillation; prevention of migraine.
Greater than first-degree heart block; significant first-degree heart block (PR interval of 0.24 sec or longer); CHF unless secondary to tachyarrhythmia treatable with beta-blockers; overt or moderate to severe cardiac failure; sick sinus syndrome (unless a permanent pacemaker is in place); sinus bradycardia; cardiogenic shock; hypersensitivity to beta-blockers; systolic BP below 100 mm Hg; heart rate less than 45 bpm; severe peripheral arterial circulatory disorders; second- and third-degree heart block; pheochromocytoma.
Dosage and AdministrationHypertension
PO 100 mg/day in single or divided doses. Give 50 to 100 mg/day in a single-dose ER tablet.Maintenance
PO 100 to 450 mg/day.Children 6 to 16 yr of age Initial
PO 1 mg/kg once daily; max, 50 mg once daily.Maintenance
Up to 2 mg/kg (or 200 mg) once daily.Angina
PO 100 mg/day in 2 divided doses. 100 mg/day in a single-dose ER tablet.Maintenance
PO 100 to 400 mg/day.MI
IV bolus injection 5 mg slowly; may repeat every 2 min up to 15 mg. If tolerated, give PO 50 mg every 6 h beginning 15 min after last IV dose; continue for 48 h followed by PO 100 mg twice daily for 1 to 3 yr. If patient is intolerant of full IV dose, give PO 25 to 50 mg every 6 h starting 15 min after last IV dose.CHF
Adults ER tablet
PO Start with 25 mg daily for 2 wk in patients with NYHA class II heart failure and 12.5 mg daily in patients with more severe heart failure, then double the dose every 2 wk to highest dosage tolerated by patient (max, 200 mg).Off-label dosing
Acute coronary syndrome (ST-elevation MI, non–ST-elevation MI, and unstable angina)
5 mg by slow IV push at 5-min intervals to a total of 15 mg.Atrial fibrillation
2.5 mg to 5 mg IV bolus over 2 min, repeat every 5 min, up to 3 doses.Prevention of migraine Adults
PO 100 to 200 mg daily.
Store at 59° to 86°F and protect from light.
Bioavailability of metoprolol may decrease.Bupropion, diphenhydramine, fluoxetine, hydroxychloroquine, methimazole, paroxetine, propafenone, propylthiouracil, quinidine, ritonavir, terbinafine, thioridazine
Effects of metoprolol may increase.Cimetidine
May increase metoprolol levels.Clonidine
May enhance or reverse antihypertensive effect; potentially life-threatening situations may occur, especially on abrupt withdrawal of clonidine.Digitalis glycosides
Concomitant use may increase the risk of bradycardia.General anesthetics
May enhance the cardiodepressant effect of beta-blockers.Hydralazine
Serum levels of both drugs may increase.Lidocaine
Lidocaine levels may increase, leading to toxicity.NSAIDs
Some agents may impair antihypertensive effect.Prazosin
Orthostatic hypotension may increase.Rifampin
May decrease effects of metoprolol.Verapamil
Effects of both drugs may be increased.
Laboratory Test Interactions
Antinuclear antibodies may develop but are usually reversible on discontinuation.
Bradycardia, edema, flushing, hypotension (3%); arterial insufficiency; CHF; palpitations; peripheral edema.
Dizziness, fatigue, headache, sleepiness (10%); depression (5%); drowsiness; forgetfulness; lethargy; paresthesias; vertigo.
Pruritus, rash (5%); alopecia; facial erythema; urticaria.
Dry eyes; visual disturbances.
Diarrhea, nausea, vomiting (5%); constipation; dry mouth; flatulence; gastric pain; heartburn.
Difficulty with urination; impotence; urinary retention.
Shortness of breath (3%); bronchospasm; dyspnea; wheezing.
Asthenia; cold extremities; increased hypoglycemic response to insulin; may mask hypoglycemic signs; muscle cramps; systemic lupus erythematosus.
WarningsIschemic heart disease
In patients with angina pectoris or coronary artery disease (CAD), metoprolol may cause exacerbation of angina, occurrence of MI, and ventricular arrhythmias. Monitor patients closely because CAD is common and often unrecognized; it may be prudent not to discontinue beta-blocker therapy abruptly in patients being treated for hypertension.Bronchospastic disease
In general, do not give beta-blockers to patients with bronchospastic disease.Major surgery
The necessity of withdrawing beta-blocker therapy prior to surgery is controversial; the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.Diabetes and hypoglycemia
Use with caution in diabetic patients if a beta-blocker is required. Beta-blockers may mask tachycardia occurring with hypoglycemia, but other manifestations such as dizziness and sweating may not be significantly altered.Pheochromocytoma
Use is contraindicated in patients with pheochromocytoma.Thyrotoxicosis
Beta-blockers may mask certain clinical signs (eg, tachycardia) of hyperthyroidism. Carefully manage patients suspected of developing thyrotoxicosis to avoid abrupt withdrawal of beta blockade, which might precipitate a thyroid storm.
Category C .
Excreted in breast milk.
Safety and efficacy not established (immediate-release); safety and efficacy not established in children younger than 6 yr of age (ER).
While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic.
Use with caution; reduced daily dose is advised.
Deaths have occurred; aggressive therapy may be required.
Slows AV conduction and may cause heart block.
Metoprolol decreases heart rate in most patients.
Beta-blockers depress myocardial contractility and may precipitate or exacerbate cardiac failure.
Administer cautiously in CHF patients controlled by digitalis and diuretics.
Transient decreases in serum potassium levels may occur caused by intracellular shunting, which can produce adverse CV effects.
If systolic blood pressure decreases to 90 mm Hg or less, discontinue metoprolol.
Peripheral vascular disease
May precipitate or aggravate symptoms of atrial insufficiency.
Atrioventricular block, bradycardia, bronchospasm, cardiac arrest, cardiac failure, cardiogenic shock, cyanosis, hypotension, impairment of consciousness/coma, nausea, and vomiting.
- Teach patient how to check pulse and BP.
- Advise patient to contact health care provider if pulse is less than 50 bpm.
- Explain why medication should not be discontinued abruptly.
- Tell diabetic patient to check blood sugar regularly and consult health care provider if levels are unstable.
- Explain that adverse reactions are usually mild and transient and will generally subside with continued therapy.
- Instruct patient to report the following symptoms to health care provider: difficulty breathing, edema, night cough.
- Advise patient that drug may cause drowsiness and to use caution while driving or performing tasks requiring mental alertness.
Copyright © 2009 Wolters Kluwer Health.
More about metoprolol
- Metoprolol Succinate (AHFS Monograph)
- Metoprolol (FDA)
- Metoprolol Succinate (FDA)
- Metoprolol Tartrate Injection (FDA)