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Recainam在抗药性心律失常患者中的剂量滴定和药代动力学。

Recainam dose titration and pharmacokinetics in patients with resistant arrhythmias.

作者信息

Davies R F, Lineberry M D, Funck-Brentano C, Echt D S, Lee J T, Capuzzi D M, Roden D M, Woosley R L

机构信息

Department of Medicine, Vanderbilt University, Nashville, Tenn.

出版信息

Clin Pharmacol Ther. 1989 Sep;46(3):324-34. doi: 10.1038/clpt.1989.146.

Abstract

Recainam, a new antiarrhythmic drug, was evaluated in 20 patients with drug-resistant stable ventricular arrhythmias. Dosage was increased stepwise every 48 to 72 hours until arrhythmia suppression, side effects, or a predetermined maximal dosage occurred. After a pharmacokinetic evaluation, efficacy was confirmed in a double-blind, crossover protocol. One patient had unusable ambulatory ECG data. There were 14 of 19 patients who responded during dose titration; efficacy was confirmed in 11 of 14. The mean effective dosage and trough plasma concentration were 427 mg every 8 hours and 1.83 micrograms/ml, respectively. One patient withdrew because of nausea. Slowing of intraventricular conduction necessitated dosage reduction in two patients. Plasma half-life was 9.4 +/- 4.1 hours, with renal elimination accounting for 62% of oral clearance. However, 66% of the variability in oral drug clearance was the result of nonrenal elimination. Oral recainam at dosages of 300 to 600 mg every 8 hours is effective in some drug-resistant ventricular arrhythmias and is well tolerated.

摘要

新型抗心律失常药物Recainam在20例耐药性稳定室性心律失常患者中进行了评估。每48至72小时逐步增加剂量,直至心律失常得到抑制、出现副作用或达到预定的最大剂量。经过药代动力学评估后,采用双盲交叉方案确认了其疗效。1例患者的动态心电图数据无法使用。19例患者中有14例在剂量滴定期间有反应;14例中有11例疗效得到确认。平均有效剂量和谷血浆浓度分别为每8小时427毫克和1.83微克/毫升。1例患者因恶心退出。2例患者因室内传导减慢需要减少剂量。血浆半衰期为9.4±4.1小时,经肾消除占口服清除率的62%。然而,口服药物清除率66%的变异性是非肾消除的结果。每8小时口服300至600毫克Recainam对某些耐药性室性心律失常有效,且耐受性良好。

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