Section 02 · Monograph

Metoprolol

Reviewed Nov 2026FDA label
LopressorBeta-blocker
Forms
Tab: 25, 50, 100mg | ER: 25-200mg
Dose
50-200mg/day (prevention)
MOA
Selective β1 blockade

Indications

  • Hypertension — to lower blood pressure, reducing risk of fatal and non-fatal cardiovascular events (succinate ER and tartrate formulations)FDA-labeled
  • Angina pectoris — long-term management to reduce angina attacks and improve exercise toleranceFDA-labeled
  • Heart failure (NYHA II-IV, stable) — metoprolol succinate extended-release only, to reduce risk of cardiovascular mortality and heart-failure hospitalizationFDA-labeled
  • Acute myocardial infarction (metoprolol tartrate IV/oral, hemodynamically stable patients) — to reduce cardiovascular mortalityFDA-labeled

Off-Label Uses

  • Migraine prophylaxis — NOT an FDA-approved indication for metoprolol (unlike propranolol and timolol, which do carry FDA-approved migraine prophylaxis indications); used off-label based on clinical evidence and guideline supportOff-label
  • Essential tremor (off-label)Off-label
  • Performance/situational anxiety (off-label)Off-label

Mechanism of Action

  • Beta-1 selective (cardioselective) adrenergic receptor blocking agent at usual clinical doses
  • Reduces heart rate, myocardial contractility, and cardiac output, thereby decreasing myocardial oxygen demand
  • Suppresses renin release from the kidney, contributing to blood-pressure-lowering effect
  • At higher doses, selectivity for beta-1 receptors diminishes and beta-2 blockade can occur

Full Dosing

Adult / usual

  • Hypertension: initiate 25-100 mg/day (succinate ER) or 100 mg/day in divided doses (tartrate); titrate at weekly intervals; usual maintenance up to 400 mg/day
  • Angina: initiate 100 mg/day (succinate ER); titrate weekly; max 400 mg/day
  • Heart failure: initiate metoprolol succinate ER 12.5-25 mg once daily; double the dose approximately every 2 weeks as tolerated, target/max 200 mg/day
  • Off-label migraine prophylaxis (not FDA-labeled dosing): typical regimens in clinical practice range roughly 47.5-200 mg/day of the succinate ER formulation or 100-200 mg/day tartrate in divided doses — verify against current guideline-based dosing, as this is not derived from an FDA-approved indication
  • Discontinuation: taper gradually over 1-2 weeks; abrupt cessation can precipitate angina, MI, or ventricular arrhythmias

Renal

  • Renal/hepatic impairment: no specific dose adjustment required per label for renal impairment; use caution and consider lower doses in significant hepatic impairment

Contraindications

  • Severe bradycardia
  • Second- or third-degree AV block
  • Sick sinus syndrome (unless a permanent pacemaker is in place)
  • Cardiogenic shock
  • Decompensated heart failure
  • Hypersensitivity to metoprolol or product components
  • Severe peripheral arterial circulatory disorders

Drug Interactions

  • CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, propafenone) can substantially increase metoprolol concentrations
  • Catecholamine-depleting drugs (reserpine, MAO inhibitors) may produce additive hypotension and bradycardia
  • Non-dihydropyridine calcium channel blockers (verapamil, diltiazem) and digitalis glycosides increase risk of bradycardia and AV conduction disturbances
  • Clonidine: concurrent use requires caution with discontinuation sequencing to avoid rebound hypertension
  • Other antihypertensives and negative inotropes/chronotropes have additive effects

Adverse Effects

  • Fatigue/tiredness
  • Dizziness
  • Depression
  • Bradycardia
  • Hypotension
  • Shortness of breath
  • Diarrhea
  • Pruritus/rash
  • Cold extremities
  • Masking of hypoglycemia symptoms in diabetic patients

Monitoring Parameters

  • Heart rate and blood pressure, especially during initiation and dose titration
  • Signs/symptoms of worsening heart failure (weight gain, edema, dyspnea) during up-titration
  • Blood glucose in diabetic patients (beta-blockade can mask tachycardia as a hypoglycemia warning sign)
  • Signs of bronchospasm in patients with reactive airway disease
  • ECG/PR interval if used with other AV-nodal blocking agents

Pregnancy & Lactation

  • Pregnancy: published observational data have not demonstrated a consistent drug-associated risk of major birth defects, though beta-blockers as a class have inconsistent reports of intrauterine growth restriction; use if potential benefit justifies potential fetal risk
  • Neonates of mothers treated with beta-blockers should be monitored for signs of bradycardia, hypotension, hypoglycemia, and respiratory depression
  • Lactation: metoprolol is present in human milk; estimated relative infant dose approximately 0.5-2% of the maternal weight-adjusted dosage; monitor breastfed infants for bradycardia and other beta-blocker effects

References

  1. FDA Prescribing Information — Toprol-XL (metoprolol succinate)
  2. FDA Prescribing Information — Lopressor (metoprolol tartrate)

Same class