Metoprolol

Name: Metoprolol

Metoprolol and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

Metoprolol has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from metoprolol, a choice should be made whether to stop nursing or to stop use of this medication. The importance of the drug to the mother should be considered.

Metoprolol Overdose

If you take too much metoprolol, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

Metoprolol FDA Warning

Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered metoprolol, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 - 2 weeks and the patient should be carefully monitored. If angina markedly worsens or acute coronary insufficiency develops, metoprolol administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken. Warn patients against interruption or discontinuation of therapy without the physician’s advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue metoprolol therapy abruptly even in patients treated only for hypertension

Metoprolol Description

Metoprolol tartrate is a selective beta 1-adrenoreceptor blocking agent, available as 25 mg, 50 mg, and 100 mg tablets for oral administration. Metoprolol tartrate is (±)-1-(isopropylamino)-3-[ p-2-methoxyethyl)phenoxy]-2-propanol (2:1) dextro-tartrate salt. Its structural formula is:

Metoprolol tartrate, USP is a white, practically odorless, crystalline powder with a molecular weight of 684.82. It is very soluble in water; freely soluble in methylene chloride, in chloroform, and in alcohol; slightly soluble in acetone; and insoluble in ether.

Each tablet for oral administration contains 25 mg, 50 mg, or 100 mg of Metoprolol tartrate and the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, povidone, sodium lauryl sulfate, titanium dioxide and triacetin. In addition, the 50 mg product contains FD&C Blue No. 2 Aluminum Lake, D&C Red No. 27 Aluminum Lake and FD&C Red No. 40 Aluminum Lake and the 100 mg product contains FD&C Blue No. 2 Aluminum Lake as coloring agents.

Adverse Reactions

Hypertension and Angina

Most adverse effects have been mild and transient.

Central Nervous System

Tiredness and dizziness have occurred in about 10 of 100 patients. Depression has been reported in about 5 of 100 patients. Mental confusion and short-term memory loss have been reported. Headache, nightmares, and insomnia have also been reported.

Cardiovascular

Shortness of breath and bradycardia have occurred in approximately 3 of 100 patients. Cold extremities; arterial insufficiency, usually of the Raynaud type; palpitations; congestive heart failure; peripheral edema; and hypotension have been reported in about 1 of 100 patients. Gangrene in patients with preexisting severe peripheral circulatory disorders has also been reported very rarely (see CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS).

Respiratory

Wheezing (bronchospasm) and dyspnea have been reported in about 1 of 100 patients (see WARNINGS). Rhinitis has also been reported.

Gastrointestinal

Diarrhea has occurred in about 5 of 100 patients. Nausea, dry mouth, gastric pain, constipation, flatulence, and heartburn have been reported in about 1 of 100 patients. Vomiting was a common occurrence. Post-marketing experience reveals very rare reports of hepatitis, jaundice and nonspecific hepatic dysfunction. Isolated cases of transaminase, alkaline phosphatase, and lactic dehydrogenase elevations have also been reported.

Hypersensitive Reactions

Pruritus or rash have occurred in about 5 of 100 patients. Very rarely, photosensitivity and worsening of psoriasis has been reported.

Miscellaneous

Peyronie’s disease has been reported in fewer than 1 of 100,000 patients. Musculoskeletal pain, blurred vision, and tinnitus have also been reported.

There have been rare reports of reversible alopecia, agranulocytosis, and dry eyes. Discontinuation of the drug should be considered if any such reaction is not otherwise explicable. There have been very rare reports of weight gain, arthritis, and retroperitoneal fibrosis (relationship to Metoprolol has not been definitely established).

The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with Metoprolol.

Myocardial Infarction

Central Nervous System

Tiredness has been reported in about 1 of 100 patients. Vertigo, sleep disturbances, hallucinations, headache, dizziness, visual disturbances, confusion, and reduced libido have also been reported, but a drug relationship is not clear.

