Pharmacology of third-generation beta-blockers: greater benefits, fewer risks

Abstract

The primary goals in the management of hypertension, angina pectoris, and postinfarction cases are to prevent further damage to the cardiovascular system and to reduce the risk of subsequent myocardial infarction. Of all the drugs currently available, the beta-blockers seem the most likely to achieve this aim. The search for new beta-blockers centers around the need for agents that offer the advantages of beta 1-adrenoceptor antagonism without the unwanted beta 2 effects, which may be dangerous in asthmatic patients and may make bronchitis, diabetes, and arteriopathy worse or more difficult to control. One solution is to use a selective beta 1-adrenoceptor antagonist. Another is to develop a molecule that acts as an antagonist at beta 1-adrenoceptors and as an agonist at beta 2-adrenoceptors. celiprolol is such a "third-generation" beta-blocker in that it combines both attributes, and thereby offers a clinically relevant advance. It does not seem to disrupt glucose homeostasis or exacerbate peripheral vascular disease, the lipid profile appears to be positively altered, and the risk of bronchospasm is reduced. Celiprolol is therefore both clinically and biochemically well tolerated.