The pharmacokinetics of midazolam in man

Smith, MT, Eadie, MJ and Brophy, TO (1981) The pharmacokinetics of midazolam in man. European Journal of Clinical Pharmacology, 19 4: 271-278. doi:10.1007/BF00562804

Author Smith, MT
Eadie, MJ
Brophy, TO
Title The pharmacokinetics of midazolam in man
Journal name European Journal of Clinical Pharmacology   Check publisher's open access policy
ISSN 0031-6970
Publication date 1981-01-01
Year available 1981
Sub-type Article (original research)
DOI 10.1007/BF00562804
Open Access Status Not yet assessed
Volume 19
Issue 4
Start page 271
End page 278
Total pages 8
Place of publication NEW YORK
Publisher Springer-Verlag
Language eng
Subject 3000 Pharmacology, Toxicology and Pharmaceutics
2736 Pharmacology (medical)
Abstract Midazolam, a new water-soluble benzodiazepine, was administered as: i) 5 mg intravenously, ii) a 10-mg oral solution and iii) a 10-mg oral tablet, to six volunteers whose informed consent had been obtained. Midazolam plasma concentrations were measured using an electron-capture gas-liquid chromatographic assay. After 5-mg intravenous midazolam, subjects fell asleep within 1-2 min and continued to sleep for an average of 1.33 h. After oral midazolam intake (solution or tablets), drowsiness appeared after a average of 0.38 h (range 0.25-0.55 h) and sleep continued for an average of 1.17 h. The time to reach peak plasma midazolam concentration after the 10-mg solution dose (0.37±0.45 h) did not differe significantly ('t'=2.04, df=10, p>0.05) from the time to reach peak plasma midazolam level after the 10-mg tablet dose (0.74±0.45 h). The terminal half-life, (t1/2), of midazolam in plasma was 1.77±0.83 h and there was no significant difference between the mean terminal half-life values obtained for the three midazolam formulations. The mean total clearance (Cl), of midazolam after 5-mg intravenous administration was 0.383±0.094 l·kg-1·h-1. The first pass effect, F, determined experimentally (0.36±0.09) indicated the substantial first pass metabolism of midazolam. The percentage of the midazolam dose excreted unchanged in urine in four subjects during the 0-8-h urine collection interval was very small (0.011%-0.028%).
Keyword benzodiazepine
first-pass metabolism
gas-liquid chromatography
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import - Archived
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Citation counts: TR Web of Science Citation Count  Cited 231 times in Thomson Reuters Web of Science Article | Citations
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