Plasma binding of benzodiazepines in humans

R. F. Johnson, S. Schenker, R. K. Roberts, P. V. Desmond, G. R. Wilkinson

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

Plasma binding of chlordiazepoxide, diazepam, lorazepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25‐86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20‐fold for oxazepam. Statistically significant linear relationships were not observed between the degree of binding and age, serum albumin, or total protein for any of the drugs. There was, however, a correlation between the extent of binding for the four drugs. Because of the importance of unbound benzodiazepine levels in eliciting any pharmacological response and also in disposition, consideration of the wide interindividual variability in plasma binding must be made in interpreting pharmacodynamic and pharmacokinetic data.

Original languageEnglish (US)
Pages (from-to)1320-1322
Number of pages3
JournalJournal of Pharmaceutical Sciences
Volume68
Issue number10
DOIs
StatePublished - Oct 1979
Externally publishedYes

Keywords

  • Benzodiazepines—plasma binding, equilibrium diaiysis, humans, individual variation, age
  • Plasma binding—benzodiazepines, humans, individual variation, age
  • Sedatives—benzodiazepines, plasma binding, equilibrium dialysis, humans, individual variation, age

ASJC Scopus subject areas

  • Pharmaceutical Science

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