Ruffin R E, Kenworthy M C, Newhouse M T
Clin Pharmacol Ther. 1978 Mar;23(3):338-45. doi: 10.1002/cpt1978233338.
A radiotracer technique is described which enables direct measurement of the dose and distribution of inhaled aerosol bronchodilator in man. The mean (+/-SD) amounts of the B2-adrenergic agonist, fenoterol, administered to a group of 12 asthmatic subjects in a double-blind randomized fashion were: placebo, 0 microgram; low dose, 5.6 (+/-1.2) microgram; medium dose, 32.7 (+/-7.3) microgram; and high dose, 127.5 (+/-29.2) microgram, with a mean of 86.3% of the total subject dose being deposited in the lungs. The medium and high doses of fenoterol produced similar increases above baseline in forced expired volume in 1 sec (FEV1), maximum flow at 50% of vital capacity (V max 50), and maximum flow at 25% of vital capacity (V max 25). These increases were greater than those with placebo for the entire 4-hr study (p less than 0.01). The low dose of fenoterol was more effective than placebo in increasing FEV1, V max 50, and V max 25 above baseline values (p less than 0.05), but not for the entire 4-hr study. The high-dose fenoterol caused palpitations and tremor in 3 of the 12 subjects, and the medium-dose fenoterol caused palpitations in one of these subjects.
本文描述了一种放射性示踪技术,该技术能够直接测量人体吸入的气溶胶支气管扩张剂的剂量和分布。以双盲随机方式给予一组12名哮喘患者β2肾上腺素能激动剂非诺特罗,其平均(±标准差)剂量为:安慰剂,0微克;低剂量,5.6(±1.2)微克;中剂量,32.7(±7.3)微克;高剂量,127.5(±29.2)微克,总给药剂量的平均86.3%沉积在肺部。中剂量和高剂量的非诺特罗使1秒用力呼气容积(FEV1)、肺活量50%时的最大流速(V max 50)和肺活量25%时的最大流速(V max 25)较基线水平有相似程度的增加。在整个4小时的研究中,这些增加幅度大于安慰剂组(p<0.01)。低剂量的非诺特罗在使FEV1、V max 50和V max 25高于基线值方面比安慰剂更有效(p<0.05),但在整个4小时的研究中并非如此。高剂量的非诺特罗在12名受试者中有3人出现心悸和震颤,中剂量的非诺特罗在其中1名受试者中引起心悸。