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普罗帕酮的多种作用模式。

The multiple modes of action of propafenone.

作者信息

Dukes I D, Vaughan Williams E M

出版信息

Eur Heart J. 1984 Feb;5(2):115-25. doi: 10.1093/oxfordjournals.eurheartj.a061621.

Abstract

Previous studies of widely different concentrations of propafenone in various species have reported that in addition to having class 1 antiarrhythmic action, the drug was a beta adrenoceptor blocker and a calcium antagonist. High concentration shortened action potential duration in animal experiments, but Q-T interval was reported as being lengthened in man. It was thought desirable to study the effects of propafenone over a range of concentrations equivalent to those used clinically in various cardiac tissues of a single species, the rabbit. It was concluded that although the primary action of propafenone was on fast inward current, the drug being categorised as of group 1c, its potency as a beta blocker was sufficient for the effect to be of clinical significance. Its potency as a calcium antagonist was relatively weak. Action potential duration and effective refractory period were lengthened in both atrium and ventricle, the effects being long-lasting and persisting on wash-out of the drug when other measurements had returned to control values.

摘要

以往对不同物种中广泛不同浓度普罗帕酮的研究报告称,该药物除具有Ⅰ类抗心律失常作用外,还是一种β肾上腺素能受体阻滞剂和钙拮抗剂。在动物实验中,高浓度可缩短动作电位时程,但据报道在人体中Q-T间期会延长。研究普罗帕酮在与兔这一单一物种的各种心脏组织中临床使用浓度相当的一系列浓度范围内的作用,被认为是可取的。得出的结论是,尽管普罗帕酮的主要作用是作用于快速内向电流,该药物被归类为Ⅰc类,但它作为β受体阻滞剂的效力足以使其作用具有临床意义。其作为钙拮抗剂的效力相对较弱。心房和心室的动作电位时程和有效不应期均延长,这些作用持久,当其他测量值恢复到对照值时,在药物洗脱后仍持续存在。

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