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透视硝酸酯给药系统。十年进展。

Nitrate delivery systems in perspective. A decade of progress.

作者信息

Abrams J

出版信息

Am J Med. 1984 Jun 22;76(6A):38-46. doi: 10.1016/0002-9343(84)91041-6.

Abstract

In recent years the use of nitroglycerin and long-acting nitrate compounds in clinical practice has been increasing. Only 10 to 15 years ago these drugs, at least in oral formulation, were felt to have no clinical utility because of concern that potent hepatic enzyme activity would degrade sufficient amounts of the nitrate compounds from reaching the systemic circulation. However, it is now recognized that oral nitrate administration when given in sufficient amounts achieves therapeutic plasma concentrations and desired clinical effects. Nitrates are routinely used for the treatment of stable and unstable angina and also play a role in therapy for complications of myocardial infarction. Nitrates are very effective agents for preload reduction in vasodilator therapy of congestive heart failure. A wide variety of nitrate delivery systems, including the standard oral and sublingual formulations, and as well as the new transdermal nitroglycerin discs and buccal nitroglycerin, are now available. Sublingual nitroglycerin, isosorbide dinitrate, and buccal nitroglycerin are used for acute treatment of attacks of ischemic chest pain. For ambulatory patients, long-acting therapy can be administered by oral, topical ointment, transdermal disc, and buccal nitroglycerin formulations. Each compound has a slightly different onset and duration of action, which is in part dose-dependent. The relative merits and problems with each of the formulations are reviewed. Intravenous nitroglycerin is now commercially available and plays an increasing role in the intensive care units. It is an ideal drug for acute chest pain syndromes, including acute myocardial infarction. Specialized tubing does not need to be employed. The wide variety of nitrate delivery systems available to physicians makes use of this tried and true therapy practical and easy to carry out for clinicians.

摘要

近年来,硝酸甘油和长效硝酸盐化合物在临床实践中的应用一直在增加。仅在10到15年前,这些药物,至少是口服制剂,被认为没有临床用途,因为担心强大的肝酶活性会使足够量的硝酸盐化合物无法进入体循环。然而,现在人们认识到,口服硝酸盐制剂给予足够剂量时可达到治疗性血浆浓度并产生预期的临床效果。硝酸盐常用于治疗稳定型和不稳定型心绞痛,在心肌梗死并发症的治疗中也发挥作用。硝酸盐是充血性心力衰竭血管扩张治疗中降低前负荷的非常有效的药物。现在有各种各样的硝酸盐给药系统,包括标准的口服和舌下制剂,以及新的硝酸甘油透皮贴剂和口腔硝酸甘油。舌下硝酸甘油、硝酸异山梨酯和口腔硝酸甘油用于急性缺血性胸痛发作的治疗。对于门诊患者,长效治疗可通过口服、外用软膏、透皮贴剂和口腔硝酸甘油制剂进行。每种化合物的起效时间和作用持续时间略有不同,部分取决于剂量。本文综述了每种制剂的相对优缺点和问题。静脉用硝酸甘油现已上市,并在重症监护病房中发挥着越来越重要的作用。它是治疗急性胸痛综合征,包括急性心肌梗死的理想药物。不需要使用特殊的输液管。医生可使用的多种硝酸盐给药系统使这种经过验证的治疗方法对临床医生来说切实可行且易于实施。

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