Strubelt O
Arzneimittelforschung. 1984;34(10):1265-70.
In rats, the intravenous infusion with acebutolol lead to a dose dependent decrease of arterial blood pressure, heart rate, cardiac output and total peripheral resistance, to sinus bradycardia, widening of the QRS complex, 1st and 2nd degree AV-block and intraventricular conductance disturbances. Nine possible antidotes were administered i.v. to rats which had been infused with 2 mg/kg X min acebutolol for 60 min. Isoprenaline proved the best antidote against acebutolol antagonizing the bradycardia by 88% and the hypotension completely. The activities of orciprenaline and prenalterol were lower than those of isoprenaline. Dopamine, epinephrine and norepinephrine antagonized acebutolol-induced hypotension, but did not influence considerably the bradycardia. Glucagon, on the other hand, antagonized the acebutolol-induced bradycardia by 47% but exerted only a small activity on the hypotension. Aminophyllin and calcium were nearly ineffective as antidotes against acebutolol. Isoprenaline and dopamine infused simultaneously restored heart rate, arterial blood pressure and cardiac output of acebutol-poisoned rats. The survival time of rats infused with 4 mg/kg X min acebutolol was doubled by the additional infusion of 0.2 mg/kg X min isoprenaline. The antagonistic activity of a treatment with isoprenaline and dopamine against the cardiovascular toxicity of acebutolol was confirmed in rabbits.
在大鼠中，静脉输注醋丁洛尔会导致动脉血压、心率、心输出量和总外周阻力呈剂量依赖性下降，出现窦性心动过缓、QRS波群增宽、一度和二度房室传导阻滞以及室内传导障碍。对已静脉输注2毫克/千克×分钟醋丁洛尔60分钟的大鼠静脉注射9种可能的解毒剂。结果证明，异丙肾上腺素是对抗醋丁洛尔的最佳解毒剂，可使心动过缓拮抗88%，并完全对抗低血压。奥西那林和普瑞特罗的活性低于异丙肾上腺素。多巴胺、肾上腺素和去甲肾上腺素可对抗醋丁洛尔引起的低血压，但对心动过缓影响不大。另一方面，胰高血糖素可使醋丁洛尔引起的心动过缓拮抗47%，但对低血压仅发挥微弱作用。氨茶碱和钙作为对抗醋丁洛尔的解毒剂几乎无效。同时输注异丙肾上腺素和多巴胺可恢复醋丁洛尔中毒大鼠的心率、动脉血压和心输出量。额外输注0.2毫克/千克×分钟异丙肾上腺素可使输注4毫克/千克×分钟醋丁洛尔的大鼠存活时间加倍。异丙肾上腺素和多巴胺联合治疗对醋丁洛尔心血管毒性的拮抗作用在兔中得到证实。
