Doggrell S A, Brown L
Cardiovascular Pharmacology, Faculty of Medicine and Health Sciences, The University of Auckland, Private Bag 92019, Auckland, New Zealand.
Expert Opin Investig Drugs. 2000 Jul;9(7):1625-34. doi: 10.1517/13543784.9.7.1625.
D-Sotalol is the dextro-rotatory isomer of sotalol and a class III anti-arrhythmic. D-Sotalol prolongs cardiac repolarisation by inhibiting the fast component of the delayed outward rectifying potassium channel. In animal studies, D-sotalol has been shown to be more effective in prolonging atrial, rather than ventricular, action potentials, suggesting that D-sotalol may be more effective against supra-ventricular than ventricular arrhythmias. Furthermore, in animal studies, D-sotalol induces after-depolarisations, which are predictors of pro-arrhythmic activity. D-Sotalol shows little or no reverse use dependence in animal and humans and has slow offset kinetics. This suggests that, in addition to being a preventative treatment for arrhythmias, D-sotalol may be effective at the start or during arrhythmia. As D-sotalol does not block the slow component of the delayed outward rectifying potassium channel, which is activated by the sympathetic nervous system, D-sotalol will not protect against sympathetic hyperactivity. D-Sotalol also has no effect on the K(ATP) channel, which is activated in ischaemia to shorten the action potential. Thus D-sotalol is less effective in ischaemia. Anti-arrhythmic activity with D-sotalol has been demonstrated in dog models of ventricular tachycardia and sudden death. Arrhythmias with D-sotalol have been demonstrated in an ischaemic guinea-pig ventricle model in the absence of action potentials. D-Sotalol is a weak beta-adrenoceptor antagonist and may also be a positive inotrope. In humans, D-sotalol has 100% systemic oral bioavailability, a terminal half-life of 7.2 h and is mainly excreted unchanged in the urine. Preliminary, mainly hospital-based, clinical trials showed that D-sotalol was effective in a variety of supraventricular and ventricular arrhythmias. However, a large clinical trial of D-sotalol as a preventative treatment for arrhythmias and sudden death after myocardial infarction, the SWORD trial, was terminated early because of increased mortality with D-sotalol. The group at greatest risk was those with a remote myocardial infarction and relatively good left ventricular function, the group that showed the lowest mortality when untreated. It is assumed that excessive prolongation of the action potential leading to pro-arrhythmia with D-sotalol, underlies the increased risk of death. However, there is little objective evidence in the SWORD trial to support this. Obviously D-sotalol should not be used in humans with a remote myocardial infarction and relatively good left ventricular function. D-Sotalol could still be considered for short-term hospital use in resistant arrhythmias and for longer-term use to prevent atrial fibrillation in those with remote myocardial infarction and poor left ventricular function.
D - 索他洛尔是索他洛尔的右旋异构体,属于Ⅲ类抗心律失常药物。D - 索他洛尔通过抑制延迟外向整流钾通道的快速成分来延长心脏复极化。在动物研究中,D - 索他洛尔在延长心房动作电位方面比延长心室动作电位更有效,这表明D - 索他洛尔对阵发性室上性心律失常可能比对室性心律失常更有效。此外,在动物研究中,D - 索他洛尔可诱发后去极化,而后去极化是促心律失常活性的预测指标。D - 索他洛尔在动物和人类中几乎没有或没有反向使用依赖性,且具有缓慢的消除动力学。这表明,除了作为心律失常的预防性治疗药物外,D - 索他洛尔在心律失常发作开始时或发作期间可能也有效。由于D - 索他洛尔不阻断由交感神经系统激活的延迟外向整流钾通道的慢速成分,因此它不能预防交感神经过度兴奋。D - 索他洛尔对在缺血时被激活以缩短动作电位的K(ATP)通道也没有作用。因此,D - 索他洛尔在缺血情况下效果较差。在室性心动过速和猝死的犬模型中已证实D - 索他洛尔具有抗心律失常活性。在无动作电位的缺血豚鼠心室模型中也已证实D - 索他洛尔可诱发心律失常。D - 索他洛尔是一种弱β - 肾上腺素能受体拮抗剂,也可能是一种正性肌力药。在人类中,D - 索他洛尔的口服全身生物利用度为100%,终末半衰期为7.2小时,主要以原形经尿液排泄。初步的、主要基于医院的临床试验表明,D - 索他洛尔对多种室上性和室性心律失常有效。然而,一项关于D - 索他洛尔作为心肌梗死后心律失常和猝死预防性治疗药物的大型临床试验——SWORD试验,由于使用D - 索他洛尔导致死亡率增加而提前终止。风险最高的人群是有陈旧性心肌梗死且左心室功能相对较好的患者,而这组患者在未治疗时死亡率最低。据推测,D - 索他洛尔导致动作电位过度延长从而引发促心律失常作用,是死亡风险增加的原因。然而,在SWORD试验中几乎没有客观证据支持这一点。显然,D - 索他洛尔不应在有陈旧性心肌梗死且左心室功能相对较好的患者中使用。对于难治性心律失常的短期住院治疗以及对于有陈旧性心肌梗死且左心室功能较差的患者预防心房颤动的长期使用,D - 索他洛尔仍可考虑。