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