Comparative absorption kinetics of intramuscular midazolam and diazepam

被引:26
作者
Hung, OR
Dyck, JB
Varvel, J
Shafer, SL
Stanski, DR
机构
[1] DALHOUSIE UNIV,DEPT ANAESTHESIA,HALIFAX,NS,CANADA
[2] DALHOUSIE UNIV,DEPT PHARMACOL,HALIFAX,NS,CANADA
[3] STANFORD UNIV,SCH MED,DEPT ANESTHESIA,PALO ALTO,CA 94304
[4] STANFORD UNIV,SCH MED,DEPT MED CLIN PHARMACOL,PALO ALTO,CA 94304
[5] ST ELIZABETH COMMUNITY HLTH CTR,DEPT ANESTHESIA,LINCOLN,NE
来源
CANADIAN JOURNAL OF ANAESTHESIA-JOURNAL CANADIEN D ANESTHESIE | 1996年 / 43卷 / 05期
关键词
PHARMACOKINETICS; intramuscular administration; intravenous administration; BENZODIAZEPINES; midazolam; diazepam;
D O I
10.1007/BF03018105
中图分类号
R614 [麻醉学];
学科分类号
100217 ;
摘要
Purpose: This study investigates the rare and extent of absorption following intramuscular injection of midazolam and diazepam. Methods: Four healthy male volunteers were recruited in this randomized three-way cross-over study. On one occasion each subject received simultaneous im injections of 5 ms midazolam and 10 ms diazepam in separate deltoid muscles. On two other separate occasions each subject received an iv infusion of 7.5 ms midazolam and 30 ms diazepam over five minutes. Frequent arterial blood samples were collected for Icp to two hours and venous blood samples were collected for up to 24 hours for midazolam and ten days for diazepam. A gas chromatography assay was used to determine the plasma concentrations of midazolam and diazepam. The im absorption profiles were estimated using constrained least-squares deconvolution. Results: There were substantial intersubject variabilities in the estimated pharmacokinetic parameters (volumes and clearances) of intravenous midazolam and diazepam The mean (+/-sd) time to peak plasma concentration ((max)) was shorter for im midazolam (17.5 +/- 6.5 min) relative to diazepam (33.8 +/- 7.5 min). The mean (+sd) time to peak absorption rate was also shorter for midazolam (9 +/- 2 vs 13.8 +/- 7.5 min). The peak rate of absorption was identical (0.18 ms min(-1)) and bioavailability was 1.0 for both drugs. Conclusions: We conclude that midazolam has more rapid absorption than diazepam following in administration.
引用
收藏
页码:450 / 455
页数:6
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