Metoprolol Oral Dosing Guidelines
For heart failure with reduced ejection fraction, start metoprolol succinate extended-release at 12.5-25 mg once daily and titrate every 2 weeks to a target dose of 200 mg once daily; for hypertension, start metoprolol tartrate at 25-50 mg twice daily or metoprolol succinate at 50 mg once daily, titrating to effect with maximum doses of 200 mg twice daily (tartrate) or 400 mg daily (succinate). 1, 2, 3
Heart Failure Dosing (Metoprolol Succinate Extended-Release ONLY)
Critical formulation distinction: Only metoprolol succinate extended-release (CR/XL) has proven mortality reduction in heart failure—metoprolol tartrate has NOT demonstrated this benefit and should not be used for heart failure management. 1, 4
Starting and Target Doses
- Initial dose: 12.5-25 mg once daily, with the lower dose (12.5 mg) preferred for NYHA Class III-IV patients and 25 mg for Class II patients. 5, 1
- Target dose: 200 mg once daily, which achieved a 34% reduction in all-cause mortality in the MERIT-HF trial. 1, 4
- Titration schedule: Double the dose every 2 weeks if well tolerated, progressing as 12.5 mg → 25 mg → 50 mg → 100 mg → 200 mg once daily. 5, 1
Minimum Effective Dosing
- If the full target dose cannot be achieved, aim for at least 50% of target (100 mg daily minimum), as dose-response relationships exist for mortality benefit. 1, 6
- Even lower doses provide benefit if target doses cannot be tolerated—some beta-blocker is better than no beta-blocker. 1, 6
Prerequisites and Monitoring
- Patients should be on background ACE inhibitor therapy (if not contraindicated) before initiating beta-blocker. 5
- The patient must be relatively stable without need for intravenous inotropic therapy and without signs of marked fluid retention. 5
- Monitor for heart rate, blood pressure, clinical status, and signs of congestion at each visit. 1
- Check blood chemistry 12 weeks after initiation and 12 weeks after final dose titration. 1
Hypertension Dosing
Metoprolol Tartrate (Immediate-Release)
- Initial dose: 25-50 mg twice daily. 2, 3
- Maintenance dose: 100-200 mg daily in divided doses. 1
- Maximum dose: 200 mg twice daily (400 mg total daily). 2
Metoprolol Succinate (Extended-Release)
- Initial dose: 50 mg once daily. 2
- Maintenance dose: 50-200 mg once daily. 1, 2
- Maximum dose: 400 mg once daily. 2, 3
Important Considerations for Hypertension
- Beta-blockers are NOT recommended as first-line agents for hypertension unless the patient has ischemic heart disease or heart failure. 1
- Titrate dose every 1-2 weeks based on blood pressure response. 2
- Target blood pressure is <130/80 mmHg for most patients. 1
Post-Myocardial Infarction Dosing
Early Treatment (First 48 Hours)
- IV phase: 5 mg IV bolus over 2 minutes, repeated every 5 minutes for up to 3 doses (15 mg total maximum). 3
- Oral phase: Begin 15 minutes after last IV dose with 50 mg every 6 hours for 48 hours (or 25 mg every 6 hours if patient shows intolerance to full IV dose). 3
Long-Term Maintenance
- Follow heart failure dosing regimen with metoprolol succinate, targeting 200 mg daily. 1
Special Populations and Comorbidities
Renal Impairment
- No dose adjustment required for metoprolol in patients with renal impairment, as systemic availability and half-life do not differ clinically from normal subjects. 3
Hepatic Impairment
- Start at low doses with cautious gradual titration according to clinical response, as metoprolol blood levels increase substantially in hepatic impairment (elimination half-life can extend up to 7.2 hours). 3
Asthma or COPD
- Cardioselective agents (metoprolol, bisoprolol) are preferred for patients with bronchospastic airway disease requiring a beta-blocker. 1
- Patients with suspicion of bronchial asthma or severe pulmonary disease should be referred for specialist care before initiating beta-blocker therapy. 5
- Absolute contraindication: Active asthma or severe reactive airway disease. 2, 3
Elderly Patients (>65 Years)
- Use a low initial starting dose given greater frequency of decreased hepatic, renal, or cardiac function. 3
- Elderly patients may show slightly higher plasma concentrations due to decreased metabolism and hepatic blood flow, though this is not clinically significant. 3
- For elderly women specifically, doses of 15 mg produce similar drug exposure to 50 mg in healthy young men. 2
Women
- Women may achieve optimal outcomes at 50% of guideline-recommended doses, with 30% lower risk of death or heart failure hospitalization. 2
- Metoprolol exposure is 50-80% higher in women than men, resulting in greater heart rate and blood pressure reduction. 2
Critical Contraindications (All Indications)
- Signs of heart failure, low output state, or decompensated heart failure. 2, 3
- Second or third-degree AV block without functioning pacemaker. 2, 3
- PR interval >0.24 seconds. 1, 2
- Active asthma or reactive airways disease. 2, 3
- Symptomatic bradycardia (heart rate <50-60 bpm with symptoms). 1, 2
- Systolic blood pressure <100 mmHg with symptoms. 1, 2
- Sick sinus syndrome without permanent pacemaker. 1
Managing Adverse Effects During Titration
Worsening Congestion
- First: Double the diuretic dose. 5, 1
- Second: Halve the beta-blocker dose only if increasing diuretic fails. 5, 1
Symptomatic Hypotension
- First: Reduce or eliminate vasodilators (nitrates, calcium channel blockers). 5, 1
- Second: If no congestion present, consider reducing diuretic dose. 1
- Third: Only if above measures fail, temporarily reduce metoprolol dose by 50%. 1
Marked Fatigue or Bradycardia
- Halve the beta-blocker dose. 5, 1
- For heart rate <50 bpm with worsening symptoms, halve dose or stop if severe deterioration. 5, 1
Critical Warnings
Never abruptly discontinue metoprolol—this can cause severe exacerbation of angina, myocardial infarction, ventricular arrhythmias, and has been associated with 50% mortality rate in one study. 1, 2 If discontinuation is necessary, taper gradually over approximately one week under close surveillance, reducing dose by 25-50% every 7 days. 1, 2