Petraglia A, Gurrieri G, Scarpitta M, Pisati R, Ansalone D
Service of Respiratory Physiopathology and Intensive Therapy of Respiratory Failure, Giovanni da Procida Hospital, Salerno, Italy.
Int J Clin Pharmacol Ther Toxicol. 1992 Oct;30(10):365-70.
To investigate the beta 2-receptor selectivity of a new beta 2-adrenoceptor agonist, broxaterol, we compared the respiratory and cardiovascular effects of this compound with those of terbutaline and placebo. Twelve asthmatic patients were evaluated in a randomized, single blind, crossover study. A single dose of each study treatment (broxaterol 400 micrograms and terbutaline 500 micrograms was administered with metered dose inhalers. Measurements of lung function (vital capacity, forced expiratory volume in one second, airway resistance and specific airway conductance), heart rate and systolic/diastolic blood pressure were performed before and at 15, 30, 60, 120, 240 and 360 min after each study treatment. No significant difference was observed between broxaterol and terbutaline in VC, FEV1 and Raw changes, although a greater and significant increase in sGaw was found only with broxaterol. Significant increases in heart rate and systolic blood pressure were observed only with terbutaline. The results of this study suggest that broxaterol can promote a greater bronchodilator effect with less cardiovascular side effects than terbutaline, probably through a greater beta 2-receptor selectivity.
为研究新型β2肾上腺素能受体激动剂溴沙特罗的β2受体选择性，我们将该化合物与特布他林及安慰剂的呼吸和心血管效应进行了比较。在一项随机、单盲、交叉研究中对12例哮喘患者进行了评估。每项研究治疗均采用定量吸入器给予单剂量药物（溴沙特罗400微克和特布他林500微克）。在每项研究治疗前及治疗后15、30、60、120、240和360分钟测量肺功能（肺活量、一秒用力呼气量、气道阻力和比气道传导率）、心率及收缩压/舒张压。溴沙特罗和特布他林在肺活量、一秒用力呼气量及气道阻力变化方面未观察到显著差异，不过仅溴沙特罗使比气道传导率有更大且显著的增加。仅特布他林使心率和收缩压显著升高。本研究结果提示，溴沙特罗可能通过更高的β2受体选择性，比特布他林能产生更强的支气管扩张作用且心血管副作用更少。
