Freedman B J, Meisner P, Hill G B
Thorax. 1968 Nov;23(6):590-7. doi: 10.1136/thx.23.6.590.
The actions of the following pressurized bronchodilators were compared by administration to 24 asthmatics: (1) Medihaler Iso Forte, (2) Alupent, (3) Medihaler-duo, (4) Bronchilator, and (5) Prenomiser Plus. These contained one or more of the following: isoprenaline, orciprenaline, isoetharine, phenylephrine, atropine methonitrate, and thenyldiamine. The dose was a single discharge from the container. The response was assessed by calculating the mean percentage change in F.E.V. at intervals after inhalation. The mean peak rises were respectively (1) 49·4%, (2) 43·6%, (3) 36·2%, (4) 33·5%, and (5) 23·5%. The amplitude of peak response to isoprenaline was related to the logarithm of the dose. Weight for weight, orciprenaline had a peak bronchodilator activity 41·5% that of isoprenaline and isoetharine 50%. The preparations did not differ significantly in the time taken to reach maximum response, which varied from 5 to 60 minutes; three-quarters of the maxima occurred within 15 minutes. The half-life for Alupent was 2 hours; for Medihaler-duo, which contains 240 μg. of phenylephrine per dose, it was 1¼ hours; for the remaining preparations it was about 1 hour. The decay rate, after the first half-hour, was 6% of the basal F.E.V. per hour for Medihaler-duo; for the other preparations it was 10-12%. In the doses given, Alupent yielded 20% and 30% increases lasting 130 and 67 minutes; after Medihaler Iso Forte these lasted 78 and 46 minutes. Similar comparative experiments, designed to eliminate effects of dosage difference, are desirable. Rebound bronchoconstriction occurred in 23% of 92 experiments. There was no response to propellent alone. The mean percentage change in F.E.V. may not be the best way of expressing results.
对24名哮喘患者使用以下几种加压支气管扩张剂并比较其作用:(1) 强力异丙肾上腺素定量气雾剂;(2) 间羟异丙肾上腺素;(3) 异丙肾上腺素-阿托品定量气雾剂;(4) 支气管扩张剂;(5) 普瑞诺米赛加强型。这些药物含有以下一种或多种成分:异丙肾上腺素、间羟异丙肾上腺素、异他林、去氧肾上腺素、硝酸甲胆碱阿托品和茶苯海明。剂量为容器的单次喷出量。通过计算吸入后不同时间点第一秒用力呼气量(F.E.V.)的平均百分比变化来评估反应。平均峰值上升分别为:(1) 49.4%;(2) 43.6%;(3) 36.2%;(4) 33.5%;(5) 23.5%。对异丙肾上腺素的峰值反应幅度与剂量的对数相关。按重量计算,间羟异丙肾上腺素的峰值支气管扩张活性为异丙肾上腺素的41.5%,异他林为50%。这些制剂达到最大反应所需时间无显著差异,时间从5分钟到60分钟不等;四分之三的最大值出现在15分钟内。间羟异丙肾上腺素的半衰期为2小时;异丙肾上腺素-阿托品定量气雾剂每剂含240μg去氧肾上腺素,其半衰期为1.25小时;其余制剂的半衰期约为1小时。半小时后,异丙肾上腺素-阿托品定量气雾剂的衰减率为每小时基础F.E.V.的6%;其他制剂为10%-12%。在给定剂量下,间羟异丙肾上腺素产生20%和30%的增加,持续130分钟和67分钟;强力异丙肾上腺素定量气雾剂给药后,增加持续78分钟和46分钟。需要进行类似的比较实验以消除剂量差异的影响。在92次实验中,23%出现了反跳性支气管收缩。单独使用抛射剂无反应。F.E.V.的平均百分比变化可能不是表达结果的最佳方式。