Cardiovascular

In the randomized comparison of Metoprolol and placebo described in the CLINICAL PHARMACOLOGY section, the following adverse reactions were reported:

 

Metoprolol

Placebo

Hypotension (systolic BP < 90 mm Hg)

27.4%

23.2%

Bradycardia (heart rate < 40 beats/min)

15.9%

6.7%

Second- or third-degree heart block

4.7%

4.7%

First-degree heart block (P-R ≥ 0.26 sec)

5.3%

1.9%

Heart failure

27.5%

29.6%

Respiratory

Dyspnea of pulmonary origin has been reported in fewer than 1 of 100 patients.

Gastrointestinal

Nausea and abdominal pain have been reported in fewer than 1 of 100 patients.

Dermatologic

Rash and worsened psoriasis have been reported, but a drug relationship is not clear.

Miscellaneous

Unstable diabetes and claudication have been reported, but a drug relationship is not clear.

Potential Adverse Reactions

A variety of adverse reactions not listed above have been reported with other beta-adrenergic blocking agents and should be considered potential adverse reactions to Metoprolol.

Central Nervous System

Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics.

Cardiovascular

Intensification of AV block (see CONTRAINDICATIONS).

Hematologic

Agranulocytosis, nonthrombocytopenic purpura and thrombocytopenic purpura.

Hypersensitive Reactions

Fever combined with aching and sore throat, laryngospasm and respiratory distress.

Post-Marketing Experience

The following adverse reactions have been reported during post-approval use of Metoprolol: confusional state, an increase in blood triglycerides and a decrease in High Density Lipoprotein (HDL). Because these reports are from a population of uncertain size and are subject to confounding factors, it is not possible to reliably estimate their frequency.

How supplied

Metoprolol Tartrate Tablets, USP are available containing 25 mg, 50 mg, or 100 mg of Metoprolol tartrate, USP.

The 25 mg tablets are white film-coated, round, scored tablets debossed with M over 18 on one side of the tablet and scored on the other side. They are available as follows:

NDC 51079-255-20 – Unit dose blister packages of 100 (10 cards of 10 tablets each).

The 50 mg tablets are pink film-coated, round, scored tablets debossed with M over 32 on one side of the tablet and scored on the other side. They are available as follows:

NDC 51079-801-20 – Unit dose blister packages of 100 (10 cards of 10 tablets each).

The 100 mg tablets are light blue film-coated, round, scored tablets debossed with M over 47 on one side of the tablet and scored on the other side. They are available as follows:

NDC 5179-802-20 – Unit dose blister packages of 100 (10 cards of 10 tablets each).

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]
Protect from light and moisture.

To report SUSPECTED ADVERSE REACTIONS, contact Mylan Pharmaceuticals Inc. at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Manufactured by:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Distributed by:
Mylan Institutional Inc.
Rockford, IL 61103 U.S.A.

S-11093 R3
9/15

PRINCIPAL DISPLAY PANEL - 25 mg

NDC 51079-255-20

Metoprolol
Tartrate
Tablets, USP
25 mg

100 Tablets (10 x 10)

Each film-coated tablet contains:
Metoprolol tartrate, USP . . . .   25 mg

Usual Dosage: See accompanying
prescribing information.

Store at 20° to 25°C (68° to 77°F).
[See USP Controlled Room Temperature.]
Protect from light and moisture.

Manufactured by:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Rx only

S-8561 R4

Packaged and Distributed by:

Mylan Institutional Inc.

Rockford, IL 61103 U.S.A.

This unit dose package is not child resistant.

For institutional use only.

Keep this and all drugs out of the reach of children.

This container provides light-resistance.

See window for lot number and expiration date.

PRINCIPAL DISPLAY PANEL - 50 mg

NDC 51079-801-20

Metoprolol
Tartrate
Tablets, USP
50 mg

100 Tablets (10 x 10)

Each film-coated tablet contains:
Metoprolol tartrate, USP . . . . 50 mg

Usual Dosage: See accompanying
prescribing information.

Store at 20° to 25°C (68° to 77°F).
[See USP Controlled Room Temperature.]
Protect from light and moisture.

Manufactured by:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Rx only

S-9546 R6

Packaged and Distributed by:

Mylan Institutional Inc.

Rockford, IL 61103 U.S.A.

