Fosazepam

Source: Wikipedia, the free encyclopedia.
Fosazepam
Clinical data
ATC code
  • none
Identifiers
  • 7-chloro-1-(dimethylphosphorylmethyl)-5-phenyl-3H-1,4-benzodiazepin-2-one
JSmol)
  • ClC1=CC2=C(C=C1)N(CP(C)(C)=O)C(CN=C2C3=CC=CC=C3)=O
  • InChI=1S/C18H18ClN2O2P/c1-24(2,23)12-21-16-9-8-14(19)10-15(16)18(20-11-17(21)22)13-6-4-3-5-7-13/h3-10H,11-12H2,1-2H3 checkY
  • Key:JMYCGCXYZZHWMO-UHFFFAOYSA-N checkY
  (verify)

Fosazepam

water soluble derivative of diazepam.[2] It has sedative and anxiolytic effects,[3] and is a derivative of diazepam which has been substituted with a dimethylphosphoryl group to improve solubility in water.[4]

Fosazepam has similar effects on sleep as other benzodiazepines. In a clinical trial it was reported that fosazepam to lead to increased sleep duration with less broken sleep but sleep quality was worsened with suppressed deep sleep and increased light sleep. Adverse effects included feelings of impaired morning vitality and upon discontinuing the drug

nordiazepam (desmethyldiazepam), rather than the parent drug.[8] The long-acting active metabolite nordazepam can cause extended sedative effects at high doses or with prolonged use, and may produce residual sedation upon awakening.[7]

Fosazepam is of relatively low potency compared to other benzodiazepine derivatives, with a 100 mg dose of fosazepam equivalent to 10 mg of nitrazepam.[5] 60 mg of fosazepam has also been estimated to be equivalent to about 5–10 mg of diazepam.[2] Fosazepam has similar effects to nitrazepam, but with a shorter duration of action and less tendency to cause over sedation, motor-impairment, amnesia, rebound insomnia, and morning grogginess.[9]

See also

References

  1. ^ DE Patent 2022503
  2. ^
    PMID 1201402
    .
  3. ^
    PMID 184806
    .
  4. PMID 409424
    .
  5. ^
    S2CID 21051544
    .
  6. S2CID 23137060
    .
  7. ^
    PMID 6106488
    .
  8. PMID 409424
    .
  9. S2CID 23137060
    .
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