Department of Pharmacology, Tulane University Medical Center, New Orleans, LA 70112-2699, USA.
Cardiol Rev. 2010 Jul-Aug;18(4):190-7. doi: 10.1097/CRD.0b013e3181c8e14a.
The organic nitrite, amyl of nitrite, was initially used as a therapeutic agent in the treatment of angina pectoris, but was replaced over a decade later by the organic nitrate, nitroglycerin (NTG), due to the ease of administration and longer duration of action. The administration of organic nitrate esters, such as NTG, continues to be used in the treatment of angina pectoris and heart failure since the birth of modern pharmacology. Their clinical effectiveness is due to vasodilator activity in large veins and arteries through an as yet unidentified method of delivering nitric oxide (NO), or a NO-like compound. The major drawback is the development of tolerance with NTG, and the duration and route of administration with amyl of nitrite. Although the nitrites are no longer used in the treatment of hypertension or ischemic heart disease, the nitrite anion has recently been discovered to possess novel pharmacologic actions, such as modulating hypoxic vasodilation, and providing cytoprotection in ischemia-reperfusion injury. Although the actions of these 2 similar chemical classes (nitrites and organic nitrates) have often been considered to be alike, we still do not understand their mechanism of action. Finally, the nitrite anion, either from sodium nitrite or an intermediate NTG form, may act as a storage form for NO and provide support for investigating the use of these agents in the treatment of ischemic cardiovascular states. We review what is presently known about the use of nitrates and nitrites including the historical, current, and potential uses of these agents, and their mechanisms of action.
有机亚硝酸盐，即亚硝酸戊酯，最初被用作心绞痛的治疗药物，但在十多年后，因其给药方便且作用持续时间更长，被有机硝酸盐，即硝酸甘油（NTG）所取代。自现代药理学诞生以来，硝酸酯类药物，如 NTG，一直被用于心绞痛和心力衰竭的治疗。它们的临床疗效是由于其在大静脉和动脉中的血管扩张活性，而这种活性的作用机制目前尚未确定，可能是通过释放一氧化氮（NO）或类似 NO 的化合物来实现的。主要的缺点是 NTG 会产生耐受性，而亚硝酸戊酯的作用持续时间和给药途径也存在问题。尽管亚硝酸盐已不再用于治疗高血压或缺血性心脏病，但最近发现亚硝酸盐阴离子具有新的药理作用，如调节缺氧性血管扩张和在缺血再灌注损伤中提供细胞保护作用。尽管这两类（亚硝酸盐和有机硝酸盐）化学物质的作用经常被认为相似，但我们仍然不了解它们的作用机制。最后，亚硝酸盐阴离子（无论是来自亚硝酸钠还是中间的 NTG 形式）可能作为 NO 的储存形式，并为研究这些药物在治疗缺血性心血管疾病中的应用提供支持。我们回顾了硝酸盐和亚硝酸盐的用途，包括这些药物的历史、当前和潜在用途，以及它们的作用机制。
