Systolic dysfunction and heart failure are major public health problems associated with a significant risk of morbidity and mortality. During the past 2 decades, considerable progress has been made in defining the underlying pathophysiology and the appropriate therapies in heart failure. In patients with chronic heart failure (CHF), sustained sympathetic overactivation leads to down-regulation of beta receptors and uncoupling of the receptors from adenylate cyclase. The clear understanding of the pivotal role of sympathetic overactivation in CHF has led to the evaluation of beta- blocker therapy in CHF. A number of large randomized clinical trials have been conducted with a variety of beta-blockers, and although most of them have shown benefit, there have been differing findings with different molecules. beta-blockers are now considered part of the standard therapy for all patients with symptomatic CHF. Despite the strong evidence supporting their use, beta-blockers continue to be underutilized in CHF.