Fung H L
Department of Pharmaceutics, School of Pharmacy, State University of New York, Buffalo 14260.
Eur Heart J. 1991 May;12 Suppl A:9-12.
Nitrate therapy has been shown to be beneficial for the treatment of coronary artery diseases and a number of chemical entities and their respective pharmaceutical formulations are available for clinical use. In this report, the performance of these nitrate drug/formulation combinations is discussed in terms of the relative onset of action, duration of action, tolerance properties/regeneration of reactivity and patient acceptance. A pharmacodynamic action scheme is presented and this allows a systematic assessment of how changes in the nitrate and/or formulation may impact on therapeutic activity. Data suggest that several sustained-release preparations of various nitrates can provide protection against exercise-induced angina for about 12 h on repeated dosing, provided a 'nitrate-free' or 'nitrate-poor' interval is also instituted. The 'ideal' nitrate substance and formulation, which theoretically can provide around-the-clock protection, is not yet available.
硝酸盐疗法已被证明对冠状动脉疾病的治疗有益，并且有多种化学实体及其相应的药物制剂可供临床使用。在本报告中，将从相对起效时间、作用持续时间、耐受性特性/反应性再生以及患者接受度等方面讨论这些硝酸盐药物/制剂组合的性能。提出了一种药效学作用方案，这使得能够系统地评估硝酸盐和/或制剂的变化如何影响治疗活性。数据表明，各种硝酸盐的几种缓释制剂在重复给药时可提供约12小时的运动诱发型心绞痛防护，前提是也要设定一个“无硝酸盐”或“低硝酸盐”间隔期。理论上能够提供全天候防护的“理想”硝酸盐物质和制剂尚未问世。
