The cardio-selective beta-1-blockers include atenolol, betaxolol, bisoprolol, esmolol, acebutolol, metoprolol, and nebivolol. FDA approved uses of beta-1-selective blockers include hypertension, chronic stable angina, heart failure, post-myocardial infarction, and decreased left ventricular function after a recent myocardial infarction. Non-FDA approved uses include migraine prophylaxis, treatment of arrhythmias, tremor reduction, and the symptomatic treatment of anxiety disorders. Their use is associated with decreased morbidity and mortality post-myocardial infarction. Treatment with beta-1 blockers decreases the risk of stroke, coronary artery disease, and congestive heart failure. This activity outlines the indications, mechanisms of action, methods of administration, important adverse effects, contraindications, and monitoring, of selective beta-1 antagonists, so providers can direct patient therapy in treating indicated disorders as part of the interprofessional team, with a basis on the current knowledge for optimal utilization.