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在过去5年中,常常提到抗心律失常药物代谢产物的临床重要性。首先,抗心律失常药物的治疗/毒性比率很狭。其次,由于有了新的测定血浆药物浓度的方法,许多作者试图将血浆浓度与疗效和副作用相联系。这对利多卡因、室安卡因和茚丙胺等是可行的,但对英卡胺、氯卡胺和普鲁卡因酰胺则不易建立这种联系。稳定状态血浆药物浓度不能与药理作用相关有许多可能的解释:(1)药物的作用是由其所产生的一种或多种活性代谢产物所介导,(2)药物排出后其所引起的细胞水平改变仍持续存在,(3)药物在心肌作用部位长期滞留而传统药动学分析方法不能发现
In the past five years, the clinical importance of anti-arrhythmic drug metabolites has often been mentioned. First, anti-arrhythmic drugs have a very low treatment / toxicity ratio. Second, many authors attempt to correlate plasma concentrations with efficacy and side effects due to new methods of determining plasma drug concentrations. This is valid for lidocaine, room-ampicillin, and indomethacin, but not for icarboxamine, procaine and procainamide. There are many possible explanations for steady-state plasma drug concentrations that can not be correlated with pharmacological effects: (1) the drug’s action is mediated by one or more of its active metabolites it produces, (2) Changes in cell levels persist, (3) Drugs remain in the myocardium for a long time and traditional pharmacokinetic analysis methods can not be found