Anderson J L, Reddy C P, Myerburg R J, Waxman H L, de Vane P J
Department of Internal Medicine, University of Utah Medical School, Salt Lake City 84143.
Am J Cardiol. 1993 Mar 15;71(8):686-94. doi: 10.1016/0002-9149(93)91011-6.
The pharmacokinetics, antiarrhythmic activity and safety of intravenously administered recainam were evaluated in 15 men and 3 women. All patients had frequent (> 30/hour) ventricular premature complexes (VPCs) and unsustained ventricular tachycardia. Recainam was administered at a loading dose of 4.5 mg/kg/hour over 40 minutes, followed by a maintenance infusion of 0.9 mg/kg/hour for 23 hours and 20 minutes. Sixteen patients had satisfactory efficacy data. The mean frequency of total VPCs decreased by 92.6% and the mean frequency of runs decreased by 99.9% during the maintenance infusion. Suppressions of > or = 70% of total VPCs and > or = 90% of runs were maintained over the 23-hour, 20-minute maintenance infusion period in 16 of the 18 patients. During the maintenance infusion, hourly group plasma recainam concentrations ranged from mean +/- SD 2.6 +/- 0.7 to 3.4 +/- 0.9 micrograms/ml. Patients were observed for 24 hours after termination of the infusion. Periodic blood samples were obtained during and after termination of the infusion to determine recainam concentration. Urine specimens were collected over scheduled intervals to determine urinary excretion of recainam. A 2-compartment pharmacokinetic model was used to analyze the data. The following pharmacokinetic parameters were obtained: terminal elimination half-life, 5.0 +/- 0.8 hours; systemic clearance, 0.27 +/- 0.08 liter/hour/kg; and central and steady-state volume of distribution, 0.32 +/- 0.11 and 1.4 +/- 0.4 liter/kg, respectively. Adverse experiences were reported in 4 of the 18 patients, possibly drug-related in 2; none was considered severe or required discontinuation of recainam.(ABSTRACT TRUNCATED AT 250 WORDS)
对15名男性和3名女性静脉注射瑞卡南的药代动力学、抗心律失常活性及安全性进行了评估。所有患者均有频发(>30次/小时)室性早搏(VPC)和非持续性室性心动过速。瑞卡南以4.5毫克/千克/小时的负荷剂量静脉输注40分钟,随后以0.9毫克/千克/小时的维持剂量输注23小时20分钟。16名患者有满意的疗效数据。在维持输注期间,总VPC的平均频率下降了92.6%,连续发作的平均频率下降了99.9%。18名患者中有16名在23小时20分钟的维持输注期内,总VPC抑制率≥70%,连续发作抑制率≥90%。在维持输注期间,每小时组血浆瑞卡南浓度范围为平均±标准差2.6±0.7至3.4±0.9微克/毫升。输注结束后对患者观察24小时。在输注期间及结束后采集定期血样以测定瑞卡南浓度。按预定间隔收集尿液标本以测定瑞卡南的尿排泄量。采用二室药代动力学模型分析数据。获得了以下药代动力学参数:终末消除半衰期,5.0±0.8小时;全身清除率,0.27±0.08升/小时/千克;中央室和稳态分布容积分别为0.32±0.11和1.4±0.4升/千克。18名患者中有4名报告了不良事件,2名可能与药物相关;均未被认为严重或需要停用瑞卡南。(摘要截短于250字)