The Role of β-Blockers as a Cornerstone of Cardiovascular Therapy

The β-adrenergic blockade as a therapeutic approach first emerged in the 1950s. During the past five decades, the total number of indications that have been suggested, and the remarkable number approved by regulatory agencies, places β-blockade far ahead of all competing treatments, not only in the cardiovascular area, but in all of therapeutics. Differentiation of β-adrenergic blocking agents has been made on the basis of β1 selectivity, duration of action, intrinsic sympathomimetic activity, lipophilicity, and whether or not the β-adrenergic blocking action is accompanied by an α-adrenergic blocking action. With the development of nebivolol, a β-adrenergic blocking agent that also activates nitric oxide synthase in blood vessels, comes a new therapeutic option. Endothelial dysfunction with loss of nitric oxide production is a common feature in many cardiovascular diseases. This fascinating class of drugs continues to provide us with new and important therapeutic opportunities.