McClellan K J, Plosker G L
Adis International Limited, Auckland, New Zealand.
Drugs. 1999 Jul;58(1):143-57. doi: 10.2165/00003495-199958010-00016.
The orally administered antianginal agent trimetazidine increases cell tolerance to ischaemia by maintaining cellular homeostasis. In theory, this cytoprotective activity should limit myocyte loss during ischaemia in patients with angina pectoris. Data from studies in patients with coronary artery disease indicate that, unlike the effects of other antianginals, the anti-ischaemic effects of trimetazidine 20 mg are not associated with alterations in haemodynamic determinants of myocardial oxygen consumption such as heart rate, systolic blood pressure and the rate-pressure product. Furthermore, limited evidence suggests trimetazidine may improve left ventricular function in patients with chronic coronary artery disease or ischaemic cardiomyopathy and in patients experiencing acute periods of ischaemia when undergoing percutaneous transluminal coronary angioplasty. Clinical studies have shown that oral trimetazidine 20 mg 3 times daily reduces the frequency of anginal attacks and nitroglycerin use and increases exercise capacity when used as monotherapy in patients with angina pectoris. Its clinical effects are broadly similar to those of nifedipine 40 mg/day and propranolol 120 to 160 mg/day but, unlike these agents, trimetazidine does not affect the rate-pressure product during peak exercise or at rest. Adjunctive trimetazidine 60 mg/day reduces the frequency of anginal attacks and nitroglycerin use and improves exercise capacity in patients with angina pectoris not sufficiently controlled by conventional antianginal agents. Furthermore, the drug appears to be more effective than isosorbide dinitrate 30 mg/day when used adjunctively in patients with angina pectoris poorly controlled by propranolol 120 mg/day. The tolerability profile of trimetazidine 60 mg/day was similar to that of placebo when used as add-on therapy in patients with angina pectoris insufficiently controlled by other antianginal agents and was superior to that of either nifedipine 40 mg/day or propranolol 120 to 160 mg/day when used as monotherapy. The most frequently reported adverse events in trimetazidine recipients were gastrointestinal disorders, although the incidence of these events was low.
Trimetazidine is an effective and well tolerated anti-ischaemic agent which, in addition to providing symptom relief and functional improvement in patients with angina pectoris, has a cytoprotective action during ischaemia. The drug is suitable for initial use as monotherapy in patients with angina pectoris and, because of its different mechanism of action, as adjunctive therapy in those with symptoms not sufficiently controlled by nitrates, beta-blockers or calcium antagonists. The role of trimetazidine in other coronary conditions has yet to be clearly established.
口服抗心绞痛药物曲美他嗪通过维持细胞内环境稳定来提高细胞对缺血的耐受性。从理论上讲，这种细胞保护活性应能限制心绞痛患者缺血期间的心肌细胞损失。冠心病患者的研究数据表明，与其他抗心绞痛药物的作用不同，20毫克曲美他嗪的抗缺血作用与心肌耗氧量的血流动力学决定因素（如心率、收缩压和心率-血压乘积）的改变无关。此外，有限的证据表明，曲美他嗪可能改善慢性冠心病或缺血性心肌病患者以及接受经皮腔内冠状动脉成形术时处于急性缺血期患者的左心室功能。临床研究表明，心绞痛患者每日3次口服20毫克曲美他嗪作为单一疗法使用时，可减少心绞痛发作频率和硝酸甘油的使用，并提高运动能力。其临床效果与每日40毫克硝苯地平和每日120至160毫克普萘洛尔大致相似，但与这些药物不同的是，曲美他嗪在运动峰值或休息时不影响心率-血压乘积。每日60毫克曲美他嗪辅助用药可减少心绞痛发作频率和硝酸甘油的使用，并改善常规抗心绞痛药物控制不佳的心绞痛患者的运动能力。此外，在每日120毫克普萘洛尔控制不佳的心绞痛患者中辅助使用时，该药物似乎比每日30毫克硝酸异山梨酯更有效。在其他抗心绞痛药物控制不佳的心绞痛患者中作为附加疗法使用时，每日60毫克曲美他嗪的耐受性与安慰剂相似，作为单一疗法使用时优于每日40毫克硝苯地平或每日120至160毫克普萘洛尔。曲美他嗪使用者中最常报告的不良事件是胃肠道疾病，不过这些事件的发生率较低。
曲美他嗪是一种有效且耐受性良好的抗缺血药物，除了能缓解心绞痛患者的症状和改善功能外，在缺血期间还具有细胞保护作用。该药物适合心绞痛患者初始作为单一疗法使用，并且由于其作用机制不同，也适合作为硝酸盐、β受体阻滞剂或钙拮抗剂控制症状不佳患者的辅助疗法。曲美他嗪在其他冠状动脉疾病中的作用尚未明确确立。
