Bisoprolol

Selective beta-adrenergic blockers

ATC code: C07AB07 (Bisoprolol)

Mechanism of action

Highly selective beta-1 adrenergic receptor blocker. Reduces heart rate, cardiac output, and renin secretion. At therapeutic doses it has negligible effect on beta-2 receptors in bronchi and vasculature. In heart failure it reduces sympathoadrenal neurohormonal activation and improves myocardial remodeling.

Indications

Atrial fibrillation

First line

Beta-blockers are first-line rate control agents in atrial fibrillation per ESC 2020. Bisoprolol is given to achieve a target resting HR below 110 bpm (lenient control) or below 80 bpm (strict control when indicated).

Ventricular rate control in atrial fibrillation.

Coronary artery disease

First line

Beta-blockers are first-line anti-anginal therapy in stable angina. They reduce heart rate, myocardial oxygen demand, and angina frequency. Target resting heart rate is 55–60 bpm.

Heart failure

First line

Bisoprolol is one of three beta-blockers proven to reduce mortality in HFrEF (alongside carvedilol and metoprolol succinate). The CIBIS-II trial showed a 34 % reduction in all-cause mortality. Start at 1.25 mg daily, titrate every 2 weeks to target dose of 10 mg.

HFrEF (LVEF 40 % or below).

Hypertension

First line

Beta-blockers are one of the five main antihypertensive classes. Bisoprolol is given at 5–10 mg once daily. Particularly preferred in patients with comorbid CAD, HF, or tachyarrhythmias. ESC/ESH 2024 notes that beta-blockers are less effective for stroke prevention compared to other classes.

Practical notes

Timing and administration

Take in the morning, once daily, with or without food. Do not stop abruptly – taper over 1–2 weeks. Sudden withdrawal can trigger rebound tachycardia and angina exacerbation.

Monitoring

Monitor heart rate and BP at each visit. If resting HR drops below 50 bpm or systolic BP below 100 mmHg, reduce dose. In HF patients, transient worsening of symptoms during titration does not warrant discontinuation unless significant hypotension or bradycardia develops.

Safety

Contraindications

Second- or third-degree AV block without a pacemaker
Sick sinus syndrome without a pacemaker
Severe bradycardia (HR below 50 bpm before treatment)
Severe bronchial asthma or COPD with significant bronchospasm
Pheochromocytoma without prior alpha-blockade
Cardiogenic shock

Serious adverse effects

AV block
Bronchospasm (rare with selective beta-blockers, but possible)
Masking of hypoglycemia in diabetic patients (tachycardia does not develop)

Common adverse effects

Bradycardia
Hypotension
Fatigue, weakness
Dizziness
Cold extremities

PregnancyFDA C

FDA category C. Beta-blockers can cause fetal growth restriction and neonatal bradycardia. If antihypertensive therapy is needed in pregnancy, labetalol or methyldopa are preferred.

Breastfeeding

Excreted in breast milk. Risk to the infant at standard doses is considered low, but the neonate should be monitored for bradycardia.