Lambeth M A, Barnes R W, Given B D, Affrime M B
Department of Surgery, University of Arkansas Medical Center, Little Rock.
Am J Cardiol. 1989 Jun 5;63(19):17I-20I. doi: 10.1016/0002-9149(89)90123-9.
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.
双醋洛尔是一种长效抗高血压药物,在动物实验中已证明它能将特定的β2受体激动剂介导的血管舒张作用与非特异性β受体阻滞作用相结合。为了证实双醋洛尔在人体中的血管舒张作用,对12名未经治疗的高血压患者随机给予单次口服剂量的200毫克双醋洛尔和安慰剂。与安慰剂相比,双醋洛尔在24小时内可显著降低舒张压(p≤0.01),且不改变心率。给药后最初4小时内每小时测量一次前臂血流量,结果显示服用双醋洛尔后血管舒张状态增强,最小前臂血流量(双醋洛尔组与安慰剂组分别为4.0 vs 2.9毫升/分/组织;p = 0.05)和平均前臂血流量(双醋洛尔组与安慰剂组分别为5.3 vs 4.0毫升/分/组织;p = 0.04)均显著增加。同样,双醋洛尔可使平均前臂血管阻力降低(双醋洛尔组与安慰剂组分别为26.5 vs 34.6毫米汞柱/毫升/分/组织;p = 0.02)。在心率无变化的情况下,这些患者对双醋洛尔的急性降压反应似乎主要是由血管舒张和血管阻力降低所致。