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充血性心力衰竭对奎尼丁药代动力学的影响。

The effect of congestive heart failure on quinidine pharmacokinetics.

作者信息

Crouthamel W G

出版信息

Am Heart J. 1975 Sep;90(3):335-9. doi: 10.1016/0002-8703(75)90322-1.

Abstract

Quinidine is an effective antiarrhythmic agent whose therapeutic effects and toxicity have been related to its serum concentrations. Many patients with cardiac arrhythmias also suffer from congestive heart failure. It is well documented that congestive heart failure can reduce blood perfusion to many regions of the body, and could conceivably alter drug pharmacokinetics. A pharmacokinetic evaluation of two sets of quinidine data in congestive heart failure patients indicates that congestive heart failure reduced the rate of absorption and volume of distribution following oral or intramuscular administration of quinidine. Furthermore, the amount of quinidine absorbed following oral administration is reduced, but congestive heart failure does not appear to alter the elimination rate of quinidine. The interpretation of the data presented herein strongly suggests that the site of administration, extent of distribution, and rate of absorption must be considered when determining dosage regimens in congestive heart failure patients since normal dosages in these patients result in abnormally high serum quinidine concentrations.

摘要

奎尼丁是一种有效的抗心律失常药物,其治疗效果和毒性与血清浓度有关。许多心律失常患者也患有充血性心力衰竭。有充分的文献记载,充血性心力衰竭会减少身体许多部位的血液灌注,并且可以想象会改变药物的药代动力学。对两组充血性心力衰竭患者的奎尼丁数据进行的药代动力学评估表明,充血性心力衰竭降低了口服或肌肉注射奎尼丁后的吸收速率和分布容积。此外,口服后吸收的奎尼丁量减少,但充血性心力衰竭似乎不会改变奎尼丁的消除速率。本文所呈现数据的解释强烈表明,在确定充血性心力衰竭患者的给药方案时,必须考虑给药部位、分布范围和吸收速率,因为这些患者使用正常剂量会导致血清奎尼丁浓度异常升高。

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