Nicorandil - An updated review of its use in ischaemic heart disease with emphasis on its cardioprotective effects
Nicorandil - An updated review of its use in ischaemic heart disease with emphasis on its cardioprotective effects
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DOI：
10.2165/00003495-200060040-00007
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发表时间：
2000-10-01
期刊：
影响因子：
11.5
通讯作者：
Goa, KL
中科院分区：
文献类型：
--
作者：
Markham, A;Plosker, GL;Goa, KL
尼可地尔是一种兼具硝酸盐样和 ATP 敏感性钾通道 (K(+)ATP) 激活特性的药物。凭借这种双重作用机制，该药物起到平衡冠状动脉和外周血管扩张剂的作用，并降低前负荷和后负荷，K(+)ATP通道已被证明参与心肌预适应现象，缺血再灌注引起的心肌顿抑或梗塞动物模型研究表明尼可地尔具有心脏保护作用。 影响。对接受经皮腔内冠状动脉成形术 (PTCA) 的患者进行的研究表明，尼可地尔可降低缺血期间 ST 段抬高的程度。在早期非比较性试验中，尼可地尔显着改善了稳定性劳力性心绞痛患者的运动耐量测试结果（与基线相比）。在早期随机、双盲、安慰剂对照试验中，相对于安慰剂，该药物还改善了运动耐量测试的结果。在心绞痛患者的随机、双盲比较研究中，通过运动耐量测试测量，尼可地尔表现出与二硝酸异山梨酯和单硝酸异山梨酯、美托洛尔、普萘洛尔、阿替洛尔、地尔硫卓、 氨氯地平和硝苯地平，尼可地尔对急性心肌梗塞引起的缺血性损伤心肌恢复的各个方面的影响已在短期内进行了研究。与对照组相比，尼可地尔接受者的局部左心室 (LV) 室壁运动（心肌功能的标志）显着改善。尼可地尔治疗心绞痛的主要不良事件是头痛。对于容易头痛的患者，可以通过低剂量开始使用尼可地尔来最大程度地减少这种情况。接受尼可地尔治疗的患者出现口腔溃疡的病例报告并不常见；因果关系尚未最终确定，但产品处方信息表明，如果发生持续性口疮或严重口腔溃疡，应考虑替代治疗。因此，尼可地尔仍然是心绞痛患者的有用背景治疗。当高危患者急性心肌梗死后直接用作干预策略的一部分时，该药物还表现出潜在的心脏保护作用。人们满怀兴趣地等待着尼可地尔在后一种适应症中的进一步大规模长期研究。
Nicorandil is a drug with both nitrate-like and ATP-sensitive potassium-channel (K(+)ATP) activating properties. By virtue of this dual mechanism of action, the drug acts as a balanced coronary and peripheral vasodilator and reduces both preload and afterload,The K(+)ATP channel has been shown to be involved in the phenomenon of myocardial preconditioning, and studies in animal models of ischaemia-reperfusion-induced myocardial stunning or infarction indicate that nicorandil has cardioprotective effects. Studies in patients undergoing percutaneous transluminal coronary angioplasty (PTCA) have shown that the administration of nicorandil reduces ST-segment elevation during ischaemia.Nicorandil significantly improved the results of exercise tolerance tests versus baseline in patients with stable effort angina pectoris in early noncomparative trials. The drug also improved the results of exercise tolerance tests relative to placebo in early randomised, double-blind, placebo-controlled trials.In randomised, double-blind comparative studies in patients with angina pectoris, nicorandil has demonstrated equivalent efficacy, as measured by exercise tolerance testing, to isosorbide di- and mononitrate, metoprolol, propranolol, atenolol, diltiazem, amlodipine and nifedipine,The effects of nicorandil on various aspects of myocardial recovery from ischaemic damage caused by acute myocardial infarction have been investigated in the short term. Regional left ventricular (LV) wall motion, a marker of myocardial function, was significantly improved in nicorandil recipients relative to control.The main adverse event associated with nicorandil as treatment for angina pectoris is headache. This can be minimised by commencing nicorandil at a low dose in patients prone to headache. There have been infrequent case reports of mouth ulcers in patients receiving nicorandil; causality has not been conclusively established, but product prescribing information indicates that an alternative treatment should be considered if persistent aphthous or severe mouth ulceration occurs.Thus, nicorandil remains a useful background therapy for patients with angina pectoris, The drug has also demonstrated potential cardioprotective effects when used as part of an intervention strategy directly after acute myocardial infarction in high-risk patients. Further large scale longer term studies of nicorandil in this latter indication are awaited with interest.