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Clinical Pharmacology of Benzodiazepines

Clinical Pharmacology of Benzodiazepines The benzodiazepines are the most widely used anxiolytic drugs. Their pharmacokinetic properties differ widely. Side effects are usually mild but dependence can supervene after long-term administration, even if normal therapeutic doses are not exceeded. Careful monitoring of use is essential. INTRODUCTION During the past 25 years, over 500 million people have taken benzo­ diazepine medication for anxiety, insomnia, muscle spasm, stress-related disorders, and epilepsy, and/or as part of pre-operative preparation. The recent decrease in prescriptions for benzodiazepines reflects both medical and lay concern regarding chronic side effects and physical dependence. However, although short-term use is less frequent, long-term use is still common. Pharmacokinetics The benzodiazepines have important pharmacokinetic differences with respect to speed of onset and duration of action. The rate of onset depends on the mode of administration, the dissolution of the formulation, the rapidity of absorption, and the rate of entry into the brain. Diazepam is rapidly absorbed after oral use and enters the brain quickly, thus promptly relieving anxiety. Given intravenously, it can rapidly stop repeated epi­ leptic seizures. Desmethyldiazepam is absorbed more slowly than diaze­ pam. Oxazepam is quite slowly absorbed and takes some time to pene­ trate the brain. Lorazepam is also slow http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Annual Review of Medicine Annual Reviews

Clinical Pharmacology of Benzodiazepines

Lader, M
Annual Review of Medicine , Volume 38 (1) – Feb 1, 1987
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References (16)

Publisher
Annual Reviews
Copyright
Copyright 1987 Annual Reviews. All rights reserved
Subject
Review Articles
ISSN
0066-4219
eISSN
1545-326X
DOI
10.1146/annurev.me.38.020187.000315
pmid
3555291
Publisher site
See Article on Publisher Site

Abstract

The benzodiazepines are the most widely used anxiolytic drugs. Their pharmacokinetic properties differ widely. Side effects are usually mild but dependence can supervene after long-term administration, even if normal therapeutic doses are not exceeded. Careful monitoring of use is essential. INTRODUCTION During the past 25 years, over 500 million people have taken benzo­ diazepine medication for anxiety, insomnia, muscle spasm, stress-related disorders, and epilepsy, and/or as part of pre-operative preparation. The recent decrease in prescriptions for benzodiazepines reflects both medical and lay concern regarding chronic side effects and physical dependence. However, although short-term use is less frequent, long-term use is still common. Pharmacokinetics The benzodiazepines have important pharmacokinetic differences with respect to speed of onset and duration of action. The rate of onset depends on the mode of administration, the dissolution of the formulation, the rapidity of absorption, and the rate of entry into the brain. Diazepam is rapidly absorbed after oral use and enters the brain quickly, thus promptly relieving anxiety. Given intravenously, it can rapidly stop repeated epi­ leptic seizures. Desmethyldiazepam is absorbed more slowly than diaze­ pam. Oxazepam is quite slowly absorbed and takes some time to pene­ trate the brain. Lorazepam is also slow

Journal

Annual Review of Medicine – Annual Reviews

Published: Feb 1, 1987

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