This unit dose package is not child resistant.

For institutional use only.

Keep this and all drugs out of the reach of children.

This container provides light-resistance.

See window for lot number and expiration date.

PRINCIPAL DISPLAY PANEL - 100 mg

NDC 51079-802-20

Metoprolol
Tartrate
Tablets, USP
100 mg

100 Tablets (10 x 10)

Each film-coated tablet contains:
Metoprolol tartrate, USP . . . . 100 mg

Usual Dosage: See accompanying
prescribing information.

Store at 20° to 25°C (68° to 77°F).
[See USP Controlled Room Temperature.]
Protect from light and moisture.

Manufactured by:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.

Rx only

S-5525 R10

Packaged and Distributed by:

Mylan Institutional Inc.

Rockford, IL 61103 U.S.A.

This unit dose package is not child resistant.

For institutional use only.

Keep this and all drugs out of the reach of children.

This container provides light-resistance.

See window for lot number and expiration date.

Metoprolol TARTRATE 
Metoprolol tartrate tablet, film coated
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:51079-255(NDC:0378-0018)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Metoprolol TARTRATE (Metoprolol) Metoprolol TARTRATE 25 mg
Inactive Ingredients
Ingredient Name Strength
ANHYDROUS LACTOSE  
SILICON DIOXIDE  
CROSCARMELLOSE SODIUM  
HYPROMELLOSE, UNSPECIFIED  
MAGNESIUM STEARATE  
MICROCRYSTALLINE CELLULOSE  
POLYDEXTROSE  
POLYETHYLENE GLYCOL, UNSPECIFIED  
POVIDONE, UNSPECIFIED  
SODIUM LAURYL SULFATE  
TITANIUM DIOXIDE  
TRIACETIN  
Product Characteristics
Color white Score 2 pieces
Shape ROUND Size 7mm
Flavor Imprint Code M;18
Contains     
Packaging
# Item Code Package Description
1 NDC:51079-255-20 100 BLISTER PACK in 1 CARTON
1 NDC:51079-255-01 1 TABLET, FILM COATED in 1 BLISTER PACK
2 NDC:51079-255-19 25 BLISTER PACK in 1 CARTON
2 NDC:51079-255-17 1 TABLET, FILM COATED in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA076704 09/20/2004
Metoprolol TARTRATE 
Metoprolol tartrate tablet, film coated
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:51079-801(NDC:0378-0032)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Metoprolol TARTRATE (Metoprolol) Metoprolol TARTRATE 50 mg
Inactive Ingredients
Ingredient Name Strength
ANHYDROUS LACTOSE  
SILICON DIOXIDE  
CROSCARMELLOSE SODIUM  
HYPROMELLOSE, UNSPECIFIED  
MAGNESIUM STEARATE  
MICROCRYSTALLINE CELLULOSE  
POLYDEXTROSE  
POLYETHYLENE GLYCOL, UNSPECIFIED  
POVIDONE, UNSPECIFIED  
SODIUM LAURYL SULFATE  
TITANIUM DIOXIDE  
TRIACETIN  
FD&C BLUE NO. 2  
D&C RED NO. 27  
FD&C RED NO. 40  
Product Characteristics
Color pink Score 2 pieces
Shape ROUND Size 8mm
Flavor Imprint Code M;32
Contains     
Packaging
# Item Code Package Description
1 NDC:51079-801-20 100 BLISTER PACK in 1 CARTON
1 NDC:51079-801-01 1 TABLET, FILM COATED in 1 BLISTER PACK
2 NDC:51079-801-19 25 BLISTER PACK in 1 CARTON
2 NDC:51079-801-17 1 TABLET, FILM COATED in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA076704 05/03/1994
Metoprolol TARTRATE 
Metoprolol tartrate tablet, film coated
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:51079-802(NDC:0378-0047)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Metoprolol TARTRATE (Metoprolol) Metoprolol TARTRATE 100 mg
Inactive Ingredients
Ingredient Name Strength
ANHYDROUS LACTOSE  
SILICON DIOXIDE  
CROSCARMELLOSE SODIUM  
HYPROMELLOSE, UNSPECIFIED  
MAGNESIUM STEARATE  
MICROCRYSTALLINE CELLULOSE  
POLYDEXTROSE  
POLYETHYLENE GLYCOL, UNSPECIFIED  
POVIDONE, UNSPECIFIED  
SODIUM LAURYL SULFATE  
TITANIUM DIOXIDE  
TRIACETIN  
FD&C BLUE NO. 2  
Product Characteristics
Color blue (Light Blue) Score 2 pieces
Shape ROUND Size 10mm
Flavor Imprint Code M;47
Contains     
Packaging
# Item Code Package Description
1 NDC:51079-802-20 100 BLISTER PACK in 1 CARTON
1 NDC:51079-802-01 1 TABLET, FILM COATED in 1 BLISTER PACK
2 NDC:51079-802-19 25 BLISTER PACK in 1 CARTON
2 NDC:51079-802-17 1 TABLET, FILM COATED in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA076704 05/03/1994
Labeler - Mylan Institutional Inc. (039615992)
Revised: 05/2017   Mylan Institutional Inc.

