pharmacopeia
GET
/api/v1/drug/metoprolol
2D structure
1-[4-(2-methoxyethyl)phenoxy]-3-(propan-2-ylamino)propan-2-ol
SMILES CC(C)NCC(COC1=CC=C(C=C1)CCOC)O
InChIKey IUBSYMUCCVWXPE-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Metoprolol is a beta 1 -selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta 2 -adrenoreceptors, chiefly located in the bronchial and vascular musculature.

Indications

Sourced from openFDA
  • Metoprolol tartrate tablets are a beta-adrenergic blocker indicated for the treatment of: Hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.ICD-10: I10

Contraindications

Sourced from openFDA
  • Metoprolol tartrate tablets are contraindicated in severe bradycardia, second- or third-degree heart block, cardiogenic shock, systolic blood pressure <100, 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. Known hypersensitivity to product components.contraindicated

Dosage & administration

Sourced from openFDA

Administer once daily with food or after a meal. Titrate at weekly or longer intervals as needed and tolerated. ( 2 ) Hypertension: Recommended starting dosage is 100 mg daily, in single or divided doses. ( 2.1 ) Angina Pectoris: Recommended starting dosage is 100 mg daily, given as two divided doses. ( 2.2 ) Myocardial Infarction: The starting dosage depends upon tolerance of intravenous metoprolol, see full prescribing information. ( 2.3 ) 2.1 Hypertension Individualize the dosage of metoprolol tartrate tablets. Metoprolol tartrate tablets should be taken with or immediately following meals. The usual initial dosage is 100 mg daily in single or divided doses. Adjust dosage at weekly (or longer) intervals until optimum blood pressure reduction is achieved. In general, the maximum effect of any given dosage level will be apparent after 1 week of therapy. The effective dosage range of metoprolol tartrate tablets is 100 mg to 450 mg per day. Dosages above 450 mg per day have not been studied. While once-daily dosing can maintain a reduction in blood pressure throughout the day, lower doses (especially 100 mg) may not maintain a full effect at the end of the 24-hour period. Larger or more frequent daily doses may be required. Measure blood pressure near the end of the dosing interval to determine whether satisfactory control is being maintained throughout the day. 2.2 Angina Pectoris The dosage of metoprolol tartrate tablets should be individualized. Metoprolol tartrate tablets should be taken with or immediately following meals.

Warnings & precautions

Sourced from openFDA

Abrupt cessation may exacerbate myocardial ischemia. ( 5.1 ) Heart Failure: Worsening cardiac failure may occur. ( 5.2 ) Bronchospastic Disease: Avoid beta-blockers. ( 5.3 ) Pheochromocytoma: Initiate therapy with an alpha blocker. ( 5.4 ) Major Surgery: Avoid initiation of high-dose extended-release metoprolol in patients undergoing non-cardiac surgery. Do not routinely withdraw chronic beta-blocker therapy prior to surgery. ( 5.5 , 6.1 ) Diabetes: May mask symptoms of hypoglycemia.( 5.6 ) Thyrotoxicosis: Abrupt withdrawal in patients with thyrotoxicosis might precipitate a thyroid storm. ( 5.7 ) Peripheral Vascular Disease: Can aggravate symptoms of arterial insufficiency. ( 5.9 ) 5.1 Abrupt Cessation of Therapy 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, gradually reduce the dosage over a period of 1 to 2 weeks and monitor the patient. If angina markedly worsens or acute coronary ischemia develops, promptly reinstate metoprolol, and take measures appropriate for the management of unstable angina. Warn patients not to interrupt therapy without their physician’s advice. Because coronary artery disease is common and may be unrecognized, avoid abruptly discontinuing metoprolol in patients treated only for hypertension. 5.2 Heart Failure Worsening cardiac failure may occur during up-titration of metoprolol.

Adverse reactions

Sourced from openFDA

The following adverse reactions are described elsewhere in labeling: Worsening angina or myocardial infarction [see Warnings and Precautions (5) ] Worsening heart failure [see Warnings and Precautions (5) ]. Worsening AV block [see Contraindications (4) ]. ­Most common adverse reactions: tiredness, dizziness, depression, shortness of breath, bradycardia, hypotension, diarrhea, pruritus, rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Rising Pharma Holdings, Inc. at 1-844-874-7464 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Hypertension and Angina Most adverse effects have been mild and transient. Central Nervous System: Tiredness and dizziness have occurred in about 10% of 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 patients. Cold extremities; arterial insufficiency, usually of the Raynaud type; palpitations; heart failure exacerbations; peripheral edema; and hypotension have been reported in about 1% of patients. Gangrene in patients with pre-existing severe peripheral circulatory disorders has also been reported.

