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首页> 外文期刊>Pulmonary pharmacology & therapeutics >A comparison of salmeterol and formoterol in attenuating airway responses to short-acting beta2-agonists.
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A comparison of salmeterol and formoterol in attenuating airway responses to short-acting beta2-agonists.

机译:沙美特罗和福莫特罗在减弱对短效β2-激动剂的气道反应中的比较。

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摘要

In vitro data suggest that salmeterol, contrary to formoterol, can partly antagonise the effect of short-acting beta(2)-agonist rescue medication. To explore whether this occurs in vivo, we compared the effects of increasing doses (200-3200 microg) of fenoterol on the recovery of methacholine induced bronchoconstriction as well as PD(20) methacholine in 23 asthmatic patients, during two-week treatment periods with placebo, and standard doses of salmeterol or formoterol in a double blind, double-dummy, crossover study. Salmeterol showed a slightly higher propensity for the development of bronchodilator tolerance. The recovery of methacholine induced bronchoconstriction was more complete during regular use of formoterol relative to salmeterol. During regular use of both long-acting beta(2)-agonists the bronchoprotective efficacy of fenoterol was attenuated, but this was more pronounced during salmeterol than during formoterol. The mean maximum increase in PD(20) metacholine after the highest dose of fenoterol was 3.97 DD during placebo, 2.47 DD during formoterol (p<0.001) and 1.81 DD during salmeterol treatment (p<0.001). We conclude that in asthmatic patients the efficacy of short-acting beta(2)-adrenoceptor agonists can be significantly attenuated during regular use of long-acting beta(2)-agonists. In this respect, differences were observed between salmeterol and formoterol that may represent the expression of partial antagonism by salmeterol.
机译:体外数据表明,沙美特罗与福莫特罗相反,可以部分拮抗短效β(2)-激动剂抢救药物的作用。为了探讨这种情况是否在体内发生,我们比较了在两周的治疗期间,在23位哮喘患者中,增加剂量的非诺特罗(200-3200微克)的非诺特罗对乙酰甲胆碱引起的支气管收缩以及PD(20)乙酰甲胆碱恢复的影响。一项双盲,双模拟,交叉研究中的安慰剂和标准剂量的沙美特罗或福莫特罗。沙美特罗显示出更高的支气管扩张药耐受性倾向。相对于沙美特罗,在定期使用福莫特罗期间,乙酰甲胆碱诱导的支气管收缩的恢复较完全。在定期使用两种长效β(2)-激动剂期间,非诺特罗的支气管保护功效减弱,但是在沙美特罗期间比在福莫特罗期间更明显。 Fenoterol最高剂量后,PD(20)乙酰胆碱的平均最大增加值在安慰剂期间为3.97 DD,在福莫特罗期间为2.47 DD(p <0.001),在沙美特罗治疗期间为1.81 DD(p <0.001)。我们得出的结论是,在哮喘患者中,在定期使用长效β(2)-激动剂的过程中,短效β(2)-肾上腺素受体激动剂的功效可能会大大减弱。在这方面,观察到沙美特罗和福莫特罗之间存在差异,这可能代表沙美特罗表达了部分拮抗作用。

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