Duration of Action

Oral: Immediate release: Variable (dose-related; 50% reduction in maximum heart rate after single doses of 20, 50, and 100 mg occurred at 3.3, 5, and 6.4 hours, respectively), Extended release: ~24 hours

Half-Life Elimination

Neonates: 5 to 10 hours (Morselli 1989); Adults: 3 to 4 hours (7 to 9 hours in poor CYP2D6 metabolizers or hepatic impairment)

Protein Binding

~10% to 12% to albumin

Use Labeled Indications

Angina (oral formulations): Long term treatment of angina pectoris.

Heart failure (extended-release oral formulation): Treatment of stable, symptomatic (NYHA Class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin to reduce the rate of mortality plus hospitalization in patients already receiving ACE inhibitors, diuretics, and/or digoxin.

Hypertension (oral formulations): Management of hypertension.

Myocardial infarction (immediate-release oral formulation; injection): Treatment of hemodynamically stable acute myocardial infarction (MI) to reduce cardiovascular mortality (injection to be used in combination with metoprolol oral maintenance therapy).

Guideline recommendations:

Acute coronary syndromes (eg, myocardial infarction, non-ST-elevation ACS [NSTE-ACS]): According to the ACCF/AHA guidelines for the management of ST-elevation myocardial infarction (STEMI) and the AHA/ACC guidelines for the management of non-ST-elevation ACS (NSTE-ACS), oral beta-blockers should be initiated within the first 24 hours unless the patient has signs of heart failure, evidence of a low-output state, an increased risk for cardiogenic shock, or other contraindications (ACC/AHA [Amsterdam 2014]; ACCF/AHA [O’Gara 2013]). Use of sustained-release metoprolol is a recommended beta-blocker therapy in patients with concomitant NSTE-ACS, stabilized HF, and reduced systolic function (ACC/AHA [Amsterdam 2014]). Intravenous beta-blocker use should be reserved for patients post-STEMI who have refractory hypertension or ongoing ischemia (ACCF/AHA [O’Gara 2013]).

Heart failure: The ACCF/AHA 2013 heart failure guidelines recommend the use of 1 of 3 beta blockers (ie, bisoprolol, carvedilol, or extended-release metoprolol succinate) for all patients with recent or remote history of MI or ACS and reduced ejection fraction (rEF) to reduce mortality, for all patients with rEF to prevent symptomatic HF (even if no history of MI), and for all patients with current or prior symptoms of HF with reduced ejection fraction (HFrEF), unless contraindicated, to reduce morbidity and mortality (ACCF/AHA [Yancy 2013]).

Hypertension: The 2014 guideline for the management of high blood pressure in adults (Eighth Joint National Committee [JNC 8]) recommends initiation of pharmacologic treatment to lower blood pressure for the following patients (JNC8 [James 2013]):

• Patients ≥60 years of age, with systolic blood pressure (SBP) ≥150 mm Hg or diastolic blood pressure (DBP) ≥90 mm Hg. Goal of therapy is SBP <150 mm Hg and DBP <90 mm Hg.