Use in specific populations

Sourced from openFDA

Hepatic Impairment: Consider initiating metoprolol therapy at low doses and gradually increase dosage to optimize therapy, while monitoring closely for adverse events. ( 8.6 ) 8.1 Pregnancy Risk Summary Available data from published observational studies have not demonstrated an association of adverse developmental outcomes with maternal use of metoprolol during pregnancy ( see Data). Untreated hypertension and myocardial infarction during pregnancy can lead to adverse outcomes for the mother and the fetus (see Clinical Considerations). In animal reproduction studies, metoprolol has been shown to increase post-implantation loss and decrease neonatal survival in rats at oral dosages of 500 mg/kg/day, approximately 11 times the daily dose of 450 mg in a 60-kg patient on a mg/m 2 basis. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption : The estimated oral bioavailability of immediate release metoprolol is about 50% because of pre-systemic metabolism which is saturable leading to non-proportionate increase in the exposure with increased dose. Distribution: Metoprolol is extensively distributed with a reported volume of distribution of 3.2 to 5.6 L/kg.

Overdosage

Sourced from openFDA

Signs and Symptoms - Overdosage of metoprolol may lead to severe bradycardia, hypotension, and cardiogenic shock. Clinical presentation can also include: atrioventricular block, heart failure, bronchospasm, hypoxia, impairment of consciousness/coma, nausea and vomiting. Treatment – Consider treating the patient with intensive care. Patients with myocardial infarction or heart failure may be prone to significant hemodynamic instability. Beta-blocker overdose may result in significant resistance to resuscitation with adrenergic agents, including beta-agonists. On the basis of the pharmacologic actions of metoprolol, employ the following measures. Hemodialysis is unlikely to make a useful contribution to metoprolol elimination [see Clinical Pharmacology (12.3) ]. Bradycardia: Evaluate the need for atropine, adrenergic-stimulating drugs or pacemaker to treat bradycardia and conduction disorders. Hypotension: Treat underlying bradycardia. Consider intravenous vasopressor infusion, such as dopamine or norepinephrine.

Approval history

Sourced from openFDA
  • Aug 7, 1978NDANDA017963Validus Pharms
  • Jan 10, 1992NDANDA019962Melinta Therap
  • Apr 27, 1995ANDAANDA074453Renata
  • Jan 16, 2004ANDAANDA076704Mylan
  • Aug 20, 2004ANDAANDA076792Mylan
  • Jan 26, 2018NDANDA210428Spil
  • Apr 10, 2025NDANDA219373Rubicon Research
  • Aug 28, 2025NDANDA218698Xtm Consulting

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
347,927 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue22,9476.6%
  2. 2Dyspnoea19,8525.7%
  3. 3Diarrhoea19,4925.6%
  4. 4Nausea19,3085.5%
  5. 5Drug Ineffective17,3085.0%
  6. 6Dizziness16,3924.7%
  7. 7Off Label Use14,4304.1%
  8. 8Death13,9464.0%
  9. 9Asthenia13,2603.8%
  10. 10Headache13,0533.8%
  11. 11Pain13,0123.7%
  12. 12Fall12,5853.6%
  13. 13Pneumonia10,1882.9%
  14. 14Vomiting10,1312.9%
  15. 15Hypotension10,1122.9%

Literature

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Recent PubMed references pinned to Metoprolol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 347 ClinicalTrials.gov registrations naming Metoprolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Metoprolol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Metoprolol work?
Metoprolol is a beta 1 -selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta 2 -adrenoreceptors, chiefly located in the bronchial and vascular musculature.
What is Metoprolol used for?
According to FDA labeling, Metoprolol carries indications including: Metoprolol tartrate tablets are a beta-adrenergic blocker indicated for the treatment of: Hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Metoprolol?
Metoprolol is classified as Beta blocking agents, selective, beta-Adrenergic Blocker, Adrenergic beta-Antagonists, Adrenergic beta1-Antagonists, Cardiac Rate Alteration, Cardiac Rhythm Alteration, Decreased Blood Pressure, Negative Chronotropy, Negative Inotropy.
What are the brand names for Metoprolol?
Metoprolol is marketed under brand names including Kapspargo, Lopressor, Lopressor HCT, Toprol.
What are the contraindications for Metoprolol?
Metoprolol labeling lists contraindications including: Metoprolol tartrate tablets are contraindicated in severe bradycardia, second- or third-degree heart block, cardiogenic shock, systolic blood pressure <100, 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. Known hypersensitivity to product components.. Always consult the full prescribing information and a clinician.
Note. Data for metoprolol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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