Bianco S
Institute of Respiratory Diseases, University of Siena, Sclavo Hospital, Italy.
Respiration. 1989;55 Suppl 2:20-7. doi: 10.1159/000195766.
The protective effect of broxaterol against bronchial hyperresponsiveness has been assessed in several double-blind randomized controlled studies in stable asthmatic patients. In three cross-over studies, broxaterol (400 micrograms by metered dose inhaler) has been shown to significantly reduce methacholine responsiveness 30, 60 and 120 min after dosing. The protective effect was similar to that obtained with terbutaline (500 micrograms), but there was a trend toward a higher activity of fenoterol (400 micrograms), even if counterbalanced by a more frequent occurrence of side effects. Broxaterol 0.5 mg by oral route provided a significant greater protection against the exercise-induced bronchospasm than 0.02 mg of clenbuterol and a placebo. Also in children, broxaterol 0.25 mg as nebulizer solution significantly prevented exercise-induced bronchospasm versus placebo, and this effect was seen to be associated with an improvement in maximal working capacity. Prevention of bronchospasm following 3 or 4 consecutive challenges with inhaled distilled water mist was demonstrated after oral and aerosol administration of broxaterol. This effect was not significantly different from that observed with salbutamol, if administered by aerosol. Finally, in a cross-over placebo-controlled study, broxaterol (400 micrograms by aerosol) significantly inhibited allergen-induced immediate bronchoconstriction. These data suggest that broxaterol represents a new valid alternative to the most effective beta 2-stimulants now commonly used.
在多项针对稳定期哮喘患者的双盲随机对照研究中,已评估了丙卡特罗对支气管高反应性的保护作用。在三项交叉研究中,已证实丙卡特罗(通过定量吸入器给予400微克)在给药后30、60和120分钟可显著降低乙酰甲胆碱反应性。其保护作用与特布他林(500微克)相似,但非诺特罗(400微克)的活性有更高的趋势,即便其副作用更频繁出现而有所抵消。口服0.5毫克丙卡特罗比0.02毫克克仑特罗及安慰剂对运动诱发的支气管痉挛提供了显著更强的保护作用。同样在儿童中,雾化溶液形式的0.25毫克丙卡特罗与安慰剂相比可显著预防运动诱发的支气管痉挛,且该作用与最大工作能力的改善相关。口服和气雾剂给予丙卡特罗后,证实可预防吸入蒸馏水雾连续3次或4次激发后的支气管痉挛。若通过气雾剂给药,该作用与沙丁胺醇观察到的作用无显著差异。最后,在一项交叉安慰剂对照研究中,丙卡特罗(气雾剂形式400微克)可显著抑制变应原诱发的即刻支气管收缩。这些数据表明,丙卡特罗是目前常用的最有效的β2激动剂的一种新的有效替代药物。