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[酒石酸普拉马林的药代动力学及抗心律失常作用]

[Pharmacokinetics and Antiarrhythmic effects of Prajmalium Bitartrate].

作者信息

Trompler A T, Woodcock B G, Bussmann W D

出版信息

Arzneimittelforschung. 1983;33(3):436-9.

PMID:6683519
Abstract

8 patients with ventricular premature contractions were treated with prajmalium bitartrate (Neo-Gilurytmal) 20 mg q.i.d. The electrocardiograms were continuously monitored by a computerized arrhythmia monitoring system. For definition of the drug's pharmacokinetic properties plasma concentrations were determined. 7 patients showed a marked arrhythmia reduction. Mean ventricular premature contraction frequency was significantly reduced 6 h after onset of treatment, maximum arrhythmia suppression to 34% of control was observed after 24 h of treatment. The correlation of antiarrhythmic response and plasma concentrations was good. Mean plasma concentrations during steady state conditions were 218 ng/ml. Plasma half-life was determined 7.3 h. The lower limit of therapeutic plasma concentrations was between 43 and 145 ng/ml. A mean total clearance of 344 ml/min indicates a low hepatic extraction of prajmalium bitartrate. Moreover, the distribution volume of 204 l suggests a high tissue affinity of the drug.

摘要

8例室性早搏患者接受了20毫克每日4次的比特律(心得脉宁)治疗。通过计算机心律失常监测系统持续监测心电图。为明确该药物的药代动力学特性,测定了血浆浓度。7例患者的心律失常明显减轻。治疗开始6小时后,平均室性早搏频率显著降低,治疗24小时后观察到心律失常最大抑制率达对照值的34%。抗心律失常反应与血浆浓度的相关性良好。稳态条件下的平均血浆浓度为218纳克/毫升。血浆半衰期测定为7.3小时。治疗性血浆浓度下限在43至145纳克/毫升之间。平均总清除率为344毫升/分钟,表明比特律的肝脏提取率较低。此外,204升的分布容积表明该药物具有较高的组织亲和力。

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