Flurazepamの生体内運命 その2 Flurazepamの代謝

西川 隆, 峯浦 和幸, 高平 汎志

doi:10.1248/yakushi1947.93.2_232

The metabolic fate of Flurazepam hydrochloride, 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one monohydrochloride, having a sleep-inducing effect, was examined in a rat after oral administration of this compound labeled with ¹⁴C at the C-5 position. Radioactive metabolites in bile and urine were fractionated to be identified. Less than 3% of the bilary ¹⁴C could be extracted with ethyl acetate at pH 9.0 and no appreciable amount of intact Flurazepam was detected in this extract. In bilary metabolites, N-dealkylated compounds (>NCH₂CH₂NHC₂H₅, >NCH₂CH₂NH₂), thier conjugates, and the conjugate of N₁-ethanol (>NCH₂CH₂OH) were found. In urinary metabolites, N₁-acetic acid (>NCH₂COOH) was found in addition to the bilary metabolites. One of major metabolites in both bile and urine remained unidentified, but it was evident that this unidentified metabolite was soluble in water, had no acidic group, kept a benzodiazepine ring structure, and had an N₁-aminoethyl group (>NCH₂CH₂N<). From these results, the pathway of Flurazepam in rat was postulated as shown in Chart 4.

Flurazepamの生体内運命その2 Flurazepamの代謝

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