• Patients <60 years of age, with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with diabetes, with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with chronic kidney disease (CKD), with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

Chronic kidney disease (CKD) and hypertension: Regardless of race or diabetes status, the use of an ACE inhibitor (ACEI) or angiotensin receptor blocker (ARB) as initial therapy is recommended to improve kidney outcomes. In the general nonblack population (without CKD) including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic, calcium channel blocker, ACEI, or ARB. In the general black population (without CKD) including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic or a calcium channel blocker instead of an ACEI or ARB.

Coronary artery disease (CAD) and hypertension: The American Heart Association, American College of Cardiology and American Society of Hypertension (AHA/ACC/ASH) 2015 scientific statement for the treatment of hypertension in patients with coronary artery disease (CAD) recommends the use of a beta blocker as part of a regimen in patients with hypertension and chronic stable angina with a history of prior MI. A BP target of <140/90 mm Hg is reasonable for the secondary prevention of cardiovascular events. A lower target BP (<130/80 mm Hg) may be appropriate in some individuals with CAD, previous MI, stroke or transient ischemic attack, or CAD risk equivalents (AHA/ACC/ASH [Rosendorff 2015]).

Contraindications

Hypersensitivity to metoprolol, any component of the formulation, or other beta-blockers; second- or third-degree heart block.

Note: Additional contraindications are formulation and/or indication specific.

Immediate-release tablets/injectable formulation:

Hypertension and angina (oral only): Sinus bradycardia; cardiogenic shock; overt heart failure; sick sinus syndrome; severe peripheral arterial circulatory disorders

Myocardial infarction (oral and injection): Severe sinus bradycardia (heart rate <45 beats/minute); significant first-degree heart block (P-R interval ≥0.24 seconds); systolic blood pressure <100 mm Hg; moderate to severe cardiac failure

Extended-release tablet: Severe bradycardia, cardiogenic shock; decompensated heart failure; sick sinus syndrome (except in patients with a functioning artificial pacemaker)

Canadian labeling: Additional contraindications (not in US labeling): Cor pulmonale; untreated pheochromocytoma; asthma and other obstructive respiratory disease (injection only); concomitant use with anesthesia agents that cause myocardial depression

Dosing Adult

Angina: Oral:

Immediate release (metoprolol tartrate): Initial: 50 mg twice daily; usual dosage range: 50 to 200 mg twice daily; may increase dose at weekly intervals to desired effect (maximum: 400 mg/day).

Extended release (metoprolol succinate): Initial: 100 mg once daily; may increase dose at weekly intervals to desired effect (maximum: 400 mg/day).

Atrial fibrillation/flutter (ventricular rate control) (acute treatment; off-label use) (AHA/ACC/HRS [January 2014]; AHA [Neumar 2010]): IV: 2.5 to 5 mg every 2 to 5 minutes (maximum total dose: 15 mg over a 10- to 15-minute period). Note: Initiate cautiously in patients with concomitant heart failure. Avoid in patients with decompensated heart failure; electrical cardioversion preferred.

Maintenance: Oral (immediate release [metoprolol tartrate]): 25 to 100 mg twice daily; Oral (extended release [metoprolol succinate]): 50 to 400 mg once daily

Heart failure: Note: Initiate only in stable patients or hospitalized patients after volume status has been optimized and IV diuretics, vasodilators, and inotropic agents have all been successfully discontinued. Caution should be used when initiating in patients who required inotropes during their hospital course. Increase dose gradually and monitor for congestive signs and symptoms of HF making every effort to achieve target dose shown to be effective (ACCF/AHA [Yancy 2013]; HFSA [Lindenfeld 2010]; MERIT-HF Study Group 1999).

Oral: Extended release (metoprolol succinate): Initial: 25 mg once daily (reduce to 12.5 mg once daily in NYHA class higher than class II); may double dosage every 2 weeks as tolerated up to target dose of 200 mg/day.

ACCF/AHA 2013 Heart Failure Guidelines: Oral (extended release [metoprolol succinate]): Initial: 12.5 to 25 mg once daily; maximum dose: 200 mg/day (Yancy 2013).

