Pharmacokinetics of midazolam and alpha-hydroxy-midazolam following rectal and intravenous administration. |
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Authors: | T G Clausen J Wolff P B Hansen F Larsen S N Rasmussen J S Dixon C Crevoisier |
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Affiliation: | Department of Anaesthesia, Bispebjerg Hospital, Copenhagen, Denmark. |
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Abstract: | 1. In an open cross-over trial, plasma concentrations of midazolam were measured in eight healthy male volunteers following administration of 0.3 mg kg-1 body weight given by the rectal and intravenous routes. 2. Maximum plasma concentrations of 92-156 ng ml-1 (mean 118 ng ml-1) were recorded from 20 to 50 min (mean 31 min) after rectal application. The rectal bioavailability was 40-65% (mean 52%) and the terminal half-life was 114-305 min (mean 161 min). 3. A substantial first-pass hepatic effect was observed following rectal administration. 4. No systemic or local intolerance was noted. 5. In conclusion, the rectal route of administration provides a rapid and reliable absorption of midazolam. |
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