Safety and Efficacy of Ranolazine for the Treatment of Chronic Angina Pectoris.

Mohammed Aldakkak, David F Stowe, Amadou K S Camara
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Abstract

Coronary heart disease is a global malady and it is the leading cause of death in the United States. Chronic stable angina is the most common manifestation of coronary heart disease and it results from the imbalance between myocardial oxygen supply and demand due to reduction in coronary blood flow. Therefore, in addition to lifestyle changes, commonly used pharmaceutical treatments for angina (nitrates, β-blockers, Ca2+ channel blockers) are aimed at increasing blood flow or decreasing O2 demand. However, patients may continue to experience symptoms of angina. Ranolazine is a relatively new drug with anti-anginal and anti-arrhythmic effects. Its anti-anginal mechanism is not clearly understood but the general consensus is that ranolazine brings about its anti-anginal effects by inhibiting the late Na+ current and the subsequent intracellular Ca2+ accumulation. Recent studies suggest other effects of ranolazine that may explain its anti-anginal and anti-arrhythmic effects. Nonetheless, clinical trials have proven the efficacy of ranolazine in treating chronic angina. It has been shown to be ineffective, however, in treating acute coronary syndrome patients. Ranolazine is a safe drug with minimal side effects. It is metabolized mainly in the liver and cleared by the kidney. Therefore, caution must be taken in patients with impaired hepatic or renal function. Due to its efficacy and safety, ranolazine was approved for the treatment of chronic angina by the Food and Drug Administration (FDA) in 2006.

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雷诺拉嗪治疗慢性心绞痛的安全性和有效性
冠心病是一种全球性疾病,也是美国人的主要死因。慢性稳定型心绞痛是冠心病最常见的表现,它是由于冠状动脉血流量减少导致心肌供氧和需氧失衡造成的。因此,除改变生活方式外,心绞痛的常用药物治疗(硝酸盐、β-受体阻滞剂、Ca2+ 通道阻滞剂)旨在增加血流量或减少氧气需求。然而,患者可能会继续出现心绞痛症状。雷诺拉嗪是一种相对较新的药物,具有抗心绞痛和抗心律失常的作用。其抗心绞痛机制尚不清楚,但普遍认为雷诺拉嗪是通过抑制晚期 Na+ 电流和随后的细胞内 Ca2+ 积累来发挥抗心绞痛作用的。最近的研究表明,雷诺拉嗪的其他作用也可能解释了其抗心绞痛和抗心律失常的作用。尽管如此,临床试验证明了雷诺拉嗪治疗慢性心绞痛的疗效。但在治疗急性冠状动脉综合征患者方面,雷诺拉嗪的疗效不佳。雷诺拉嗪是一种安全的药物,副作用极小。它主要在肝脏代谢,由肾脏清除。因此,肝功能或肾功能受损的患者必须慎用。由于其疗效和安全性,雷诺拉嗪于2006年被美国食品药品管理局(FDA)批准用于治疗慢性心绞痛。
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