Hashimoto K, Tsukada T, Matsuda H, Matsubara I, Imai S
Jpn J Pharmacol. 1978 Aug;28(4):535-44. doi: 10.1254/jjp.28.535.
Antiarrhythmic effects of oxprenolol, a beta-blocker, were studied quantitatively on arhythmias produced by epinephrine during halothane anesthesia and by two-stage coronary ligation, and were compared to those of other beta-blockers, propranolol and Kö 1400, which have been already reported. Though oxprenolol has potent beta-blocking activity, the antiarrhythmic effect on halothane-epinephrine arrhythmia was significantly weaker than those of propranolol and Kö 1400. The effective dose of oxprenolol was 60 +/- 18 microgram/kg (mean +/- S.E., N = 6), which is in the range of the so-called beta-adrenergic blocking dose. The weaker antiarrhythmic effect of oxprenolol as compared to propranolol and Kö 1400 is probably due to the intrinsic positive chronotropic effect, which is most clearly observed in oxprenolol as compared to the other two drugs. As for two-stage coronary ligation arrhythmia, oxprenolol suppressed only that observed 48 hours after coronary ligation using higher doses (5 to 10 mg/kg). Other beta-blockers also showed similar effects. Because of the high doses necessary for the antiarrhythmic effects on the coronary ligation arrhythmia, the mechanism for suppressing the arrhythmia is probably due to the local anesthetic action of the beta-blockers.
研究了β受体阻滞剂氧烯洛尔对氟烷麻醉期间肾上腺素诱发的心律失常以及两阶段冠状动脉结扎诱发的心律失常的抗心律失常作用,并与已报道的其他β受体阻滞剂普萘洛尔和Kö 1400的作用进行了比较。尽管氧烯洛尔具有强大的β受体阻滞活性,但其对氟烷-肾上腺素心律失常的抗心律失常作用明显弱于普萘洛尔和Kö 1400。氧烯洛尔的有效剂量为60±18微克/千克(平均值±标准误,N = 6),处于所谓的β肾上腺素能阻滞剂量范围内。与普萘洛尔和Kö 1400相比,氧烯洛尔的抗心律失常作用较弱可能是由于其内在的正性变时作用,与其他两种药物相比,这种作用在氧烯洛尔中最为明显。至于两阶段冠状动脉结扎心律失常,氧烯洛尔仅在使用较高剂量(5至10毫克/千克)时抑制冠状动脉结扎后观察到的48小时的心律失常。其他β受体阻滞剂也显示出类似的作用。由于对冠状动脉结扎心律失常产生抗心律失常作用所需的剂量较高,抑制心律失常的机制可能是由于β受体阻滞剂的局部麻醉作用。