Pharmacological and therapeutic properties of an ideal beta-blocker

With hindsight it is now possible to define some of the additional pharmacological characteristics which enhance the pharmacodynamic and therapeutic efficacy of a drug whose primary purpose is to antagonize competitively sympathetic stimulation of the heart. The ideal pharmacokinetic profile for a beta-blocker includes ready and unimpeded absorption; a predominantly hydrophilic distribution; a relatively long duration of pharmacological activity and alternative routes of elimination. The ideal pharmacodynamic activity of such a drug involves a number of factors, including the essential element of beta 1-adrenoceptor selectivity. In addition, moderate beta 2-adrenoceptor agonist activity and mild stimulation of myocardial contractibility afford enhanced haemodynamic efficacy. The intrinsic ability to relax vascular and bronchial smooth muscle are also highly desirable ancillary pharmacodynamic properties. From the therapeutic aspect, a drug administered with the primary objective of reducing myocardial ischaemia in patients with a coronary heart disease, or of lowering blood pressure in patients with hypertension, should not only prove effective in clinical practice, but should also be shown to have beneficial haemodynamic properties and a minimum of undesirable pharmacological effects. The unique pharmacological profile of celiprolol appears to allow fulfillment of many of these desirable objectives.