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妥卡尼在合并左心室衰竭的急性心肌梗死患者中的药代动力学和血流动力学效应

Pharmacokinetics and haemodynamic effects of tocainide in patients with acute myocardial infarction complicated by left ventricular failure.

作者信息

MacMahon B, Bakshi M, Branagan P, Kelly J G, Walsh M J

出版信息

Br J Clin Pharmacol. 1985 Apr;19(4):429-34. doi: 10.1111/j.1365-2125.1985.tb02666.x.

Abstract

The pharmacokinetics and haemodynamic effects of tocainide, an orally active structural analogue of lignocaine, were studied in patients with acute myocardial infarction complicated by left ventricular failure. Fourteen patients (mean age 65 years) with acute myocardial infarction complicated by mild left ventricular failure were studied, following a single dose of tocainide (250 mg) by intravenous infusion, over 30 min. Heart rate, systemic arterial pressure, pulmonary artery pressure and cardiac output were monitored. Plasma tocainide levels were estimated by gas chromatography. The mean plasma level of tocainide achieved was 2.95 micrograms/ml (15.37 mmol/l). The mean plasma half-life was 15.6 h. The mean cardiac index was reduced 5 min after completion of the infusion, from 2.24 1 min-1 m-2 (+/- 0.40) to 2.07 1 min-1 m-2 (+/- 0.29) (P less than 0.01). At 90 min the cardiac index had returned to pre-treatment levels. Small changes were seen in the heart rate, arterial blood pressure and the pulmonary artery pressure but these changes were not statistically significant. The pharmacokinetics of tocainide were not significantly altered in patients with acute myocardial infarction complicated by mild left ventricular failure.

摘要

对利多卡因的口服活性结构类似物妥卡尼的药代动力学和血流动力学效应进行了研究,研究对象为并发左心室衰竭的急性心肌梗死患者。对14例(平均年龄65岁)并发轻度左心室衰竭的急性心肌梗死患者进行了研究,静脉输注单剂量妥卡尼(250mg),输注时间超过30分钟。监测心率、体动脉压、肺动脉压和心输出量。通过气相色谱法测定血浆妥卡尼水平。妥卡尼的平均血浆水平为2.95微克/毫升(15.37毫摩尔/升)。平均血浆半衰期为15.6小时。输注结束后5分钟,平均心脏指数从2.24升/分钟·平方米(±0.40)降至2.07升/分钟·平方米(±0.29)(P<0.01)。90分钟时,心脏指数已恢复至治疗前水平。心率、动脉血压和肺动脉压有小的变化,但这些变化无统计学意义。并发轻度左心室衰竭的急性心肌梗死患者中,妥卡尼的药代动力学无显著改变。

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