Document Detail


Entrance into brain of dextropropoxyphene and the toxic metabolite norpropoxyphene.
MedLine Citation:
PMID:  288347     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Several studies show that dextropropoxyphene after oral administration is intensively biotransformed to norpropoxyphene by first pass metabolism in the liver. While dextropropoxyphene is analgesic, cardiotoxic and shows CNS toxicity with convulsions and respiratory depression, norpropoxyphene is cardiotoxic to the same degree as dextropropoxyphene, but is without analgesic or CNS-toxic effects (Lund-Jacobsen, 1978). This principal difference between the effects of dextropropoxyphene and norpropoxyphene might be due to differences in penetration into the brain. We investigated the penetration of the two compounds in 14C-labelled moities into the brain of rats by the technique originally described by Oldendorf (1970). By this method the extraction of dextropropoxyphene was found extremely high, while it was much lower for the metabolite. The extraction percentage for dextropropoxyphene after 5 and 10 S was 350 +/- 34.1 and 164 +/- 15.2, respectively, while the values for norpropoxyphene was 62 +/- 6.2 and 44 +/- 4.1 (mean +/- S.E.M.), respectively. This difference may at least partly explain the missing CNS-symptoms with the metabolite.
Authors:
W L Way; J Schou
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Archives of toxicology. Supplement. = Archiv für Toxikologie. Supplement     Volume:  -     ISSN:  0171-9750     ISO Abbreviation:  Arch. Toxicol. Suppl.     Publication Date:  1979  
Date Detail:
Created Date:  1979-09-25     Completed Date:  1979-09-25     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  7802567     Medline TA:  Arch Toxicol Suppl     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  367-70     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Brain / metabolism*
Dealkylation
Dextropropoxyphene / metabolism*
Female
Male
Rats
Time Factors
Chemical
Reg. No./Substance:
469-62-5/Dextropropoxyphene

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


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