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Dilevalol: A Selective Beta‐2 Adrenergic Agonist Vasodilator with Beta Adrenergic Blocking Activity
Author(s) -
Wallin J. David,
Frishman William H.
Publication year - 1989
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1989.tb03280.x
Subject(s) - labetalol , medicine , propranolol , metoprolol , atenolol , blood pressure , vascular resistance , vasodilation , hemodynamics , cardiology , antagonist , receptor
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 he 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.