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肌内注射东莨菪碱加吗啡的药代动力学及临床效果。两个注射部位的比较。

Pharmacokinetics and clinical effects of intramuscular scopolamine plus morphine. A comparison of two injection sites.

作者信息

Kentala E, Scheinin H, Kaila T, Seppälä T, Kanto J

机构信息

Department of Anaesthesiology, University of Turku, Finland.

出版信息

Acta Anaesthesiol Scand. 1998 Mar;42(3):323-8. doi: 10.1111/j.1399-6576.1998.tb04924.x.

Abstract

BACKGROUND

Intramuscular scopolamine plus morphine premedication is traditionally used when prominent sedative or antisialogogue effect is needed. Knowledge of the pharmacokinetics of scopolamine is limited due to low plasma concentrations found after therapeutic doses. This investigation compares the pharmacokinetics and the clinical responses of this drug combination injected into two commonly used injection sites.

METHODS

Twelve ASA class 1 patients scheduled for minor surgery under spinal anaesthesia received scopolamine 6 micrograms/kg plus morphine 200 micrograms/kg injected in either deltoid (group D, n = 6) or gluteal (group G, n = 6) muscle.

RESULTS

The peak plasma concentrations of scopolamine after deltoid or gluteal injection (2.2 vs 1.6 micrograms/l) and the time they were reached (17 vs 19 min) were comparable. The absorption of morphine was similar in both groups (Tmax 16 min), but the peak plasma concentrations were higher after deltoid injection (71 vs 49 micrograms/l). The individual variation in the elimination half-lives of both scopolamine and morphine was smaller after deltoid injection (T1/2 scopolamine 1.9 +/- 0.7 vs 2.1 +/- 1.1 h, morphine 1.3 +/- 0.7 vs 2.3 +/- 1.5 h). Moderate slowing (25%) of heart rate was found in both groups. A heavy sedation and antisialogogue effect (VAS) was found in both groups with faster occurrence of maximal effect in group D (60 vs 120-180 min).

CONCLUSION

More predictable pharmacokinetics and clinical effects of intramuscular scopolamine plus morphine premedication can be achieved after an injection into deltoid muscle.

摘要

背景

当需要显著的镇静或抗唾液分泌作用时,传统上使用肌内注射东莨菪碱加吗啡进行术前用药。由于治疗剂量后血浆浓度较低,关于东莨菪碱的药代动力学知识有限。本研究比较了将这种药物组合注射到两个常用注射部位后的药代动力学和临床反应。

方法

12例计划在脊髓麻醉下进行小手术的ASA 1级患者接受了6微克/千克东莨菪碱加200微克/千克吗啡的注射,分别注射到三角肌(D组,n = 6)或臀肌(G组,n = 6)。

结果

三角肌或臀肌注射后东莨菪碱的血浆峰值浓度(2.2对1.6微克/升)及其达到的时间(17对19分钟)相当。两组中吗啡的吸收相似(达峰时间16分钟),但三角肌注射后血浆峰值浓度更高(71对49微克/升)。三角肌注射后,东莨菪碱和吗啡消除半衰期的个体差异较小(东莨菪碱半衰期1.9±0.7对2.1±1.1小时,吗啡半衰期1.3±0.7对2.3±1.5小时)。两组均发现心率适度减慢(25%)。两组均出现深度镇静和抗唾液分泌作用(视觉模拟评分),D组达到最大效应的时间更快(60对120 - 180分钟)。

结论

肌内注射东莨菪碱加吗啡进行术前用药时,注射到三角肌后药代动力学和临床效果更可预测。

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