Tantucci C, Burni B, Dottorini M L, Malerba M, Peccini F, Gurrieri G, Sorbini C A, Grassi V
Department of Internal Medicine, University of Ancona, Italy.
Int J Clin Pharmacol Res. 1990;10(3):183-9.
The ventilatory and gas-exchange effects of broxaterol, a new selective beta 2-adrenoceptor agonist, were investigated in ten asthmatics following intravenous administration of a single dose of 200 mcg. Broxaterol elicited a prompt and marked bronchodilating effect (increase in forced expiratory volume in one second and specific conductance), maintained at least up to the sixtieth minute. Minute ventilation and the mean expiratory flow did not increase significantly, the pattern of breathing showing a reduction of expiratory time, without modification of inspiratory time. On the other hand, occlusion pressure did not show any significant rise at all times of observation. Furthermore, the partial arterial oxygen and carbon dioxide pressures and alveolar-arterial difference in oxygen and physiological dead space remained unchanged, when measured at 20 min. The results demonstrated that broxaterol was an effective bronchodilating agent, also when rapidly injected, causing a prompt relief of bronchospasm. With respect to other beta 2-adrenoceptor agonists, this compound did not appear to increase minute ventilation or to induce an impairment of ventilation/perfusion ratio, at least after 20 min, when the bronchodilation was still evident. Finally, no side-effects or alterations of heart rate or blood pressure were reported.
在10名哮喘患者静脉注射单剂量200微克新型选择性β2肾上腺素能受体激动剂溴沙特罗后,研究了其通气和气体交换作用。溴沙特罗引发了迅速且显著的支气管扩张效应(一秒用力呼气量和比传导率增加),至少持续到第60分钟。分钟通气量和平均呼气流量未显著增加,呼吸模式显示呼气时间缩短,吸气时间未改变。另一方面,在所有观察时间点,阻断压均未出现任何显著升高。此外,在20分钟测量时,动脉血氧分压和二氧化碳分压以及肺泡-动脉氧分压差和生理死腔均保持不变。结果表明,溴沙特罗是一种有效的支气管扩张剂,即使快速注射也能迅速缓解支气管痉挛。与其他β2肾上腺素能受体激动剂相比,该化合物似乎不会增加分钟通气量或导致通气/灌注比值受损,至少在20分钟后,此时支气管扩张仍很明显。最后,未报告有副作用或心率及血压改变。