Chodosh S, Tuck J, Blasucci D J
Veterans Administration Medical Center, Boston, Massachusetts 02108.
J Cardiovasc Pharmacol. 1988;11 Suppl 2:S18-24. doi: 10.1097/00005344-198800000-00005.
Dilevalol combines a nonselective blocking action on beta-receptors with selective beta 2-agonist activity. In this double-blind, three-way, crossover study, the effects of relatively high single doses of dilevalol (400 mg), metoprolol (200 mg), a placebo on pulmonary function and their interaction with isoproterenol (160 and 480 micrograms) were evaluated in 16 patients with reversible bronchial asthma [isoproterenol-induced increase in forced expiratory volume in 1 s (FEV1) of greater than or equal to 15%]. When the lowest or minimum values observed during the 2 h postdrug evaluation period were considered, there was no significant difference from baseline in the percentage change in FEV1 after placebo (-4.4%) and dilevalol (-10%), with the difference between these treatments not being statistically significant. However, following metoprolol, FEV1 decreased by 18.3%, a decrease significantly different (p less than 0.01), from baseline and from the effects of placebo (p less than 0.01), although not from dilevalol. Furthermore, following metoprolol, 7 of 16 patients (44%) showed a greater than or equal to 20% decrease in FEV1 as compared to only 3 patients (19%) following dilevalol and 1 patient (6%) following placebo. The effects of the three treatments on forced vital capacity (FVC) and maximal midexpiratory flow (MMEF) were qualitatively similar to those observed in FEV1. Both dilevalol and metoprolol similarly and significantly (p less than or equal to 0.01) inhibited the isoproterenol (160 and 480 micrograms) response in FEV1 as compared to placebo.(ABSTRACT TRUNCATED AT 250 WORDS)
双醋洛尔兼具对β受体的非选择性阻断作用和选择性β₂激动剂活性。在这项双盲、三向、交叉研究中,对16例可逆性支气管哮喘患者[异丙肾上腺素诱发的1秒用力呼气量(FEV₁)增加≥15%]评估了相对高剂量单次服用双醋洛尔(400毫克)、美托洛尔(200毫克)、安慰剂对肺功能的影响及其与异丙肾上腺素(160和480微克)的相互作用。当考虑给药后2小时评估期内观察到的最低或最小值时,安慰剂(-4.4%)和双醋洛尔(-10%)给药后FEV₁的百分比变化与基线相比无显著差异,这些治疗之间的差异无统计学意义。然而,服用美托洛尔后,FEV₁下降了18.3%,与基线相比以及与安慰剂的作用相比均有显著差异(p<0.01),但与双醋洛尔相比无差异。此外,服用美托洛尔后,16例患者中有7例(44%)FEV₁下降≥20%,而服用双醋洛尔后为3例(19%),服用安慰剂后为1例(6%)。三种治疗对用力肺活量(FVC)和最大呼气中期流速(MMEF)的影响在性质上与FEV₁中观察到的相似。与安慰剂相比,双醋洛尔和美托洛尔对FEV₁中异丙肾上腺素(160和480微克)反应的抑制作用相似且具有显著性(p≤0.01)。(摘要截短于250字)