Metabolism of flurazepam, a benzodiazepine, in man and dog

✍ Scribed by Morton A. Schwartz; Edward Postma

• Publisher: John Wiley and Sons
• Year: 1970
• Tongue: English
• Weight: 721 KB
• Volume: 59
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600591220

✦ Synopsis

The metabolism of 14C-flurazepam hydrochloride, 7-

hydr0-2H-l,4-benzodiazepin-2-one-5-~~C dihydrochloride, was studied in a dog administered oral and intravenous 2-mg./kg. doses and in two human subjects who each received a 28-mg. oral dose. In both species, evidence was obtained for rapid and essentially complete absorption followed by a rapid elimination of plasma flurazepam. Biotransformation of the drug was rapid and virtually complete in man and dog. Pathways of biotransformation were similar in both species. All the metabolites identified either showed some alteration in the N1-diethylaminoethyl moiety or lacked the Nl-substituent altogether. The major metabolite in the dog was a carboxylic acid, the Nl-acetic acid analog of flurazepam. In man, the analogous alcohol (the Nl-ethanol analog) predominated.

Keyphrases 0 14C-Flurazepam HCI metabolism-humans, dogs 0 Metabolites, flurazepam HCI-isolation, identification 0 Urinary, fecal excretion-14C-flurazepam 0 Plasma le~els-1~C-flurazepam 0 TLC-separation 0 UV spectrophotometry-analysis 0 Scintillometry-analysis