Hypertension: Oral:

Immediate release (metoprolol tartrate): Initial: 50 mg twice daily; effective dosage range: 100 to 450 mg daily in 2 to 3 divided doses; may increase dose at weekly (or longer) intervals to desired effect; maximum dose: 450 mg/day; usual dosage range (ASH/ISH [Weber 2014]): 50 to 100 mg twice daily; target dose (JNC 8 [James 2013]): 100 to 200 mg daily

Extended release (metoprolol succinate): Initial: 25 to 100 mg once daily; may increase dose at weekly (or longer) intervals to desired effect; maximum: 400 mg/day.

Hypertension/ventricular rate control: IV (in patients having nonfunctioning GI tract): Initial: 1.25 to 5 mg every 6 to 12 hours; titrate initial dose to response. Initially, low doses may be appropriate to establish response (Huckleberry 2003); however, although not routine, up to 15 mg administered as frequently as every 3 hours has been employed in patients with refractory tachycardia.

Myocardial infarction:

Early treatment: Note: The ACCF/AHA guidelines for the management of STEMI recommend the use of IV metoprolol at the time of presentation only in patients with STEMI who are hypertensive or have ongoing ischemia without contraindications. Oral metoprolol (immediate release) initiated within the first 24 hours is recommended in all other patients. Do not initiate metoprolol in those with signs of heart failure, a low output state, increased risk of cardiogenic shock, or other contraindications (eg, second- or third-degree heart block) (ACCF/AHA [O'Gara 2013]).

IV: 5 mg every 5 minutes as tolerated for up to 3 doses in the early treatment of ST elevation myocardial infarction; titrate to heart rate and blood pressure; then begin oral therapy (ACCF/AHA [O'Gara 2013]).

Oral: 25 to 50 mg (metoprolol tartrate [immediate release]) every 6 to 12 hours; transition over the next 2 to 3 days to twice daily dosing of metoprolol tartrate (immediate release) or to daily metoprolol succinate (extended release) and increase as tolerated to a maximum dose of 200 mg/day (ACCF/AHA [O'Gara 2013]).

Secondary prevention (off-label use): Oral: Immediate release (metoprolol tartrate): 25 to 100 mg twice daily; optimize dose based on heart rate and blood pressure; continue indefinitely (Olsson 1992).

Supraventricular tachycardia (off-label use):

Acute treatment: IV: Initial: 2.5 to 5 mg bolus over 2 minutes, may repeat with 2.5 to 5 mg bolus within a 10-minute period, up to 3 doses (ACC/AHA/HRS [Page 2015])

Ongoing management: Oral: Initial: 50 mg once daily (extended-release [metoprolol succinate]) or 25 mg twice daily (immediate-release [metoprolol tartrate]); maximum maintenance dose: 400 mg once daily (extended-release [metoprolol succinate]) or 200 mg twice daily (immediate-release [metoprolol tartrate]) (ACC/AHA/HRS [Page 2015])

Thyrotoxicosis (off-label use): Oral: Immediate release (metoprolol tartrate): 25 to 50 mg every 6 hours; may also consider administering extended-release formulation (metoprolol succinate) (Bahn 2011).

Note: Switching dosage forms:

When switching from immediate release (metoprolol tartrate) to extended release (metoprolol succinate), the same total daily dose of metoprolol should be used.

When switching between oral and intravenous dosage forms, in most cases, equivalent beta-blocking effect is achieved when doses in a 2.5:1 (Oral:IV) ratio is used. However, in one bioavailability study including healthy volunteers, a range of Oral:IV conversion ratios was found to be approximately 2:1 to 5:1 (Regardh 1974). Therefore, patient variability may exist and a specific ratio may not apply to all patients, especially if comorbid conditions are present. For example, based on a range of 2.5:1 to 5:1 ratios, if the patient is receiving a chronic oral dose of 25 mg twice daily (50 mg daily), this would translate to 2.5 to 5 mg IV every 6 hours. Recognizing that patients receiving larger chronic oral doses should not automatically be converted to a large IV dose, consideration should be given to further reducing the initial IV dose and basing subsequent doses on the clinical response (Huckleberry 2003).

