Ranolazine: effects on ischemic heart.

Andrea Rognoni, Lucia Barbieri, Chiara Cavallino, Sara Bacchini, Alessia Veia, Anna Degiovanni, Francesco Rametta, Federico Nardi, Maurizio Lazzero, Alessandro Lupi, Angelo S Bongo
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引用次数: 1

Abstract

Coronary artery disease is the major cause of mortality and morbidity in the industrialized countries; in the United States of America and in Europe, it is responsible for one of every six deaths per year. In the setting of ischemic heart disease, angina pectoris and chest pain, in particular, are the major causes of emergency department accesses. Angina pectoris is a clinical syndrome characterized by discomfort typically in the chest, neck, chin and left arm induced by physical exertion, emotional stress and cold and is relieved by rest or by taking of nitrates. The main targets of treatment of angina pectoris are to improve quality of life by reducing the frequency and the severity of symptoms, to increase functional capacity and to improve prognosis. Ranolazine is a recent antianginal drug with unique methods of action. It was approved by the US Food and Drug Administration in 2006 as add-on therapy in patients symptomatic for stable angina. With the inhibition of the late sodium current, Ranolazine protects against ion deregulation, prevents cellular calcium overload and the subsequent increase in diastolic tension without impacting heart rate and blood pressure. Short term clinical trials and patent research show that add on therapy with Ranolazine in patients with chronic stable angina significantly improves exercise duration, exercise time to angina and reduces the use of nitro glycerine. Long term clinical trials showed no significant differences in the rate of cardiovascular death and myocardial infarction in patients with non-ST segment elevation acute coronary syndromes but a reduction in terms of recurrent ischemia. Ranolazine is generally well tolerated and even if it increases the duration of QTc interval it is not associated with atrial and ventricular arrhythmias. Therefore Ranolazine represents a good therapeutic approach in patients with chronic stable angina still symptomatic, while on optimal anti-ischemic therapy, or intolerant to traditional anti-ischemic drugs.

雷诺嗪对缺血性心脏的作用。
冠状动脉疾病是工业化国家死亡率和发病率的主要原因;在美利坚合众国和欧洲,每年每六人死亡中就有一人死于疟疾。在缺血性心脏病的情况下,心绞痛和胸痛是进入急诊室的主要原因。心绞痛是一种临床综合征,主要表现为由体力消耗、情绪紧张和寒冷引起的胸部、颈部、下巴和左臂不适,可通过休息或服用硝酸盐缓解。治疗心绞痛的主要目标是通过减少症状的发生频率和严重程度来改善生活质量,增加功能能力和改善预后。雷诺嗪是一种最新的抗心绞痛药物,具有独特的作用方法。2006年,它被美国食品和药物管理局批准作为稳定型心绞痛患者的附加疗法。通过抑制晚期钠电流,雷诺嗪可以防止离子解除管制,防止细胞钙超载和随后的舒张张力增加,而不影响心率和血压。短期临床试验和专利研究表明,慢性稳定型心绞痛患者加用雷诺嗪治疗可显著提高运动时间、运动时间,减少硝基甘油的使用。长期临床试验显示,非st段抬高急性冠状动脉综合征患者的心血管死亡和心肌梗死发生率无显著差异,但复发性缺血发生率有所降低。雷诺嗪通常耐受性良好,即使它增加QTc间期的持续时间,也与心房和室性心律失常无关。因此,雷诺嗪对于仍有症状的慢性稳定型心绞痛患者是一种很好的治疗方法,而抗缺血治疗是最佳的,或者对传统的抗缺血药物不耐受。
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