Atenolol is a cardio selective β1 adrenergic receptor blocker extensively used in the prevention and treatment of cardiovascular disorders. It produces its therapeutic effects primarily by reducing heart rate, myocardial contractility, and systemic blood pressure, thereby decreasing cardiac workload and oxygen demand. Atenolol has gained wide clinical acceptance due to its relative selectivity for cardiac β1 receptors, which minimizes adverse respiratory and metabolic effects commonly associated with non selective beta blockers. Its hydrophilic nature limits central nervous system penetration, contributing to improved tolerability during long term therapy. Atenolol is routinely prescribed for hypertension, chronic stable angina, cardiac arrhythmias, and secondary prevention following myocardial infarction. This review comprehensively discusses the pharmacological profile of atenolol, including its mechanism of action, pharmacological effects, pharmacokinetics, therapeutic applications, adverse reactions, contraindications, drug interactions, and overall clinical relevance.