Elson J, Strong J M, Lee W K, Atkinson A J
Clin Pharmacol Ther. 1975 Feb;17(2):134-40. doi: 10.1002/cpt1975172134.
Compared to procainamide in an animal arrhythmic model, the antiarrhythmic potency of the N-acetylated metabolite of procainamide (NAPA) was 92% with respect to dose and 70% with respect to plasma level. The antiarrhythmic effects of combinations of the drugs were additive. Measurements of procainamide and NAPA plasma levels needed to suppress ventricular extrasystoles suggested that both compounds are nearly equipotent in patients as well. The average plasma level required for arrhythmia control in these patients was equivalent to 5.1 mcg/ml procainamide. Since patients on long-term procainamide therapy have plasma concentrations of NAPA that are usually comparable to, and occasionally greater than, their procainamide levels, dose regiments based on procainamide levels alone need revision to include consideration of the levels of this metabolite.
在动物心律失常模型中，与普鲁卡因胺相比，普鲁卡因胺的N - 乙酰化代谢产物（NAPA）的抗心律失常效力，按剂量计算为92%，按血浆水平计算为70%。药物组合的抗心律失常作用是相加的。抑制室性早搏所需的普鲁卡因胺和NAPA血浆水平的测量表明，这两种化合物在患者中也几乎等效。这些患者控制心律失常所需的平均血浆水平相当于5.1 mcg/ml的普鲁卡因胺。由于长期接受普鲁卡因胺治疗的患者血浆中NAPA的浓度通常与他们的普鲁卡因胺水平相当，偶尔还会高于后者，因此仅基于普鲁卡因胺水平的给药方案需要修订，以考虑这种代谢产物的水平。
