Sanders S W, Nappi J M, Foltz R L, Lutz J R, Anderson J L
J Clin Pharmacol. 1983 Feb-Mar;23(2-3):113-22. doi: 10.1002/j.1552-4604.1983.tb02713.x.
Twelve patients having frequent premature ventricular complexes (PVCs) averaging more than 60 per hour received a single 150-mg intravenous dose of pirmenol. Plasma pirmenol concentration declined biexponentially following the infusion and was analyzed according to a two-compartment open model. Following an erratic distribution phase, the terminal elimination half-life ranged from 4.2 to 16.9 hours, with a geometric mean of 7.6 hours. Total body clearance averaged 164 +/- 58 ml/min, and the mean volume of distribution was 1.45 +/- 0.38 liter/kg. Renal clearance averaged 46.6 +/- 21.2 ml/min, representing 30 +/- 10 per cent of total body clearance. Excretion of unchanged drug in the urine averaged 31.8 +/- 8 per cent of the dose. Renal clearance and elimination half-life were correlated (r = -0.61, P less than 0.05). Eight of the 12 patients achieved greater than 95 per cent suppression of PVCs with a duration between 20 minutes and 23 hours. These favorable pharmacokinetics indicate that pirmenol may be a useful addition to the therapy of ventricular arrhythmias.
12名频发室性早搏（PVCs）平均每小时超过60次的患者接受了单次150毫克静脉注射吡美诺。输注后血浆吡美诺浓度呈双指数下降，并根据二室开放模型进行分析。在不稳定的分布相之后，终末消除半衰期为4.2至16.9小时，几何均值为7.6小时。总体清除率平均为164±58毫升/分钟，平均分布容积为1.45±0.38升/千克。肾清除率平均为46.6±21.2毫升/分钟，占总体清除率的30±10%。尿中原形药物排泄平均占剂量的31.8±8%。肾清除率与消除半衰期相关（r = -0.61，P<0.05）。12名患者中有8名实现了PVCs抑制超过95%，持续时间在20分钟至23小时之间。这些良好的药代动力学表明吡美诺可能是室性心律失常治疗中的一种有用药物。