ALERT U.S. Boxed Warning

Ischemic heart disease:

Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction (MI) have occurred. When discontinuing chronically administered metoprolol, particularly in patients with ischemic heart disease, gradually reduce the dosage over a period of 1 to 2 weeks and carefully monitor the patient. If angina markedly worsens or acute coronary insufficiency develops, reinstate metoprolol administration promptly, at least temporarily, and take other measures appropriate for the management of unstable angina. Warn patients against interruption or discontinuation of therapy without their health care provider's advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue metoprolol therapy abruptly, even in patients treated only for hypertension.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Metoprolol side effects

Get emergency medical help if you have any signs of an allergic reaction to metoprolol: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • very slow heartbeats;

  • a light-headed feeling, like you might pass out;

  • shortness of breath (even with mild exertion), swelling, rapid weight gain; or

  • cold feeling in your hands and feet.

Common metoprolol side effects may include:

  • dizziness, tired feeling;

  • confusion, memory problems;

  • nightmares, trouble sleeping;

  • diarrhea; or

  • mild itching or rash.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect metoprolol?

Tell your doctor about all medicines you use, and those you start or stop using during your treatment with metoprolol, especially:

  • prazosin;

  • terbinafine;

  • an antidepressant - bupropion, clomipramine, desipramine, duloxetine, fluoxetine, fluvoxamine, paroxetine, sertraline;

  • an ergot medicine - dihydroergotamine, ergonovine, ergotamine, methylergonovine;

  • heart or blood pressure medications - amlodipine, clonidine, digoxin, diltiazem, dipyridamole, hydralazine, methyldopa, nifedipine, quinidine, reserpine, verapamil, and others;

  • a MAO inhibitor - isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, tranylcypromine; or

  • medicine to treat mental illness - chlorpromazine, fluphenazine haloperidol, thioridazine.

This list is not complete. Other drugs may interact with metoprolol, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Precautions

US BOXED WARNING:
-ISCHEMIC HEART DISEASE: Following abrupt discontinuation of therapy with beta adrenergic blockers, exacerbations of angina pectoris and myocardial infarction have occurred. When discontinuing chronically administered metoprolol, particularly in patients with ischemic heart disease, gradually reduce the dose over a period of 1 to 2 weeks and monitor the patient. If angina markedly worsens or acute coronary insufficiency develops, promptly resume therapy, at least temporarily, and take other measures appropriate for the management of unstable angina. Warn patients against interruption or discontinuation of therapy without the physician's advice. Because coronary artery disease is common and may be unrecognized, avoid abrupt discontinuation of metoprolol therapy even in patients treated only for hypertension.

Metoprolol tartrate safety and efficacy have not been established in patients younger than 18 years.
Metoprolol succinate safety and efficacy have not been established in patients younger than 6 years.

Consult WARNINGS section for additional precautions.

Other Comments

Administration advice:
-If a dose is missed, the patient should take only the next scheduled dose without doubling it.
-Administer immediate release tablets with or immediately after meals.
-Extended release tablets are scored and can be divided; however, do not crush or chew the whole or half tablet.

Monitoring:
-Monitor heart rate and rhythm.
-When discontinuing a chronically administered beta blocker, reduce dose over 1 to 2 weeks and monitor carefully, especially in patients with coronary artery disease.

Patient advice:
-Warn patients not to interrupt or discontinue therapy without a physician's advice.
-Avoid operating automobiles and machinery or engaging in other tasks requiring alertness until the patient's response to therapy has been determined.
-Contact the physician if difficulty in breathing occurs.
-Inform the physician or dentist of use of this drug before any type of surgery.
-Advise heart failure patients to consult their physician if signs or symptoms of worsening heart failure occur such as weight gain or increasing shortness of breath.

Bottom Line

Metoprolol is a selective beta-blocker at dosages usually prescribed to lower blood pressure or relieve the symptoms of angina. Two different salts are available, metoprolol tartrate and metoprolol succinate. These are not interchangeable. Metoprolol should not be stopped abruptly.

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