Hegardt B, Löwhagen O, Svedmyr N
Allergy. 1980 Mar;35(2):105-12. doi: 10.1111/j.1398-9995.1980.tb01724.x.
The equipotent bronchodilating doses of terbutaline and a new beta-agonist KWD 2131 with a relatively stronger anti-allergic (inhibition of mediator release) than bronchodilating effect given in nebulized form was estimated in eight patients with intrinsic asthma. The subthreshold bronchodilating dose of KWD 2131 was also evaluated. The study was a 2-day, single-blind cross-over comparison between cumulative doses of KWD 2131 (0.5 mg to 12 mg) and terbutaline (0.05 mg to 1.2 mg). Both drugs gave a dose-dependent bronchodilating effect as measured spirometrically. It was already statistically significant at the 0.05 mg dose of terbutaline, but not until the cumulative 1.5 mg dose (0.5 + 1 mg) of KWD 2131. The median value of the bronchodilating potency of terbutaline relative to KWD 2131 was 30. The influence of the two substances on tremor and the cardiovascular system was minimum and clinically unimportant. The search for the subthreshold bronchodilating dose of KWD 2131 was of interest, as this dose was to be used in a subsequent antigen provocation study in order to selectively evaluate KWD 2131's anti-allergic property. The mean subthreshold bronchodilating dose of KWD 2131 was 1 mg. However, four of the eight patients showed bronchodilatation at the 1 mg dose, and two of the four also at 0.5 mg.
在8名内源性哮喘患者中,评估了特布他林和气雾吸入形式给予的一种新型β受体激动剂KWD 2131的等效支气管扩张剂量,KWD 2131具有相对较强的抗过敏作用(抑制介质释放),其支气管扩张作用相对较弱。还评估了KWD 2131的阈下支气管扩张剂量。该研究是对KWD 2131(0.5毫克至12毫克)和特布他林(0.05毫克至1.2毫克)的累积剂量进行的为期2天的单盲交叉比较。两种药物通过肺活量测定法测量均产生剂量依赖性支气管扩张作用。特布他林在0.05毫克剂量时已具有统计学意义,但KWD 2131直到累积1.5毫克剂量(0.5 + 1毫克)时才有统计学意义。特布他林相对于KWD 2131的支气管扩张效力的中值为30。两种物质对震颤和心血管系统的影响最小,在临床上无重要意义。寻找KWD 2131的阈下支气管扩张剂量很有意义,因为该剂量将用于随后的抗原激发研究,以便选择性地评估KWD 2131的抗过敏特性。KWD 2131的平均阈下支气管扩张剂量为1毫克。然而,8名患者中有4名在1毫克剂量时出现支气管扩张,这4名患者中的2名在0.5毫克剂量时也出现支气管扩张。