Plasma binding of benzodiazepines in humans.

Abstract:

:Plasma binding of chlordiazepoxide, diazepam, loraxepam, 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.

journal_name

J Pharm Sci

authors

Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GR

doi

10.1002/jps.2600681034

subject

Has Abstract

pub_date

1979-10-01 00:00:00

pages

1320-2

issue

10

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)42858-8

journal_volume

68

pub_type

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