Document Detail


Clinical pharmacokinetics of the newer benzodiazepines.
MedLine Citation:
PMID:  6133664     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
New benzodiazepine derivatives continue to be developed and introduced into clinical use. The pharmacokinetic properties of these newer drugs can best be understood by their categorisation according to range of elimination half-life and pathway of metabolism (oxidation versus conjugation). Clobazam and halazepam are long half-life (and therefore accumulating) anxiolytics metabolised by oxidation. Alprazolam and clotiazepam also are oxidised compounds but have short to intermediate half-life values and therefore produce considerably less accumulation. Temazepam and lormetazepam are hypnotic agents with intermediate half-lives but metabolised by conjugation. The most unique of the newer benzodiazepines are the ultra-short half-life (oxidised) compounds midazolam, triazolam and brotizolam, which are essentially non-accumulating during multiple dosage.
Authors:
D J Greenblatt; M Divoll; D R Abernethy; H R Ochs; R I Shader
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.; Review    
Journal Detail:
Title:  Clinical pharmacokinetics     Volume:  8     ISSN:  0312-5963     ISO Abbreviation:  Clin Pharmacokinet     Publication Date:    1983 May-Jun
Date Detail:
Created Date:  1983-07-08     Completed Date:  1983-07-08     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  7606849     Medline TA:  Clin Pharmacokinet     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  233-52     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Alprazolam
Anti-Anxiety Agents / metabolism*
Azepines / metabolism
Benzodiazepines / metabolism
Benzodiazepinones / metabolism
Humans
Kinetics
Lorazepam / analogs & derivatives,  metabolism
Midazolam
Temazepam / metabolism
Triazolam / metabolism
Grant Support
ID/Acronym/Agency:
MH-34223/MH/NIMH NIH HHS
Chemical
Reg. No./Substance:
0/Anti-Anxiety Agents; 0/Azepines; 0/Benzodiazepinones; 12794-10-4/Benzodiazepines; 22316-47-8/clobazam; 23092-17-3/halazepam; 28911-01-5/Triazolam; 28981-97-7/Alprazolam; 57801-81-7/brotizolam; 59467-70-8/Midazolam; 846-49-1/Lorazepam; 846-50-4/Temazepam; 848-75-9/lormetazepam

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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