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N-Desalkylflurazepam

Benzodiazepine analog From Wikipedia, the free encyclopedia

N-Desalkylflurazepam (also known as norflurazepam) is a benzodiazepine analog and an active metabolite of several other benzodiazepine drugs including flurazepam,[5] flutoprazepam,[6] fludiazepam,[7] midazolam,[8] flutazolam,[9] quazepam,[10] and ethyl loflazepate.[11][12] It is long-acting, prone to accumulation,[10][3] and binds unselectively to the various benzodiazepine receptor subtypes.[10] It has been sold as a designer drug from 2016 onward.[13]

Legal status
BioavailabilityPeak plasma concentration achieved within 90-120 minutes
Quick facts Clinical data, Routes ofadministration ...
N-Desalkylflurazepam
Clinical data
Routes of
administration
By mouth
Legal status
Legal status
Pharmacokinetic data
BioavailabilityPeak plasma concentration achieved within 90-120 minutes
MetabolismLiver
Elimination half-life47-150 hours[1] (~71hr avg)[2]
150-200 hours (under continuous administration)[3]
ExcretionKidney
Identifiers
  • 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.018.863 Edit this at Wikidata
Chemical and physical data
FormulaC15H10ClFN2O
Molar mass288.71 g·mol−1
3D model (JSmol)
Melting point205 to 206 °C (401 to 403 °F) [4]
  • Fc1ccccc1C2=NCC(=O)Nc3ccc(Cl)cc23
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Pharmacology

Pharmacokinetics

N-Desalkylflurazepam has an elimination half-life of 47–150 hours[1] (up to 200 hours in some healthy volunteers),[3] with an average of ~71 hours.[2] Peak blood concentrations of N-Desalkylflurazepam is reached at 10.2 h following a single 15 mg dose of Flurazepam, typically around ~10-20.4 ng/mL.[2][3]

Its plasma levels are unreliable amongst patients, and are largely influenced by liver disease, liver enzyme inducers and inhibitors, as well as old age (in men).[3]

References

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