Anderson Joe R, Nawarskas James J
University of New Mexico College of Pharmacy, Albuquerque, NM 87131-0001, USA.
Cardiol Rev. 2005 Jul-Aug;13(4):202-10. doi: 10.1097/01.crd.0000161979.62749.e7.
Ranolazine is a novel new antianginal agent currently under investigation as monotherapy and adjunct therapy for the treatment of chronic stable angina. While the mechanism of action of ranolazine is not completely understood, it is believed to involve a reduction in fatty acid oxidation, ultimately leading to a shift in myocardial energy production from fatty acid oxidation to glucose oxidation. Since the oxidation of glucose requires less oxygen than the oxidation of fatty acids, ranolazine can help maintain myocardial function in times of ischemia. In addition, ranolazine has minimal effect on blood pressure and heart rate. Ranolazine, by inhibiting cellular ionic channels, prolongs the corrected QT interval. However, ranolazine has not yet been associated with any incidences of ventricular arrhythmia. The clinical data with ranolazine focuses on its use in chronic stable angina, where it has been shown to increase exercise tolerance and decrease angina compared with placebo, as well as in combination with beta-blockers and calcium channel blockers. The use of ranolazine for other cardiac conditions and the effect of ranolazine on morbidity and mortality remains to be determined. Ongoing clinical trials will help further establish the role of ranolazine in the treatment of cardiovascular disorders.
雷诺嗪是一种新型抗心绞痛药物,目前正在作为单一疗法和辅助疗法用于治疗慢性稳定性心绞痛进行研究。虽然雷诺嗪的作用机制尚未完全明确,但据信它涉及减少脂肪酸氧化,最终导致心肌能量产生从脂肪酸氧化转向葡萄糖氧化。由于葡萄糖氧化比脂肪酸氧化需要的氧气更少,雷诺嗪可在缺血时帮助维持心肌功能。此外,雷诺嗪对血压和心率的影响极小。雷诺嗪通过抑制细胞离子通道,延长校正QT间期。然而,雷诺嗪尚未与任何室性心律失常的发生相关联。雷诺嗪的临床数据主要集中在其用于慢性稳定性心绞痛的情况,在这种情况下,与安慰剂相比,它已被证明可提高运动耐量并减少心绞痛发作,以及与β受体阻滞剂和钙通道阻滞剂联合使用时的情况。雷诺嗪用于其他心脏疾病的情况以及它对发病率和死亡率的影响仍有待确定。正在进行的临床试验将有助于进一步明确雷诺嗪在治疗心血管疾病中的作用。