Basil B, Jordan R, Loveless A H, Maxwell D R
Br J Pharmacol. 1974 Mar;50(3):323-33. doi: 10.1111/j.1476-5381.1974.tb09607.x.
1 The beta-adrenoceptor blocking agent, acebutolol (M & B 17,803), has been compared with propranolol, practolol, lignocaine and quinidine for its ability to revert or prevent various types of experimental arrhythmias.2 By intravenous infusion, acebutolol had one half the potency of propranolol in reverting an established ouabain-induced ventricular arrhythmia in the anaesthetized dog. Practolol was ineffective in the conditions used.3 High oral doses of acebutolol or propranolol significantly increased the arrhythmic dose of ouabain in the conscious rabbit. Similar doses of practolol produced a significant decrease (i.e. potentiation) in the dose of ouabain required to produce arrhythmia. Lignocaine and quinidine showed no or little activity in this test.4 Propranolol, acebutolol and practolol were all effective in decreasing the frequency of ectopic beats induced by adrenaline and methylchloroform in the anaesthetized cat. Lignocaine and quinidine were only weakly effective.5 Acebutolol and propranolol were equally effective either intravenously or orally in reducing the incidence of ventricular fibrillation produced by chloroform in mice.6 It is suggested that the wide spectrum of experimental anti-arrhythmic activity of acebutolol coupled with its cardioselectivity may make it an interesting compound in the treatment of cardiac arrhythmias in man.
已将β-肾上腺素能受体阻滞剂醋丁洛尔(M&B 17,803)与普萘洛尔、普拉洛尔、利多卡因和奎尼丁在恢复或预防各种类型实验性心律失常的能力方面进行了比较。
通过静脉输注,醋丁洛尔在恢复麻醉犬中已建立的哇巴因诱导的室性心律失常方面的效力是普萘洛尔的一半。在所用条件下,普拉洛尔无效。
高口服剂量的醋丁洛尔或普萘洛尔显著增加清醒兔中哇巴因的致心律失常剂量。相似剂量的普拉洛尔使产生心律失常所需的哇巴因剂量显著降低(即增强作用)。利多卡因和奎尼丁在该试验中无活性或活性很小。
普萘洛尔、醋丁洛尔和普拉洛尔在降低麻醉猫中由肾上腺素和氯仿诱导的异位搏动频率方面均有效。利多卡因和奎尼丁仅具有微弱的效果。
醋丁洛尔和普萘洛尔静脉内或口服在降低小鼠中由氯仿产生的心室颤动发生率方面同样有效。
有人提出,醋丁洛尔广泛的实验性抗心律失常活性及其心脏选择性可能使其成为治疗人类心律失常的一种有趣化合物。