Document Detail

Entrance into brain of dextropropoxyphene and the toxic metabolite norpropoxyphene.
MedLine Citation:
PMID:  288347     Owner:  NLM     Status:  MEDLINE    
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.
W L Way; J Schou
Related Documents :
19821017 - Effect of exercise on synaptophysin and calcium/calmodulin-dependent protein kinase lev...
15831797 - Effects of endurance exercise-training on single-fiber contractile properties of insuli...
10421227 - Insulin activation of pyruvate dehydrogenase complex is enhanced by exercise training.
12933347 - Activation of jnk in rat heart by exercise: effect of training.
2875657 - O2 consumption during exercise in dogs--roles of splenic contraction and alpha-adrenerg...
6189637 - Variations in amylase isoenzymes and lipase during acute pancreatitis, and in other dis...
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    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Brain / metabolism*
Dextropropoxyphene / metabolism*
Time Factors
Reg. No./Substance:

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

Previous Document:  Monoamine oxidase inhibiting and toxic effects of acetyl-phenylhydrazide on rat liver in vivo.
Next Document:  Prostaglandins in rat placenta following acute and chronic administration of morphine.