Uses of Atenolol in Clinical Practice
Atenolol should not be used as first-line therapy for hypertension as it is less effective than placebo in reducing cardiovascular events. 1, 2
Primary Indications
Atenolol is FDA-approved for three main indications:
For hypertension management, atenolol is not recommended as a first-line agent due to its inferior cardiovascular outcomes compared to other beta-blockers 1, 2
Dosing Considerations
- For hypertension, the initial dose is typically 50 mg once daily, which may be increased to 100 mg once daily if needed 3
- For angina pectoris, starting with 50 mg once daily, potentially increasing to 100 mg or even 200 mg once daily for optimal effect 3, 4
- For acute myocardial infarction, treatment begins with intravenous administration followed by oral dosing 3
- Dosage adjustment is required in elderly patients and those with renal impairment 3
Pharmacological Properties
- Atenolol is a beta-1 selective (cardioselective) adrenergic receptor blocking agent without membrane stabilizing or intrinsic sympathomimetic activities 3, 5
- It has a long duration of activity (24 hours), allowing for once-daily dosing 5, 4
- Approximately 50% of an oral dose is absorbed from the gastrointestinal tract 3
- Unlike some other beta-blockers, atenolol undergoes little or no metabolism by the liver and is primarily eliminated by renal excretion 3, 5
Limitations and Warnings
- The American College of Cardiology/American Heart Association guidelines explicitly state that atenolol should not be used because it is less effective than placebo in reducing cardiovascular events 1
- Preferred beta-blockers for hypertension and stable ischemic heart disease include carvedilol, metoprolol tartrate, metoprolol succinate, nadolol, bisoprolol, propranolol, and timolol 1, 6
- Atenolol may still be used in combination therapy for patients with persistent hypertension and angina when other preferred agents are not suitable 2
Special Populations
- In patients with renal impairment, dosage should be adjusted as atenolol is primarily eliminated by the kidneys 3, 5
- For patients with creatinine clearance 15-35 mL/min/1.73m², maximum dosage is 50 mg daily 3
- For patients with creatinine clearance <15 mL/min/1.73m², maximum dosage is 25 mg daily 3
- While atenolol is cardioselective, this selectivity is not absolute and diminishes at higher doses 3
Clinical Efficacy
- Multiple studies have shown that atenolol effectively reduces blood pressure and improves exercise tolerance in patients with angina 7, 4, 8, 9
- The optimal dose for treating mild to moderate hypertension appears to be 100 mg daily 8
- The magnitude of hypotensive response is related to the initial systolic blood pressure and the degree of inhibition of exercise tachycardia 9
Common Pitfalls
- Abrupt cessation of atenolol should be avoided to prevent rebound hypertension 2
- Despite its effectiveness in lowering blood pressure, atenolol has been shown to be less effective than other agents in reducing cardiovascular events 1, 2
- For patients with stable ischemic heart disease, the target blood pressure should be less than 130/80 mm Hg 1
- Monitoring for side effects including bradycardia, hypotension, and worsening heart failure is essential 2