摘要(美国)：心血管疾病仍是美国人的首位死因. 有证据表明高尿酸血症与心血管事件的增加有直接关系，而这也是我们研究降尿酸药物在心血管疾病治疗中作用的基础。别嘌呤醇是传统的治疗痛风的基石，它可竞争性阻断尿酸生成所需的关键酶——黄嘌呤氧化酶，近期有临床研究评估了其作为心血管药物的作用。尿酸生成的流行病学及生化研究显示，不仅尿酸本身可导致心血管事件的增加及恶化，黄嘌呤氧化酶作用生成的自由基及超氧化物也可导致心血管事件的增加。尿酸盐及自由基会最终导致冠脉内皮功能受损及心肌氧化应激能力下降。别嘌呤醇减少尿酸形成的同时，也能够清除阴离子超氧化及尿酸形成过程中释放的自由基。临床研究显示，别嘌呤醇能够改善内皮功能受损，并因此改善心绞痛患者的运动耐量。别嘌呤醇可能通过改善机械能解偶联，增强心肌收缩力，改善左室射血分数，减轻氧化应激，减少充血性心衰的发病率及死亡率。本文综述了别嘌呤醇对心血管系统的药理作用，并提出别嘌呤醇可作为潜在药物治疗两种心血管疾病——缺血性心脏病和充血性心衰。

附原文 Abstract Cardiovascular disease (CVD) remains the leading cause of death in the United States. There is evidence that shows a direct relationship between an elevated uric acid level and an increased risk of cardiovascular (CV) events, which has set the foundation for the investigation of uric acid-lowering drugs for the treatment of CVD. Although traditionally the cornerstone therapy for gout, allopurinol's ability to be a competitive inhibitor of the key enzyme, xanthine oxidase, needed for uric acid formation, has prompted recent clinical research evaluating allopurinol as a CV drug. Epidemiologic and biochemical studies on uric acid formation have shown that it is not only uric acid itself that leads to worsening prognosis and increased CV events, but also the free radicals and superoxides formed during xanthine oxidase activity. The combination of uric acid formation and formed free radicals could ultimately lead to coronary endothelial dysfunction and worsening of myocardial oxidative stress. Along with preventing uric acid formation, allopurinol also has the ability to behave as a free radical scavenger of the superoxide anions and free radicals released during uric acid formation.Clinical studies have shown that allopurinol improves endothelial dysfunction and subsequently improves the exercise capacity in patients diagnosed with angina pectoris. Allopurinol has also been shown to decrease oxidative stress and ameliorate the morbidity and mortality of congestive heart failure patients by possibly improving mechanoenergetic uncoupling, with the enhancement of myocardial contractility and the left ventricular ejection fraction. This review presents the pharmacologic action of allopurinol on the CV system and describes the effectiveness of allopurinol as a potential drug to treat 2 CVD morbidities: ischemic heart disease and congestive heart failure.

引自 Kelkar A, Kuo A, Frishman WH.Allopurinol as a cardiovascular drug. Cardiol Rev. 2011