Arimori K, Hashimoto Y, Nakano M
Department of Pharmacy, Kumamoto University Hospital, Japan.
Chem Pharm Bull (Tokyo). 1990 Jul;38(7):2050-2. doi: 10.1248/cpb.38.2050.
Transfer of procainamide and its active metabolite, N-acetylprocainamide (NAPA) from the blood into the intestinal lumen was compared with that into the peritoneal cavity after i.v. administration of procainamide at the dose of 10 mg/kg to rats. The amounts of both drugs transferred from the blood into the intestinal lumen were much greater than those into the peritoneal cavity. The average amounts of procainamide transferred in 2 h into the intestinal lumen and the peritoneal cavity were 12.7% and 1.7% of dose (10 mg/kg), respectively, while those of NAPA were 3.5% and 1.4% of dose. The intestinal and peritoneal clearance values of procainamide were 143.5 and 59.4 ml/h, respectively, and those of NAPA were 32.6 and 13.5 ml/h. The difference in transfer rates across the intestinal and peritoneal membranes may be due to difference in the area of permeative surface and the extent of ionization in the dialysate. Consequently, it is expected that the gastrointestinal dialysis by oral administration of activated charcoal may serve as one of the more useful hemopurification methods than the peritoneal dialysis in procainamide and NAPA intoxication.
给大鼠静脉注射10mg/kg剂量的普鲁卡因胺后，比较了普鲁卡因胺及其活性代谢产物N - 乙酰普鲁卡因胺（NAPA）从血液向肠腔和向腹腔的转运情况。从血液转运到肠腔的两种药物的量远大于转运到腹腔的量。2小时内转运到肠腔和腹腔的普鲁卡因胺的平均量分别为给药剂量（10mg/kg）的12.7%和1.7%，而NAPA的平均量分别为给药剂量的3.5%和1.4%。普鲁卡因胺的肠清除率和腹腔清除率分别为143.5和59.4ml/h，NAPA的肠清除率和腹腔清除率分别为32.6和13.5ml/h。跨肠膜和腹膜的转运速率差异可能是由于渗透表面积和透析液中离子化程度的差异。因此，预计口服活性炭进行胃肠透析可能是比腹膜透析更有效的普鲁卡因胺和NAPA中毒血液净化方法之一。
