Cardiovascular Research Institute Maastricht, Department of Cardiothoracic Surgery, Maastricht, The Netherlands.
Int J Cardiol. 2011 Jun 16;149(3):341-6. doi: 10.1016/j.ijcard.2010.02.014. Epub 2010 Mar 4.
Amiodarone is currently the most effective antiarrhythmic drug for sinus rhythm maintenance. However, due to serious extracardiac adverse effects, prophylactic amiodarone therapy is only appropriate for patients at high risk for postoperative atrial fibrillation (AF). We hypothesized that epicardial application of an amiodarone-releasing hydrogel would produce therapeutic myocardial drug concentrations, while systemic levels would remain low.
Goats were fitted with right atrial epicardial patch electrodes. A poly(ethylene glycol)-based hydrogel with amiodarone (1mg/kg bw) (n=10) or without drug (n=6) was applied to the right atrial epicardium. Atrial effective refractory period (AERP), conduction time and atrial response to burst pacing (rapid atrial response, RAR) were assessed up to 28days in awake goats. Myocardial, plasma and extracardiac tissue amiodarone concentrations were analysed by high-performance liquid chromatography.
The amiodarone-loaded hydrogel produced therapeutic drug concentrations in the right atrium up to 21days after application. In this period, AERP and conduction time were prolonged, while RAR inducibility was reduced (P<0.05) compared to animals treated with drug-free hydrogel. Mean amiodarone concentrations in the right atrium were 1 order of magnitude higher than in other heart chambers and 2 orders of magnitude higher than in extracardiac tissues. Plasma amiodarone levels remained below the detection limit (<10ng/mL) during the 28-day follow-up.
Epicardial application of an amiodarone-releasing hydrogel reduces atrial vulnerability to tachyarrhythmias up to 3weeks, while extracardiac drug levels remain low. Therefore, amiodarone-releasing hydrogel could be applied during cardiac surgery to prevent postoperative AF at minimal risk for extracardiac adverse side effects.
胺碘酮目前是维持窦性心律最有效的抗心律失常药物。然而,由于严重的心脏外不良反应,预防性胺碘酮治疗仅适用于术后心房颤动(AF)高危患者。我们假设在心外膜应用胺碘酮释放水凝胶将产生治疗性心肌药物浓度,而全身水平仍保持较低。
给山羊配备右心房心外膜贴片电极。将含有胺碘酮(1mg/kg bw)的聚乙二醇基水凝胶(n=10)或不含药物的水凝胶(n=6)应用于心外膜。在清醒的山羊中,评估心房有效不应期(AERP)、传导时间和心房对burst pacing 的反应(快速心房反应,RAR),直至 28 天。通过高效液相色谱法分析心肌、血浆和心外膜组织中的胺碘酮浓度。
胺碘酮负载的水凝胶在应用后 21 天内产生了右心房的治疗药物浓度。在此期间,与用不含药物的水凝胶治疗的动物相比,AERP 和传导时间延长,而 RAR 的诱导性降低(P<0.05)。右心房的平均胺碘酮浓度比其他心腔高 1 个数量级,比心外膜组织高 2 个数量级。在 28 天的随访期间,血浆胺碘酮水平仍低于检测限(<10ng/mL)。
在心外膜应用胺碘酮释放水凝胶可降低心房对心动过速的易感性长达 3 周,同时保持低的心外膜药物水平。因此,胺碘酮释放水凝胶可在心外科手术期间应用,以预防术后 AF,同时最大限度地降低心脏外不良反应的风险。