• Molecular NameDiazepam
  • SynonymDAP; Methyldiazepinon
  • Weight284.746
  • Drugbank_IDDB00829
  • ACS_NO439-14-5
  • Show 3D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)2.87
  • pka3.3
  • LogD (pH=7, predicted)2.87
  • Solubility (experiment)0.05 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)-3.83
  • LogSw (predicted, AB/LogsW2.0)0.04
  • Sw (mg/ml) (predicted, ACD/Labs)0.04
  • No.of HBond Donors0
  • No.of HBond Acceptors3
  • No.of Rotatable Bonds1
  • TPSA32.67
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA benzodiazepine derivative drug. It is commonly used for treating anxiety, insomnia, seizures, muscle spasms, restless legs syndrome, alcohol withdrawal, benzodiazepine withdrawal, and Ménière's disease. It may also be used before certain medical procedures (such as endoscopies) to reduce tension and anxiety, and in some surgical procedures to induce amnesia.
  • Absorption_value99.0
  • Absorption (description)Rapidly and completely absorbed after oral administration, with peak plasma levels occurring within about 30 to 90 min.
  • Caco_2-4.32
  • Bioavailability93.0
  • Protein binding98.7
  • Volume of distribution (VD)Diazepam and desmethyldiazepam 1.1 to 2.5 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)Plasma:whole blood ratio, diazepam 1.8, desmethyldiazepam 1.7.
  • MetabollsmActive metabolites, desmethyldiazepam and oxazepam, formed by CYP2C19 (polymorphic) and CYP3A
  • Half lifediazepam 43 h, desmethyldiazepam about 40~100 h but there is considerable intersubject variation
  • ExcretionOnly small traces of unchanged diazepam are excreted in the urine and the relative amounts of metabolites are variable and appear to be dose-dependent. About 70% of a dose is excreted in the urine, mainly as oxazepam glucuronide and conjugated desmethyldiazepam, together with smaller amounts of conjugated temazepam. About 10% of the dose may be eliminated in the faeces. Diazepam and its metabolites cross the blood–brain barrier and the placeta; they are also found in breast milk. Diazepam is a metabolite of ketazolam and medazepam.
  • Urinary Excretion<1
  • Clerance0.38 ml/min/kg, desmethyldiazepam about 0.1~0.3 ml/min/kg
  • ToxicitySymptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=1386