Olsson G, Allgén J
Department of Medicine, Cardiovascular Research, AB Hässle, Mölndal, Sweden.
Eur Heart J. 1991 May;12 Suppl A:21-3.
Nitrates have a place in the prophylactic treatment of patients with angina pectoris. Their efficacy is not in doubt. However, there may be some practical problems associated with their use, such as unreliable absorption, short duration of action, treatment-induced headache, development of nitrate tolerance and a suggested rebound phenomenon observed during intermittent dosing. This article discusses how many of these problems may be solved by selection of formulation as well as nitrate compound. Thus, the development of a controlled-release formulation producing sufficiently high nitrate plasma concentrations during part of the day, followed by a low nitrate level rather than a nitrate-free interval, seems to have the potential to prevent both nitrate tolerance and rebound phenomenon. This system would also offer a sufficiently long duration of action with a convenient once-daily dose regimen.
硝酸盐在心绞痛患者的预防性治疗中占有一席之地。其疗效毋庸置疑。然而，使用硝酸盐可能存在一些实际问题，如吸收不可靠、作用持续时间短、治疗引起的头痛、硝酸盐耐受性的产生以及间歇给药期间观察到的所谓反跳现象。本文讨论了如何通过制剂以及硝酸盐化合物的选择来解决其中的许多问题。因此，开发一种控释制剂，使其在一天中的部分时间产生足够高的血浆硝酸盐浓度，随后是低硝酸盐水平而非无硝酸盐间隔，似乎有可能预防硝酸盐耐受性和反跳现象。该系统还将提供足够长的作用持续时间，并采用方便的每日一次给药方案。
