Abrams J
Division of Cardiology, University of New Mexico School of Medicine, Albuquerque.
Eur Heart J. 1989 May;10 Suppl A:11-9. doi: 10.1093/eurheartj/10.suppl_a.11.
The transdermal nitroglycerin patches have been very successful nitrate formulations since their introduction in 1982. Nevertheless, considerable controversy regarding efficacy and tolerance has arisen. Nitroglycerin has multiple mechanisms of action in angina pectoris. Transdermal nitroglycerin in ointment formulation has been known to be effective in angina. The patches, when used in a dose of greater than or equal to 10 mg (24 h)-1, provide classic nitrate NTG effects in angina patients. However, the problem of nitrate tolerance is significant; in acute dosing, the transdermal patches lose their efficacy by 24 h and, with chronic dosing, appear usually to have little advantage over placebo in improvement of angina. An intermittent or interval approach to transdermal patch delivery appears to be the best method of avoiding nitrate tolerance. Current data suggest using the patches for 12 or 14 h consecutively and then removing them for 10-12 h. Such dosing strategies appear to eliminate or markedly reduce the problem of nitrate tolerance.
自1982年引入以来，透皮硝酸甘油贴片一直是非常成功的硝酸盐制剂。然而，关于其疗效和耐受性出现了相当大的争议。硝酸甘油在心绞痛中有多种作用机制。已知软膏剂型的透皮硝酸甘油对心绞痛有效。当以大于或等于10 mg（24小时）-1的剂量使用贴片时，可为心绞痛患者提供经典的硝酸盐硝酸甘油效应。然而，硝酸盐耐受性问题很严重；在急性给药中，透皮贴片在24小时内失去疗效，而在慢性给药中，在改善心绞痛方面通常似乎比安慰剂几乎没有优势。间歇性或间隔性的透皮贴片给药方法似乎是避免硝酸盐耐受性的最佳方法。目前的数据表明，连续使用贴片12或14小时，然后去除10 - 12小时。这种给药策略似乎可以消除或显著减少硝酸盐耐受性问题。
