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Biliary elimination of diazepam in man
Author(s) -
Mahon W. A.,
Inaba T.,
Umeda T.,
Tsutsumi E.,
Stone R.
Publication year - 1976
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1976194443
Subject(s) - oxazepam , diazepam , enterohepatic circulation , urine , metabolite , bolus (digestion) , chemistry , half life , metabolism , pharmacology , pharmacokinetics , medicine , endocrinology , benzodiazepine , receptor
The metabolism of 14 C‐5‐diazepam has been studied in 5 patients with T tube biliary drainage. A single bolus of 40 to 50 μCi was given intravenously and blood, urine, and bile were analyzed from 5 to 14 days. The mean half‐life of elimination from blood was 93.2 hr; the major metabolite noted in blood was N‐desmethyl‐diazepam. in urine the average recovery of radioactivity was 48.9% and consisted of 3 OH‐diazepam, 4'OH‐diazepam, and oxazepam. in bile the average recovery of radioactivity was 5.35% (corrected to a bile flow of 700 ml was 15.0%) and consisted of the same metabolites as in the urine. Essentially no diazepam or N‐desmethyl‐diazepam was found, and therefore an enterohepatic circulation cannot be held to account for the prolonged half‐life of these substances in man.