Propranolol is NOT Cardioselective
Propranolol is a nonselective beta-adrenergic blocker that blocks both beta-1 receptors (in the heart) and beta-2 receptors (in the lungs and blood vessels), making it fundamentally different from cardioselective agents like metoprolol, atenolol, or bisoprolol. 1
Pharmacologic Classification
- Propranolol competitively blocks both beta-1 and beta-2 adrenergic receptors without selectivity 1
- Beta-1 receptors are located primarily in the myocardium and control heart rate, contractility, and AV node conduction 2
- Beta-2 receptors are located in vascular and bronchial smooth muscle; their blockade causes vasoconstriction and bronchoconstriction 2
- This nonselective blockade distinguishes propranolol from cardioselective agents like metoprolol (beta-1 selective) 2
Clinical Implications of Nonselective Blockade
The lack of cardioselectivity has important clinical consequences:
- Respiratory effects: Propranolol causes more bronchoconstriction than cardioselective agents and should be avoided in patients with asthma or obstructive airway disease 2
- Peripheral vascular effects: Beta-2 blockade leads to peripheral vasoconstriction, which can worsen symptoms in patients with peripheral vascular disease 3
- Metabolic effects: Nonselective beta blockade may cause more hypoglycemia and mask hypoglycemic symptoms compared to cardioselective agents 4
Comparison with Cardioselective Agents
The ACC/AHA guidelines explicitly distinguish propranolol from cardioselective beta blockers:
- Cardioselective agents (beta-1 selective): metoprolol, atenolol, bisoprolol, esmolol, betaxolol 2
- Nonselective agents: propranolol, nadolol, timolol 2
- When patients have reactive airway disease or COPD, guidelines recommend using "low doses of a beta-1–selective agent" rather than nonselective agents like propranolol 2
Practical Prescribing Guidance
When beta-2 blockade is problematic:
- In patients with mild wheezing or COPD, use a cardioselective agent like metoprolol at reduced doses (e.g., 12.5 mg) rather than propranolol 2
- Cardioselective beta blockers do not produce clinically significant adverse respiratory effects in most COPD patients, whereas nonselective agents like propranolol carry higher risk 2
- For hypertension management, cardioselective agents (metoprolol, bisoprolol) are preferred over nonselective agents like propranolol 2
When nonselective blockade may be acceptable: