Document Detail

Effect of heparin administration on flunitrazepam protein binding.
MedLine Citation:
PMID:  2707926     Owner:  NLM     Status:  MEDLINE    
Non-esterified fatty acids have been shown to displace diazepam from its plasma binding sites both in vitro and in vivo. However, the binding of other benzodiazepines such as lorazepam is not affected in similar situations. Flunitrazepam exhibits a substantial degree of binding to plasma proteins, therefore it was deemed interesting to investigate the role of free fatty acids on flunitrazepam binding to human plasma proteins. Incubation of plasma with sodium oleate (1.5 and 3.0 microEq per ml) produced a decrease in the binding of flunitrazepam. The free fraction increased from 4.20 +/- 0.34 to 6.30 +/- 0.53 and to 22.18 +/- 1.28% respectively). Sodium heparin administration (10IU/kg, intravenously) increased free fatty acids levels and produced similar changes in the binding of flunitrazepam. After ten minutes of heparin administration free fatty acids increased from 0.16 +/- 0.03 mEq/l to 0.34 +/- 0.01 mEq/l and the free fraction of flunitrazepam in plasma increased from 3.70 +/- 0.22% to 6.20 +/- 1.24%. These binding data further support a relationship between increases in the concentrations of free fatty acids and decreases in the fraction of flunitrazepam bound to plasma proteins.
R Calvo; L Aguilera; C Aguirre; J M Rodríguez Sasiaín
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  International journal of clinical pharmacology research     Volume:  9     ISSN:  0251-1649     ISO Abbreviation:  Int J Clin Pharmacol Res     Publication Date:  1989  
Date Detail:
Created Date:  1989-06-01     Completed Date:  1989-06-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8110183     Medline TA:  Int J Clin Pharmacol Res     Country:  SWITZERLAND    
Other Details:
Languages:  eng     Pagination:  59-63     Citation Subset:  IM    
Department of Pharmacology, University of Basque Country, Leioa, Vizcaya, Spain.
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MeSH Terms
Flunitrazepam / metabolism*
Heparin / pharmacology*
Protein Binding / drug effects
Reg. No./Substance:
1622-62-4/Flunitrazepam; 9005-49-6/Heparin

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