Patchett P, Patchett S M, Burge P S
Br J Clin Pharmacol. 1985 Oct;20(4):349-53. doi: 10.1111/j.1365-2125.1985.tb05076.x.
Reproterol is a synthetic selective beta-adrenoceptor agonist with a xanthine side chain. The bronchial and cardiovascular responses to inhaled reproterol were studied in 14 asthmatics. The study was placebo controlled and double-blind, comparing doubling doses of reproterol from 500 micrograms-8 mg. The peak improvement in FEV1 showed a non-linear dose-response, with an initial plateau at the 1 mg dose producing a mean increase in FEV1 of 17%, but significant further improvement at the 8 mg dose, producing a mean improvement of 29% in FEV1. The time taken for improvement in airways obstruction to start shortened with increasing doses. The duration of bronchodilation was dose-dependent, with the 8 mg dose showing a significantly longer duration of action than the lower doses. The time to drop below 75% of the maximum achieved bronchodilation was 125 min, and was independent of the dose. There were no significant changes in pulse or blood pressure at any dose. The study shows that reproterol is a well tolerated selective beta 2-adrenoceptor agonist whose duration of action and peak effect can be significantly increased by increasing the dose to 8 mg, without producing more unwanted effects.
瑞普特罗是一种带有黄嘌呤侧链的合成选择性β肾上腺素能受体激动剂。在14名哮喘患者中研究了吸入瑞普特罗后的支气管和心血管反应。该研究采用安慰剂对照且为双盲设计,比较了500微克至8毫克剂量加倍的瑞普特罗。第一秒用力呼气容积(FEV1)的峰值改善呈现非线性剂量反应,在1毫克剂量时最初有一个平台期,FEV1平均增加17%,但在8毫克剂量时有显著进一步改善,FEV1平均改善29%。气道阻塞改善开始的时间随剂量增加而缩短。支气管扩张的持续时间呈剂量依赖性,8毫克剂量的作用持续时间明显长于较低剂量。降至最大支气管扩张效果的75%以下的时间为125分钟,且与剂量无关。任何剂量下脉搏或血压均无显著变化。该研究表明,瑞普特罗是一种耐受性良好的选择性β2肾上腺素能受体激动剂,将剂量增加至8毫克可显著延长其作用持续时间和增强峰值效应,且不会产生更多不良影响。