Comparative protein binding of diazepam and desmethyldiazepam

The extent of plasma protein binding of diazepam (DZ) and its major metabolite, desmethyldiazepam (DMDZ), was determined by equilibrium dialysis in plasma samples drawn from 62 nonfasting unheparinized volunteers aged 20 to 85 years. The free fraction for diazepam averaged 1.48 per cent (range 0.85 to 2.30 per cent) and increased with age (r = 0.33). Desmethyldiazepam also was extensively bound. The mean free fraction was 2.97 per cent (range 1.78 to 5.28 per cent) and increased with age (r = 0.27). Free fractions for both diazepam and desmethyldiazepam were negatively correlated with plasma albumin concentration (r = --0.17 and --0.39). However, age, sex, and albumin explained only a small proportion of variability in free fraction for either compound. Free fraction for desmethyldiazepam always exceeded that for diazepam, and the two were correlated (r = 0.32). Thus, at any given total plasma concentration, the unbound concentration of desmethyldiazepam will exceed that of diazepam.
CiteULike    Complore    Connotea    Del.icio.us    Digg    Reddit    Technorati    Twitter    What's this?

This article has been cited by other articles:

				M. M. Iqbal, T. Sobhan, and T. Ryals Effects of Commonly Used Benzodiazepines on the Fetus, the Neonate, and the Nursing Infant Psychiatr Serv, January 1, 2002; 53(1): 39 - 49. [Abstract] [Full Text] [PDF]