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雷诺嗪:其在慢性稳定型心绞痛中应用的综述

Ranolazine: a review of its use in chronic stable angina pectoris.

作者信息

Keating Gillian M

机构信息

Wolters Kluwer Health | Adis, Auckland, New Zealand.

出版信息

Drugs. 2008;68(17):2483-503. doi: 10.2165/0003495-200868170-00006.

DOI:10.2165/0003495-200868170-00006
PMID:19016575
Abstract

Extended-release ranolazine (ranolazine ER) [Ranexa] is a piperazine derivative with a novel mechanism of action that was recently approved in the EU for use as add-on therapy in patients with stable angina pectoris. Ranolazine ER achieves its antianginal effect without affecting heart rate or blood pressure (BP) to a clinically significant extent. Results of well designed, placebo-controlled, short-term studies demonstrate that add-on therapy with ranolazine ER in patients with chronic stable angina improves exercise performance, and reduces anginal frequency and nitroglycerin use. Although longer-term therapy with ranolazine ER did not reduce the incidence of major cardiovascular events in patients with non-ST-elevation acute coronary syndromes, it did reduce the incidence of recurrent ischaemia. Ranolazine ER is a generally well tolerated antianginal agent. Although it is associated with modest dose-related increases in the corrected QT (QTc) interval, ranolazine ER does not appear to be associated with an excess of arrhythmias. Thus, ranolazine ER is a useful new option for patients with chronic stable angina whose symptoms are not controlled with first-line antianginal therapy or who do not tolerate first-line antianginal agents.

摘要

缓释雷诺嗪(雷诺嗪缓释剂)[Ranexa]是一种哌嗪衍生物,具有新颖的作用机制,最近在欧盟被批准用作稳定型心绞痛患者的附加治疗药物。雷诺嗪缓释剂在临床上未对心率或血压产生显著影响的情况下发挥其抗心绞痛作用。精心设计的、安慰剂对照的短期研究结果表明,在慢性稳定型心绞痛患者中,使用雷诺嗪缓释剂进行附加治疗可改善运动能力,减少心绞痛发作频率并减少硝酸甘油的使用。尽管在非ST段抬高型急性冠状动脉综合征患者中,雷诺嗪缓释剂的长期治疗并未降低主要心血管事件的发生率,但它确实降低了复发性缺血的发生率。雷诺嗪缓释剂是一种耐受性普遍良好的抗心绞痛药物。尽管它与校正QT(QTc)间期适度的剂量相关增加有关,但雷诺嗪缓释剂似乎与心律失常的增加无关。因此,对于症状未被一线抗心绞痛治疗控制或不耐受一线抗心绞痛药物的慢性稳定型心绞痛患者,雷诺嗪缓释剂是一种有用的新选择。

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Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial.雷诺嗪联合阿替洛尔、氨氯地平或地尔硫䓬对严重慢性心绞痛患者运动耐量和心绞痛发作频率的影响:一项随机对照试验。
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Effects of ranolazine on recurrent cardiovascular events in patients with non-ST-elevation acute coronary syndromes: the MERLIN-TIMI 36 randomized trial.雷诺嗪对非ST段抬高型急性冠状动脉综合征患者心血管事件复发的影响:MERLIN-TIMI 36随机试验
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Ranolazine for the management of coronary artery disease.雷诺嗪用于冠状动脉疾病的管理。
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Efficacy of ranolazine in patients with chronic angina observations from the randomized, double-blind, placebo-controlled MERLIN-TIMI (Metabolic Efficiency With Ranolazine for Less Ischemia in Non-ST-Segment Elevation Acute Coronary Syndromes) 36 Trial.雷诺嗪对慢性心绞痛患者的疗效——来自随机、双盲、安慰剂对照的MERLIN-TIMI 36试验(非ST段抬高型急性冠状动脉综合征中使用雷诺嗪提高代谢效率以减少缺血)的观察结果
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Ranolazine for stable angina pectoris.雷诺嗪用于稳定型心绞痛。
Cochrane Database Syst Rev. 2017 Feb 8;2(2):CD011747. doi: 10.1002/14651858.CD011747.pub2.
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Ranolazine: a review of its use as add-on therapy in patients with chronic stable angina pectoris.雷诺嗪:用于慢性稳定性心绞痛患者附加治疗的综述。

本文引用的文献

1
Efficacy of ranolazine in patients with chronic angina observations from the randomized, double-blind, placebo-controlled MERLIN-TIMI (Metabolic Efficiency With Ranolazine for Less Ischemia in Non-ST-Segment Elevation Acute Coronary Syndromes) 36 Trial.雷诺嗪对慢性心绞痛患者的疗效——来自随机、双盲、安慰剂对照的MERLIN-TIMI 36试验(非ST段抬高型急性冠状动脉综合征中使用雷诺嗪提高代谢效率以减少缺血)的观察结果
J Am Coll Cardiol. 2009 Apr 28;53(17):1510-6. doi: 10.1016/j.jacc.2009.01.037.
2
Ranolazine shortens repolarization in patients with sustained inward sodium current due to type-3 long-QT syndrome.由于3型长QT综合征导致持续内向钠电流,雷诺嗪可缩短患者的复极化时间。
J Cardiovasc Electrophysiol. 2008 Dec;19(12):1289-93. doi: 10.1111/j.1540-8167.2008.01246.x. Epub 2008 Jul 25.
3
Drugs. 2013 Jan;73(1):55-73. doi: 10.1007/s40265-012-0005-z.
Rapid kinetic interactions of ranolazine with HERG K+ current.雷诺嗪与HERG钾电流的快速动力学相互作用。
J Cardiovasc Pharmacol. 2008 Jun;51(6):581-9. doi: 10.1097/FJC.0b013e3181799690.
4
Effect of ranolazine on ventricular vulnerability and defibrillation threshold in the intact porcine heart.
J Cardiovasc Electrophysiol. 2008 Oct;19(10):1073-9. doi: 10.1111/j.1540-8167.2008.01204.x. Epub 2008 May 9.
5
Late sodium current inhibition as a new cardioprotective approach.晚钠电流抑制作为一种新的心脏保护方法。
J Mol Cell Cardiol. 2008 Jun;44(6):954-967. doi: 10.1016/j.yjmcc.2008.03.019. Epub 2008 Apr 8.
6
Ranolazine improves diastolic dysfunction in isolated myocardium from failing human hearts--role of late sodium current and intracellular ion accumulation.雷诺嗪可改善衰竭人类心脏离体心肌的舒张功能障碍——晚钠电流和细胞内离子蓄积的作用
J Mol Cell Cardiol. 2008 Jul;45(1):32-43. doi: 10.1016/j.yjmcc.2008.03.006. Epub 2008 Mar 14.
7
Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits.
J Pharmacol Exp Ther. 2008 Jun;325(3):875-81. doi: 10.1124/jpet.108.137729. Epub 2008 Mar 5.
8
Metabolic efficiency with ranolazine for less ischemia in non-ST elevation acute coronary syndromes (MERLIN TIMI-36) study.雷诺嗪提高非ST段抬高型急性冠脉综合征患者代谢效率以减少心肌缺血(MERLIN TIMI-36)研究
Expert Rev Cardiovasc Ther. 2008 Jan;6(1):9-16. doi: 10.1586/14779072.6.1.9.
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Br J Pharmacol. 2008 Mar;153(6):1133-42. doi: 10.1038/sj.bjp.0707492. Epub 2007 Dec 10.
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Br J Pharmacol. 2008 Mar;153(6):1128-32. doi: 10.1038/sj.bjp.0707522. Epub 2007 Dec 10.