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一例索他洛尔大量中毒病例的药代动力学评估

Pharmacokinetic evaluation of a case of massive sotalol intoxication.

作者信息

Gustavsson C G, Vinge E, Norlander B O, Pantev E

机构信息

Department of Cardiology, University Hospital, Malmö, Sweden.

出版信息

Ann Pharmacother. 1997 Jul-Aug;31(7-8):856-9. doi: 10.1177/106002809703100709.

Abstract

OBJECTIVE

To describe serum concentrations and clearance of sotalol after a massive overdose.

CASE SUMMARY

A 37-year-old white man took 11.2 g of sotalol hydrochloride tablets in a suicide attempt. The first serum d,l-sotalol concentration 3 hours after taking the first tablet was 20.6 mg/L and the last measured concentration 59 hours later was 1.8 mg/L. Logarithmic transformation of the concentration data indicated two separate monoexponential phases in the elimination curve, with half-lives of 30.1 and 11.6 hours.

DISCUSSION

The shorter serum half-life in the later phase is comparable with that in four previously reported sotalol intoxications and within the normal range. The elimination rate increased in a temporal manner with an increase in systolic blood pressure about 30 hours after the patient was admitted. Since the sotalol elimination rate depends principally on renal function, we believe the initially slow elimination is due to a temporary reduction of the renal function caused by the systolic hypotension.

CONCLUSIONS

An initial phase of slow sotalol elimination may occur after severe overdoses. In our patient this was probably due to hypotension. Thus, blood pressure should be monitored carefully.

摘要

目的

描述大剂量过量服用索他洛尔后的血清浓度及清除情况。

病例摘要

一名37岁白人男性为自杀企图服用了11.2克盐酸索他洛尔片。服用首剂后3小时测得的首个血清d,l-索他洛尔浓度为20.6毫克/升,59小时后测得的最后一个浓度为1.8毫克/升。浓度数据的对数转换表明消除曲线中有两个独立的单指数相,半衰期分别为30.1小时和11.6小时。

讨论

后期较短的血清半衰期与之前报道的4例索他洛尔中毒情况相当,且在正常范围内。患者入院后约30小时,消除率随收缩压升高呈时间依赖性增加。由于索他洛尔的消除率主要取决于肾功能,我们认为最初消除缓慢是由于收缩期低血压导致肾功能暂时降低所致。

结论

严重过量服用后可能会出现索他洛尔消除的初始缓慢阶段。在我们的患者中,这可能是由于低血压所致。因此,应仔细监测血压。

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