Propranolol

Propranolol is a 1st-generation, nonselective beta-blocker that blocks both β1 and β2 receptors.

It is one of the oldest and most widely studied beta-blockers.

Classification: • 1st Generation (Nonselective) • No intrinsic sympathomimetic activity (ISA)

Beta-Blockers Overview


Mechanism of Action

Blocks:

• β1 receptors → ↓ Heart rate, ↓ contractility, ↓ renin • β2 receptors → ↓ Bronchodilation, ↓ peripheral vasodilation

Net Effects:

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

Because it blocks β2 receptors, bronchospasm is possible.


Indications

Cardiovascular

• Hypertension (not first-line) • Angina • Post-myocardial infarction • Certain arrhythmias

Hypertension ModuleAnti-Anginal ModuleDysrhythmias Module


Non-Cardiac (High-Yield Uses)

• Essential tremor • Migraine prophylaxis • Hyperthyroidism (symptom control) • Performance anxiety • Portal hypertension (variceal bleed prevention)

These extra-cardiac uses make propranolol uniquely versatile.


Pharmacokinetics

• Lipophilic (crosses blood-brain barrier) • Extensive first-pass metabolism • Short to moderate half-life • Available in immediate and extended-release forms

CNS penetration explains:

• Fatigue • Depression • Vivid dreams


Adverse Effects

• Bradycardia • Hypotension • Bronchospasm • Fatigue • Depression • Sexual dysfunction • Masked hypoglycemia

Avoid in:

• Asthma • Severe COPD


Contraindications

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

Use caution in:

• Diabetes (masks hypoglycemia) • Peripheral vascular disease


Propranolol vs Cardioselective Agents

Propranolol: • Blocks β1 and β2 • Higher bronchospasm risk • Greater CNS penetration

Cardioselective agents (e.g., Metoprolol): • Primarily block β1 • Safer in reactive airway disease


Clinical Pearls

✔ Prototype nonselective beta-blocker ✔ Excellent for migraine and tremor ✔ Avoid in asthma ✔ Crosses blood-brain barrier ✔ Not preferred in HFrEF

For heart failure mortality benefit, see:

CarvedilolMetoprolol SuccinateBisoprolol


Related:

Beta-Blockers OverviewHypertension ModuleAnti-Anginal ModuleDysrhythmias ModuleReturn to Cardiovascular Modules