Markham A, Plosker G L, Goa K L
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2000 Oct;60(4):955-74. doi: 10.2165/00003495-200060040-00007.
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 cardio-protective 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.
尼可地尔是一种兼具硝酸盐样和三磷酸腺苷敏感性钾通道（K+ATP）激活特性的药物。凭借这种双重作用机制，该药物可作为一种平衡的冠状动脉和外周血管扩张剂，降低前负荷和后负荷。K+ATP通道已被证明与心肌预处理现象有关，在缺血再灌注诱导的心肌顿抑或梗死动物模型中的研究表明，尼可地尔具有心脏保护作用。对接受经皮腔内冠状动脉成形术（PTCA）的患者的研究表明，服用尼可地尔可降低缺血期间的ST段抬高。在早期非对照试验中，尼可地尔显著改善了稳定劳力型心绞痛患者运动耐量试验相对于基线的结果。在早期随机、双盲、安慰剂对照试验中，该药物相对于安慰剂也改善了运动耐量试验的结果。在心绞痛患者的随机、双盲对照研究中，通过运动耐量试验测量，尼可地尔已证明与二硝酸异山梨酯、单硝酸异山梨酯、美托洛尔、普萘洛尔、阿替洛尔、地尔硫䓬、氨氯地平和硝苯地平具有等效疗效。短期内已对尼可地尔对急性心肌梗死所致缺血性损伤后心肌恢复各方面的影响进行了研究。区域左心室（LV）壁运动是心肌功能的一个指标，相对于对照组，接受尼可地尔治疗的患者有显著改善。与尼可地尔作为心绞痛治疗相关的主要不良事件是头痛。对于易患头痛的患者，可通过低剂量开始使用尼可地尔将其降至最低。接受尼可地尔治疗的患者有口腔溃疡的罕见病例报告；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有用的背景治疗药物。在高危患者急性心肌梗死后直接作为干预策略的一部分使用时，该药物也已证明具有潜在的心脏保护作用。人们期待着对尼可地尔在这后一种适应症方面进行进一步的大规模长期研究。
