Bisoprolol

Bisoprolol is a 2nd-generation, highly β1-selective beta-blocker.

It reduces heart rate, contractility, and renin release with minimal β2 activity at therapeutic doses.

Classification: • 2nd Generation (Cardioselective) • No intrinsic sympathomimetic activity (ISA)

Mechanism of Action

Selective β1 blockade:

• ↓ Heart rate • ↓ Contractility • ↓ AV nodal conduction • ↓ Renin release

Net Effects:

• ↓ Cardiac output • ↓ Blood pressure • ↓ Myocardial oxygen demand

High β1 selectivity makes it safer in patients with reactive airway disease compared to nonselective agents.

Selectivity is dose-dependent.

• Proven mortality benefit • Reduces hospitalizations • Part of guideline-directed medical therapy (GDMT)

Evidence-based HFrEF beta-blockers:

• Effective antihypertensive • Not first-line for uncomplicated HTN

• Reduces myocardial oxygen demand • Used post-MI

• Rate control in atrial fibrillation • Suppress supraventricular tachycardia

• Start low • Titrate slowly every 2–4 weeks • Initiate only when patient is euvolemic • Avoid starting during acute decompensation

• Bradycardia • Hypotension • Fatigue • Dizziness • Masked hypoglycemia

Lower bronchospasm risk than nonselective agents.

• Severe bradycardia • High-grade AV block (without pacemaker) • Cardiogenic shock • Acute decompensated heart failure

Use caution in: • Asthma (though safer than nonselective agents) • Severe hypotension

Carvedilol: • α1 + β blockade • More vasodilation • More orthostatic hypotension

Metoprolol Succinate: • β1 selective • Extended-release

Bisoprolol: • Highly β1 selective • Once-daily dosing • Strong mortality data

All three reduce mortality in HFrEF.

✔ One of three mortality-reducing beta-blockers in HFrEF

✔ Highly β1 selective

✔ Once-daily dosing

✔ Safer in mild reactive airway disease

✔ Not first-line for uncomplicated hypertension