• Molecular NameFlunitrazepam
  • SynonymFlunitrazepamum [inn-latin]
  • Weight313.288
  • Drugbank_IDDB01544
  • ACS_NO1622-62-4
  • Show 2D model
  • LogP (experiment)2.1
  • LogP (predicted, AB/LogP v2.0)2.2
  • pka1.8
  • LogD (pH=7, predicted)2.2
  • Solubility (experiment)N/A
  • LogS (predicted, ACD/Labs)(ph=7)-3.88
  • LogSw (predicted, AB/LogsW2.0)0.06
  • Sw (mg/ml) (predicted, ACD/Labs)0.04
  • No.of HBond Donors0
  • No.of HBond Acceptors6
  • No.of Rotatable Bonds2
  • TPSA81.5
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA hypnotic drug and has sedative, anticonvulsant, anxiolytic, amnestic, hypnotic and skeletal muscle relaxant properties.
  • Absorption_valueN/A
  • Absorption (description)Readily absorbed after oral administration.
  • Caco_2N/A
  • Bioavailability80.0
  • Protein binding78.0
  • Volume of distribution (VD)3.5~5.5 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, about 0.75.
  • MetabollsmIt is extensively metabolised in the liver to desmethylflunitrazepam, which has some activity, and 7-aminoflunitrazepam, which is inactive; other metabolites include 3-hydroxyflunitrazepam, 3-hydroxy-7-acetamidoflunitrazepam, and 7-amino-1-desmethylflunitrazepam. Flunitrazepam is excreted in the urine almost entirely as metabolites, both free and conjugated, with less than 1% as unchanged drug.
  • Half life3 h (distribution); 16 to 35 h (elimination).
  • ExcretionAbout 10% of a dose is eliminated in the faeces. Flunitrazepam crosses the placental barrier and it is excreted in breast milk.
  • Urinary ExcretionN/A
  • Clerance2 ml/min/kg
  • ToxicityOf 8 deaths involving flunitrazepam, 4 had 7-aminoflunitrazepam levels of 0.45 mg/L (where the fatality involved flunitrazepam alone) and 4 had 7-aminoflunitrazepam levels of 0.16 mg/L (where the fatality involved flunitrazepam and ethanol); in the latter group the mean ethanol concentration was 1600 mg/L. Levels of flunitrazepam were low, suggesting that 7-aminoflunitrazepam was produced postmortem [O. H. Drummer et al.,Am. J. Forensic Med. Pathol.,1993, 14, 238–243.]
  • LD50 (rat)N/A
  • LD50 (mouse)N/A