Sica D A, Yonce C, Small R, Cefali E, Harford A, Poynor W
Department of Medicine, Medical College of Virginia, Richmond.
Int J Clin Pharmacol Ther Toxicol. 1988 Feb;26(2):59-64.
Procainamide (PA) and N-acetylprocainamide (NAPA) pharmacokinetics were examined in six patients undergoing continuous ambulatory peritoneal dialysis (CAPD) following a single oral dose of 625 mg of procainamide HCl. Peak serum PA concentrations occurred between 1 and 3 h after drug administration whereas peak NAPA levels were reached 14 to 48 h following the administration of PA. NAPA levels 1.2 mcg/ml or greater were present for 72 h and in four of the six subjects little further decline occurred at 96 h. PA total body clearance (TBC) averaged 143 ml/min; TBC for NAPA was 29.8 ml/min. PA and NAPA half-lives were considerably prolonged averaging 26.0 and 42.8 h, respectively. V beta for PA was 4.1 l/kg and for NAPA was 1.46 l/kg. PA and NAPA dialysance varied from 0.28 to 5.55 ml/min and from 1.74 to 7.20 ml/min, respectively. This, in turn, represented less than 5 and 25% of the TBC for each drug.
在6例接受持续性非卧床腹膜透析(CAPD)的患者中,口服单剂量625 mg盐酸普鲁卡因胺后,对普鲁卡因胺(PA)和N - 乙酰普鲁卡因胺(NAPA)的药代动力学进行了研究。给药后1至3小时出现血清PA浓度峰值,而PA给药后14至48小时达到NAPA水平峰值。NAPA水平在1.2 mcg/ml或更高时持续72小时,在6名受试者中的4名中,96小时时几乎没有进一步下降。PA的全身清除率(TBC)平均为143 ml/min;NAPA的TBC为29.8 ml/min。PA和NAPA的半衰期显著延长,平均分别为26.0小时和42.8小时。PA的Vβ为4.1 l/kg,NAPA的Vβ为1.46 l/kg。PA和NAPA的透析率分别在0.28至5.55 ml/min和1.74至7.20 ml/min之间变化。这反过来分别占每种药物TBC的不到5%和25%。