From the Guidelines
Beta blockers that only affect beta-1 adrenergic receptors include metoprolol, atenolol, bisoprolol, acebutolol, and betaxolol, as they are cardioselective and primarily target beta-1 receptors in the heart. These medications are beneficial for patients with conditions such as asthma or COPD, as they are less likely to cause bronchospasm compared to non-selective beta blockers that also block beta-2 receptors in the lungs 1.
Key Characteristics of Beta-1 Selective Blockers
- Preferentially block beta-1 receptors found predominantly in the heart
- Control heart rate and contractility
- Advantages for patients with asthma or COPD due to reduced risk of bronchospasm
- Commonly prescribed for hypertension, angina, heart failure, and post-myocardial infarction management
Important Considerations
- Selectivity is dose-dependent and can be lost at higher doses
- Should be used with caution in patients with respiratory conditions
- Benefits should be weighed against potential risks
Recommended Beta-1 Selective Blockers
- Metoprolol: 50 to 200 mg twice daily
- Atenolol: 50 to 200 mg per day
- Bisoprolol: 10 mg per day
- Acebutolol: 200 to 600 mg twice daily
- Betaxolol: 10 to 20 mg per day
According to the most recent study 1, these beta-1 selective blockers are recommended for their effectiveness in managing various cardiovascular conditions while minimizing the risk of adverse effects on the lungs.
From the FDA Drug Label
Metoprolol is a beta 1-selective (cardioselective) adrenergic receptor blocker. Atenolol is a beta1-selective (cardioselective) beta-adrenergic receptor blocking agent Nebivolol is preferentially β1 selective.
The beta blockers that only affect beta 1 are not explicitly identified in the provided drug labels, as all three drugs (metoprolol, atenolol, and nebivolol) have a preferential but not absolute effect on beta 1 receptors, and may also inhibit beta 2 receptors at higher doses or concentrations 2, 3, 4.
- Key points:
- Metoprolol, atenolol, and nebivolol are all beta 1-selective blockers.
- None of these drugs exclusively affect beta 1 receptors.
- The effect on beta 2 receptors increases at higher doses or concentrations.
From the Research
Beta Blockers that Only Affect Beta 1
- Bisoprolol is a highly beta 1-selective beta-adrenoceptor blocking drug, devoid of intrinsic sympathomimetic effects 5
- It has been shown to be effective in reducing systolic and diastolic blood pressures in patients with hypertension for a 24-hour dosing interval 6
- Bisoprolol is also used in the treatment of angina pectoris, arrhythmias, and heart failure, with a favorable side-effect profile 5, 6
- Other beta blockers such as metoprolol and betaxolol also have beta 1-selective properties, but may not be as selective as bisoprolol 7, 8
- The choice of beta blocker is important, as benefit is not a class-effect, and some beta blockers may have diminished efficacy due to intrinsic sympathomimetic activity (ISA) 7
Key Characteristics of Beta 1-Selective Beta Blockers
- Highly selective for beta 1-adrenoceptors, with minimal effects on beta 2-adrenoceptors 5
- Devoid of intrinsic sympathomimetic effects, which can diminish efficacy in certain conditions 5, 6
- Effective in reducing heart rate and blood pressure, with beneficial hemodynamic effects in patients with myocardial ischemia 5, 6
- May have a favorable side-effect profile, with minimal effects on glucose tolerance and plasma lipid profiles 6