The role of beta-blockers as a cornerstone of cardiovascular therapy.

The beta-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 beta-blockade far ahead of all competing treatments, not only in the cardiovascular area, but in all of therapeutics. Differentiation of beta-adrenergic blocking agents has been made on the basis of beta1 selectivity, duration of action, intrinsic sympathomimetic activity, lipophilicity, and whether or not the beta-adrenergic blocking action is accompanied by an alpha-adrenergic blocking action. With the development of nebivolol, a beta-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.