Sheppard D, DiStefano S, Byrd R C, Eschenbacher W L, Bell V, Steck J, Laddu A
J Clin Pharmacol. 1986 Mar;26(3):169-74. doi: 10.1002/j.1552-4604.1986.tb02929.x.
In a double-blind, randomized, crossover study in ten patients with asthma, the effects on specific airway resistance of esmolol, a new ultra-short-acting beta 1-selective adrenoceptor blocker, were compared with those of placebo. Specific airway resistance was measured during increasing doses of esmolol infusion, during dry air provocation tests, and following isoproterenol inhalation. These same studies were later carried out on six of ten patients following intravenous propranolol infusion. All patients were able to tolerate the maximum dose of esmolol (300 micrograms/kg/min); treatment differences between esmolol and placebo were not found. In contrast, intravenous propranolol produced marked symptomatic bronchoconstriction after the lowest dose (1 mg) in two of six patients. Esmolol produced slight but statistically significant enhancement of patients' sensitivity to dry air provocation. Similarly, a slight but significant inhibition of bronchomotor sensitivity to isoproterenol was noted during esmolol infusion. After infusion of 5 mg of intravenous propranolol, one of four patients had a clinically significant increase in sensitivity to dry air. It is concluded that esmolol, because of its short duration of action and relative lack of effect on airway resistance, may be preferred over propranolol in patients with asthma who require treatment with an intravenous beta-blocking agent.
在一项针对10名哮喘患者的双盲、随机、交叉研究中,将新型超短效β1选择性肾上腺素能受体阻滞剂艾司洛尔对特定气道阻力的影响与安慰剂进行了比较。在递增剂量的艾司洛尔输注期间、干燥空气激发试验期间以及异丙肾上腺素吸入后,测量特定气道阻力。在10名患者中的6名患者静脉输注普萘洛尔后,随后进行了相同的研究。所有患者均能耐受艾司洛尔的最大剂量(300微克/千克/分钟);未发现艾司洛尔与安慰剂之间的治疗差异。相比之下,在6名患者中的2名患者中,静脉注射普萘洛尔在最低剂量(1毫克)后出现了明显的症状性支气管收缩。艾司洛尔使患者对干燥空气激发的敏感性略有但具有统计学意义的增强。同样,在艾司洛尔输注期间,观察到对异丙肾上腺素的支气管运动敏感性有轻微但显著的抑制。在静脉注射5毫克普萘洛尔后,4名患者中的1名对干燥空气的敏感性出现了临床上显著的增加。得出的结论是,由于艾司洛尔作用持续时间短且对气道阻力相对无影响,在需要静脉注射β受体阻滞剂治疗的哮喘患者中,艾司洛尔可能比普萘洛尔更受青睐。