Mackay A D, Gribbin H R, Baldwin C J, Tattersfield A E
Clin Pharmacol Ther. 1981 Jan;29(1):1-6. doi: 10.1038/clpt.1981.1.
We have applied a new method for quantitative measurement of bronchial beta adrenoceptor blockade to a new beta adrenoceptor antagonist, bevantolol. Dose-response curves to a beta agonist, albuterol, were obtained in six normal subjects by measuring specific airway conductance (sGaw) after increasing doses of inhaled albuterol. These were repeated on three separate occasions 2 hr after subjects had taken oral placebo or bevantolol (75 or 150 mg), double-blind in random order. The dose-response curves after bevantolol 75 mg were displaced in the right of placebo in four subjects and after 150 mg were displaced to the right of placebo in all subjects. The mean dose ratios for bevantolol 75 or 150 mg were 1.02 and 2.77, much the same as those obtained in the same subjects after practolol 100 and 200 mg and considerably less than that after propranolol 40 mg. The mean reductions in exercise heart rate were 25% and 29% after bevantolol 75 and 150 mg. Our data show that bronchial beta blockade after a beta blocking drug can be assessed quantitatively in many by a double-blind technique.
我们已将一种用于定量测量支气管β肾上腺素能受体阻滞的新方法应用于一种新的β肾上腺素能受体拮抗剂——贝凡洛尔。通过测量吸入递增剂量沙丁胺醇后特定气道传导率(sGaw),在6名正常受试者中获得了对β激动剂沙丁胺醇的剂量反应曲线。在受试者口服安慰剂或贝凡洛尔(75或150毫克)2小时后,以随机双盲顺序在三个不同场合重复进行这些测量。75毫克贝凡洛尔后的剂量反应曲线在4名受试者中向右偏离安慰剂,150毫克贝凡洛尔后的剂量反应曲线在所有受试者中均向右偏离安慰剂。75毫克和150毫克贝凡洛尔的平均剂量比分别为1.02和2.77,与100毫克和200毫克心得宁在相同受试者中获得的剂量比大致相同,且远低于40毫克普萘洛尔后的剂量比。75毫克和150毫克贝凡洛尔后运动心率的平均降低分别为25%和29%。我们的数据表明,许多β受体阻滞剂后的支气管β阻滞可用双盲技术进行定量评估。