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盐酸瑞卡南在心脏病人静脉负荷及维持输注期间和之后的处置情况。

The disposition of recainam hydrochloride during and after intravenous loading and maintenance infusion in cardiac patients.

作者信息

Hampton E M, Anastasiou-Nana M I, Nanas J N, Nappi J M, Capuzzi D M, Anderson J L

机构信息

College of Pharmacy, University of Oklahoma, Oklahoma City.

出版信息

J Clin Pharmacol. 1987 Dec;27(12):951-6. doi: 10.1002/j.1552-4604.1987.tb05595.x.

Abstract

Recainam hydrochloride is a newly synthesized propylurea compound demonstrating potent antidysrhythmic effects. Recainam was administered as a loading dose of 3 mg/kg/40 minutes followed by a continuous infusion of 0.9 mg/kg/hr for 23 hours and 20 minutes to ten patients with cardiac disease and frequent PVCs (more than 30/hr). A total of 15 plasma samples were drawn over 36 hours during and after the infusion. Plasma recainam concentration was determined by high performance liquid chromatography (HPLC). The mean (+/- SD) postload and 24-hour plasma concentrations were 5.19 +/- 0.51 and 3.41 +/- 0.71 micrograms/mL, respectively. The data were best described by a two-compartment model yielding the following mean (+/- SD) pharmacokinetic parameters: lambda 1 = 2.62 +/- 0.68 hr-1, lambda 2 = 0.144 +/- 0.014 hr-1, t1/2 lambda 2 = 4.84 +/- 0.46 hr, CLT = 0.268 +/- 0.057 L/hr/kg, CLR = 0.143 +/- 0.052 L/kg/hr, CLNR = 0.125 +/- 0.041 L/hr/kg, Vdss = 1.3 +/- 0.19 L/kg, and Vd lambda 2 = 1.9 +/- 0.43 L/kg. There were no adverse reactions. Based on these data, recainam can be safely administered as a loading dose followed by a continuous infusion in patients with stable cardiac disease without significant ventricular dysfunction.

摘要

盐酸瑞卡南是一种新合成的丙基脲化合物,具有强大的抗心律失常作用。对10例患有心脏病且频发室性早搏(每小时超过30次)的患者,给予3毫克/千克/40分钟的负荷剂量的瑞卡南,随后以0.9毫克/千克/小时的速度持续输注23小时20分钟。在输注期间及之后的36小时内共采集了15份血浆样本。采用高效液相色谱法(HPLC)测定血浆瑞卡南浓度。负荷剂量后及24小时的血浆平均浓度(±标准差)分别为5.19±0.51和3.41±0.71微克/毫升。数据用二室模型描述最佳,得出以下平均(±标准差)药代动力学参数:λ1 = 2.62±0.68小时-1,λ2 = 0.144±0.014小时-1,t1/2λ2 = 4.84±0.46小时,CLT = 0.268±0.057升/小时/千克,CLR = 0.143±0.052升/千克/小时,CLNR = 0.125±0.041升/小时/千克,Vdss = 1.3±0.19升/千克,Vdλ2 = 1.9±0.43升/千克。未出现不良反应。基于这些数据,对于无明显心室功能障碍的稳定心脏病患者,瑞卡南可以安全地给予负荷剂量后持续输注。

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