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Carvedilols antiarrhythmic properties: Therapeutic implications in patients with left ventricular dysfunction

机译:卡维地洛的抗心律不齐特性:对左心功能不全患者的治疗意义

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摘要

Carvedilol is a beta‐and alpha‐adrenergic‐blocking drug with clinically important antiarrhythmic properties. It possesses anti‐ischemic and antioxidant activity and inhibits a number of cationic channels in the cardiomyocyte, including the HERG‐associated potassium channel, the L‐type calcium channel, and the rapid‐depolarizing sodium channel. The electrophysiologic properties of carvedilol include moderate prolongation of action potential duration and effective refractory period; slowing of atrioventricular conduction; and reducing the dispersion of refractoriness. Experimentally, carvedilol reduces complex and repetitive ventricular ectopy induced by ischemia and reperfusion.In patients, carvedilol is effective in controlling the ventricular rate response in atrial fibrillation (AF), with and without digitalis, and is useful in maintaining sinus rhythm after cardioversion, with and without amiodarone. In patients with AF and heart failure (HF), carvedilol reduces mortality risk and improves left ventricular (LV) function. Large‐scale clinical trials have demonstrated that combined carvedilol and angiotensin‐converting enzyme inhibitor therapy significantly reduces sudden cardiac death, mortality, and ventricular arrhythmia in patients with LV dysfunction (LVD) due to chronic HF or following myocardial infarction (MI).Despite intensive neurohormonal blockade, mortality rates remain relatively high in patients with post‐MI and nonischemic LVD. Recent trials of implantable cardioverter‐defibrillators added to pharmacologic therapy, especially beta blockers, have shown a further reduction in arrhythmic deaths in these patients.
机译:卡维地洛是具有临床重要抗心律不齐特性的β和α肾上腺素能阻滞药物。它具有抗缺血和抗氧化的功能,并抑制心肌细胞中的许多阳离子通道,包括与HERG相关的钾通道,L型钙通道和快速去极化钠通道。卡维地洛的电生理特性包括动作电位持续时间和有效不应期的适度延长。减慢房室传导;并减少耐火材料的分散。在实验上,卡维地洛可减轻由缺血和再灌注引起的复杂且反复的心室异位症。在患者中,卡维地洛可有效控制房颤(AF)伴或不伴洋地黄的心室率反应,并有助于维持心脏复律后的窦性心律而且没有胺碘酮。对于患有房颤和心力衰竭(HF)的患者,卡维地洛可降低死亡风险并改善左心室(LV)功能。大规模的临床试验表明,卡维地洛和血管紧张素转换酶抑制剂联合治疗可显着降低因慢性HF或心肌梗死(LV)导致的LV功能不全(LVD)患者的猝死,死亡率和室性心律失常。神经激素阻滞,心梗后和非缺血性LVD患者的死亡率仍然相对较高。最近在药物治疗中增加了植入式心脏复律除颤器(尤其是β受体阻滞剂)的试验表明,这些患者的心律失常死亡进一步减少。

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