Vasodilating beta-adrenoceptor blockers as cardiovascular therapeutics.

beta-Adrenoceptor blocking agents (beta-blockers) have been established as therapeutics for treatment of patients with hypertension, ischemic heart diseases, chronic heart failure, arrhythmias, and glaucoma. However, their clinical use is limited because some patients are adversely affected by their side effects. The discovery of cardioselective (beta(1)-selective) blockers has overcome some of the problems. Current retrospective studies have revealed that vasodilating beta-blockers (so-called beta-blockers of the third generation) have advantages over the conventional type of beta-blockers in terms of minimizing the adverse effects and improving the disease-derived dysfunction, thus enhancing the quality of life variables. Some of the possible advantages include improvement of insulin resistance, decrease in low-density lipoprotein cholesterol in association with increase in high-density lipoprotein cholesterol, attenuation of bronchial asthma attack and respiratory dysfunction, alleviation of coronary vasospasm provocation, peripheral circulatory disturbances, and erectile dysfunction, and better patient compliance. Release of nitric oxide, antioxidant action, beta(2)-adrenoceptor activation, Ca(2+) entry blockade, and other mechanisms underlying the vasodilating action may be responsible for the beneficial therapeutic effects of these agents.