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奎尼丁:治疗学、药代动力学及血清浓度监测的最新进展

Quinidine: an update on therapeutics, pharmacokinetics and serum concentration monitoring.

作者信息

Crevasse L

机构信息

Department of Medicine, J. Hillis Miller Health Center, Gainesville, Florida 32610.

出版信息

Am J Cardiol. 1988 Nov 3;62(14):22I-23I. doi: 10.1016/0002-9149(88)91344-6.

Abstract

After 70 years of regular use, quinidine remains one of the most useful drugs in the management of both supraventricular and ventricular arrhythmias. Quinidine sulfate, from conventional dosage forms, is absorbed rapidly and reaches peak levels in 1 hour. Sustained-release quinidine sulfate and gluconate are absorbed more slowly and, thus, may provide a more satisfactory response with less fluctuation in the peak and trough at quinidine concentrations. The half-life and absorption characteristics of sustained-release quinidine suggest that an 8- to 12-hour dosage regimen will produce smooth, sustained quinidine levels. Whereas quinidine and digitalis have been used concomitantly for years, dramatic elevations in blood digoxin levels have been observed. When quinidine is added to the regimen of a patient taking digitalis, these increased digoxin levels may be responsible for some of the adverse effects previously attributed to quinidine administration and can be reduced by adjustment of the digoxin dosage. Drug monitoring of serum quinidine concentrations as well as peak levels is essential to assess patient compliance and to determine that therapeutic levels are maintained. This is especially important because of the drug's relatively narrow therapeutic index and the changes in clearance that can result from drug interactions and renal and hepatic disturbances. A personal computer program is available to carry out pharmacokinetic calculations and assist in determining appropriate doses for individual patients.

摘要

经过70年的常规使用,奎尼丁仍然是治疗室上性和室性心律失常最有效的药物之一。常规剂型的硫酸奎尼丁吸收迅速,1小时内达到峰值水平。硫酸奎尼丁缓释剂和葡萄糖酸盐吸收较慢,因此,在奎尼丁浓度的峰值和谷值波动较小的情况下,可能会提供更令人满意的反应。硫酸奎尼丁缓释剂的半衰期和吸收特性表明,8至12小时的给药方案将产生平稳、持续的奎尼丁水平。尽管奎尼丁和洋地黄已经联合使用多年,但已观察到血液中地高辛水平显著升高。当将奎尼丁添加到服用洋地黄的患者治疗方案中时,这些升高的地高辛水平可能是一些先前归因于奎尼丁给药的不良反应的原因,并且可以通过调整地高辛剂量来降低。监测血清奎尼丁浓度以及峰值水平对于评估患者的依从性和确定维持治疗水平至关重要。这一点尤为重要,因为该药物的治疗指数相对较窄,并且药物相互作用以及肾脏和肝脏功能紊乱可能导致清除率发生变化。有一个个人计算机程序可用于进行药代动力学计算,并协助确定个体患者的合适剂量。

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