ABSTRACT
Dilevalol is a long-acting antihypertensive drug that has been demonstrated in animals to combine specific beta 2-agonist-mediated vasodilation with nonspecific beta blockade. To document vasodilation in humans, single oral doses of dilevalol, 200 mg, and placebo were randomly administered to 12 untreated hypertensive patients. Dilevalol produced significant reductions (p less than or equal to 0.01) in diastolic blood pressure throughout a 24-hour period relative to placebo, without changing heart rate. Forearm blood flow, measured hourly over the initial 4 hours after dosing, demonstrated a shift to a more vasodilated state after dilevalol administration, with significant increases in minimal forearm blood flow (4.0 vs 2.9 ml/dl tissue/min, dilevalol vs placebo, respectively; p = 0.05) and in mean average forearm blood flow (5.3 vs 4.0 ml/dl tissue/min, dilevalol vs placebo; p = 0.04). Similarly, dilevalol produced a decrease in mean forearm vascular resistance (26.5 vs 34.6 mm Hg/ml/dl tissue/min, dilevalol vs placebo; p = 0.02). In the absence of a change in heart rate, the acute hypotensive response to dilevalol in these patients appears to have resulted primarily from vasodilation and reduced vascular resistance.
