Bisoprolol Dosing Recommendations
For hypertension, start bisoprolol at 5 mg once daily (or 2.5 mg in patients with bronchospastic disease), titrating to 10 mg and then 20 mg once daily if needed; for heart failure with reduced ejection fraction, start at 1.25 mg once daily and titrate every 2 weeks to a target dose of 10 mg once daily. 1, 2
Dosing by Indication
Hypertension
- The FDA-approved starting dose is 5 mg once daily, with dose escalation to 10 mg and then 20 mg once daily if blood pressure control is inadequate 1
- For patients with bronchospastic disease, initiate at 2.5 mg once daily 1
- The American College of Cardiology notes that beta-blockers are not first-line agents for hypertension unless the patient has ischemic heart disease or heart failure 2
Heart Failure with Reduced Ejection Fraction (HFrEF)
- Start at 1.25 mg once daily and double the dose every 2 weeks as tolerated, targeting 10 mg once daily 2, 3
- The titration schedule follows: 1.25 mg → 2.5 mg → 5 mg → 10 mg once daily 2
- The European Society of Cardiology emphasizes that bisoprolol is one of only three beta-blockers proven to reduce mortality in HFrEF (34% relative risk reduction), making this a class effect specific to bisoprolol, carvedilol, and metoprolol succinate 2, 3
- Even if the target dose of 10 mg cannot be achieved, maintaining at least 50% of target dose (5 mg daily minimum) provides mortality benefit 2
- Monitor heart rate, blood pressure, clinical status, and signs of congestion at each visit during titration 2
Special Populations
Renal Impairment
- For mild to moderate renal dysfunction, no dose adjustment is necessary 1, 4
- For severe renal impairment (creatinine clearance <40 mL/min) or end-stage renal disease, start at 2.5 mg once daily and do not exceed 10 mg once daily 1, 4, 5
- Bisoprolol has balanced clearance (both renal and hepatic), preventing accumulation beyond a factor of 2 even in complete renal failure 4, 5
- The elimination half-life increases by a factor of 1.96 in severe renal dysfunction (from 10 hours to 18.5-24.2 hours) 4, 5
- Bisoprolol is not dialyzable, so drug replacement is not necessary in patients undergoing dialysis 1, 4
Hepatic Impairment
- For hepatitis or cirrhosis, start at 2.5 mg once daily and use caution during dose titration 1, 5
- In liver cirrhosis, the elimination half-life increases to 13.5 hours and total body clearance decreases to 10.8 L/h, but accumulation does not exceed a factor of 2 5
- In terminal stages of liver insufficiency, do not exceed 10 mg daily 5
Elderly Patients
- No dose adjustment is necessary in elderly patients unless significant renal or hepatic dysfunction is present 1
- Start at the lowest possible dose (1.25 mg/day for heart failure) and increase very progressively, with stages longer than 15 days if necessary 6
- Age, eGFR, and bisoprolol dose are independent predictors of high plasma concentration 7
- High bisoprolol plasma concentration (≥5.38 ng/mL) is independently associated with worsening heart failure in elderly patients (HR 6.32,95% CI 1.34-29.83) 7
- The SENIORS study confirmed that bisoprolol is both efficacious and well-tolerated in elderly people with heart failure regardless of ejection fraction 6
Titration Protocol for Heart Failure
Initiation Requirements
- Patients must be in stable NYHA class II or III, at least 1 month after any decompensation 6
- Ensure background ACE inhibitor or ARB therapy is established before initiating beta-blocker 2
- Bisoprolol is contraindicated in current or recent (within 4 weeks) exacerbation of heart failure requiring hospitalization 2
Dose Escalation Schedule
- Double the dose at intervals of not less than 2 weeks, aiming for target doses used in clinical trials (10 mg daily) or the highest tolerated dose 2
- Monitor heart rate, blood pressure, clinical status, and signs of congestion at each visit 2
- Check blood chemistry 1-2 weeks after initiation and 1-2 weeks after final dose titration 2
Managing Adverse Effects During Titration
For worsening congestion:
- First, double the dose of diuretic 2
- Second, halve the dose of bisoprolol only if increasing diuretic does not work 2
For marked fatigue or bradycardia:
- Halve the dose of bisoprolol 2
For heart rate <50 beats/min with worsening symptoms:
- Halve the dose or stop bisoprolol if severe deterioration occurs 2
For symptomatic hypotension:
- First reconsider need for nitrates, calcium channel blockers, and other vasodilators—reduce or eliminate these before adjusting bisoprolol 2
- If no signs of congestion, consider reducing diuretic dose 2
- Only as a last resort, temporarily reduce bisoprolol dose by 50% 2
Critical Contraindications
- Decompensated heart failure or current/recent (within 4 weeks) exacerbation requiring hospitalization 2, 6
- Second or third-degree heart block, sick sinus syndrome without a permanent pacemaker 2
- Sinus bradycardia <50 beats/min 2
- Active asthma or severe reactive airway disease 2, 1
- Symptomatic bradycardia or hypotension 2
Important Clinical Pearls
- Never stop bisoprolol abruptly unless absolutely necessary, as this risks rebound ischemia, myocardial infarction, and arrhythmias 2, 3
- If discontinuation is necessary, taper gradually over about one week under close surveillance 2
- Bisoprolol offers once-daily dosing and consistent 24-hour beta-blockade, which may improve compliance compared to twice-daily formulations 2, 3
- In the CIBIS-II trial, treatment with bisoprolol at target doses of 10 mg/day was associated with significant mortality reduction 2
- Some beta-blocker is better than no beta-blocker when target doses cannot be achieved 2
- For patients with bronchospastic airway disease requiring a beta-blocker, bisoprolol (a cardioselective agent) is preferred over non-selective agents 2