PT  - JOURNAL ARTICLE
AU  - Y Igari
AU  - Y Sugiyama
AU  - Y Sawada
AU  - T Iga
AU  - M Hanano
TI  - Tissue distribution of 14C-diazepam and its metabolites in rats.
DP  - 1982 Nov 01
TA  - Drug Metabolism and Disposition
PG  - 676--679
VI  - 10
IP  - 6
4099  - http://dmd.aspetjournals.org/content/10/6/676.short
4100  - http://dmd.aspetjournals.org/content/10/6/676.full
SO  - Drug Metab Dispos1982 Nov 01; 10
AB  - We have kinetically investigated the tissue distribution of 14C-diazepam and described the appearance and disappearance of its metabolites (3-hydroxydiazepam, desmethyldiazepam, and oxazepam) following a single iv injection of 14C-diazepam into rats. Significant amounts of oxazepam were detected in plasma and various tissues in the rat, contrary to previous reports. Concentration-time profiles of diazepam in the main disposing organs (liver, kidney, and lung) and the other organs (brain, heart, and small intestine) indicated that diazepam was distributed rapidly to these organs. Concentration-time profiles of diazepam in the main tissues for drug distribution (skin and adipose) indicated that diazepam was slowly distributed to these tissues, whereas that in muscle, which is also responsible for drug distribution, indicated that diazepam was less rapidly distributed to this tissue. Metabolites appeared in plasma and various tissues or organs immediately after iv injection of diazepam. Metabolites levels in plasma and various tissues or organs were significantly lower than that of diazepam except for liver and small intestine, where metabolites levels were higher compared to that of diazepam and metabolites exhibited a considerable persistence.