• Molecular NameFlurazepam
  • SynonymFlurazepam HCL
  • Weight387.886
  • Drugbank_IDDB00690
  • ACS_NO17617-23-1
  • Show 3D model
  • LogP (experiment)3.94
  • LogP (predicted, AB/LogP v2.0)3.57
  • pka1.9, 8.2
  • LogD (pH=7, predicted)2.01
  • Solubility (experiment)N/A
  • LogS (predicted, ACD/Labs)(ph=7)-2.09
  • LogSw (predicted, AB/LogsW2.0)0.04
  • Sw (mg/ml) (predicted, ACD/Labs)0.02
  • No.of HBond Donors0
  • No.of HBond Acceptors4
  • No.of Rotatable Bonds6
  • TPSA35.91
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties.
  • Absorption_value100.0
  • Absorption (description)Readily absorbed after oral administration
  • Caco_2N/A
  • Bioavailability83.0
  • Protein binding96.6
  • Volume of distribution (VD)N/A
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmAbout 70% of a dose is metabolised during the first pass through the liver. The major metabolites in blood are N1-desalkylflurazepam and N1-(2-hydroxyethyl)flurazepam which are both pharmacologically active and accumulate on daily administration; 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2-oxo-2H-1,4-benzodiazepin-1-acetaldehyde has also been detected in plasma. Other active metabolites found in urine include monodesethyl- and didesethylflurazepam and N1-desalkyl-3-hydroxyflurazepam, but these are not detectable in blood.
  • Half lifeflurazepam 2~3 h, N1-desalkylflurazepam 2 to 5 days, N1-(2-hydroxyethyl)flurazepam 10 to 20 h.
  • ExcretionUp to 60% of a dose may be excreted in the urine in 48 h, with about 40% of the dose as a glucuronide/sulfate conjugate of N1-(2-hydroxyethyl)flurazepam and about 4% as conjugated N1-desalkyl-3-hydroxyflurazepam and conjugated flurazepam-N1-ylacetic acid; only trace amounts of unchanged flurazepam and the unconjugated metabolites are present. N1-(Hydroxyethyl)-3-hydroxyflurazepam has also been detected. About 9% of a dose is eliminated in the faeces.
  • Urinary ExcretionN/A
  • CleranceN/A
  • ToxicityBlood concentrations greater than 0.2 mg/L of flurazepam or 0.5 mg/L of N1-desalkylflurazepam may be toxic, and blood concentrations greater than 0.5 mg/L of flurazepam may be fatal.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A