Dilevalol: A Selective Beta‐2 Adrenergic Agonist Vasodilator with Beta Adrenergic Blocking Activity

Dilevalol is the R-R' optical isomer of labetalol and differs pharmacologically from the racemic mixture in the following ways: it is seven-fold more potent as a selective beta-2 agonist; it is four times more potent as a nonselective beta antagonist; it has no clinically significant alpha antagonist property. Dilevalol is a vasodilator and reduces blood pressure by reducing systemic vascular resistance. It has a half-life of 15-18 hours, and is demonstrated to be effective as an antihypertensive agent for 24-30 hours. Hemodynamic studies in humans show that following administration of dilevalol either orally or intravenously, blood pressure falls as a consequence of a decrease in systemic vascular resistance. Cardiac index is unchanged and heart rate decreases slightly. Dilevalol is shown to cause regression of left ventricular hypertrophy in younger individuals, to improve left ventricular performance and to have no effect on parameters of renal function. Prospective double-blinded clinical trials in comparison with placebo, propranolol, metoprolol and atenolol were conducted and demonstrate dilevalol to be an effective antihypertensive agent with a favorable side effect profile with a particularly low incidence of central nervous system side effects.