Pharmacokinetics of prazepam in man

Smith, MT, Evans, Lej, Eadie, MJ and Tyrer, JH (1979) Pharmacokinetics of prazepam in man. European Journal of Clinical Pharmacology, 16 2: 141-147. doi:10.1007/BF00563121


Author Smith, MT
Evans, Lej
Eadie, MJ
Tyrer, JH
Title Pharmacokinetics of prazepam in man
Journal name European Journal of Clinical Pharmacology   Check publisher's open access policy
ISSN 0031-6970
Publication date 1979-01-01
Sub-type Article (original research)
DOI 10.1007/BF00563121
Volume 16
Issue 2
Start page 141
End page 147
Total pages 7
Publisher Springer-Verlag
Language eng
Subject 3000 Pharmacology, Toxicology and Pharmaceutics
2736 Pharmacology (medical)
Abstract An original electron-capture gas chromatographic assay was developed for simultaneous measurement of plasma levels of the benzodiazepine derivative prazepam and of its principal unconjugated metabolite, N-desmethyldiazepam. The assay was used to study the pharmacokinetics of the drug and its comparative bioavailability from tablets and from a specially prepared solution. Nine healthy adult volunteers were studied. Each volunteer on one occasion took 30 mg of the drug in tablet form, and on another occasion 30 mg of the drug in solution. In all subjects, N-desmethyldiazepam appeared in plasma shortly after prazepam appeared and reached a peak within four hours of prazepam ingestion. Thereafter plasma N-desmethyldiazepam levels were much higher than plasma prazepam levels throughout. Prazepam became undetectable within six hours of intake, whereas its metabolite could still be measured in plasma fourteen days after dosage. Thus much of the pharmacological action of prazepam may be mediated through its metabolite, N-desmethyldiazepam. In five of the nine subjects, areas under the plasma level curves for the metabolite were not markedly different for the tablet and solution formulations studied. In the other four subjects the area under the curve for the tablets was 50% to 80% of the area under the curve for the solution. The time to reach peak plasma level for the metabolite was shorter after the solution formulation (mean 2.0±SD 1.2 h) than after the tablet formulation (mean 4.2±SD 1.7 h).
Keyword bioavailability
electron-capture gasliquid chromatography
N-desmethyldiazepam
pharmokinetics
prazepam
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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Created: Sat, 02 Jul 2016, 02:18:58 EST by Ms Kate Rowe