• Molecular NameFlumazenil
  • SynonymFlumazenilo [Spanish]; Flumazenilum [Latin]
  • Weight303.293
  • Drugbank_IDDB01205
  • ACS_NO78755-81-4
  • Show 2D model
  • LogP (experiment)0.78
  • LogP (predicted, AB/LogP v2.0)0.64
  • pka1.8
  • LogD (pH=7, predicted)0.64
  • Solubility (experiment)0.128 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)-2.99
  • LogSw (predicted, AB/LogsW2.0)1.27
  • Sw (mg/ml) (predicted, ACD/Labs)0.31
  • No.of HBond Donors0
  • No.of HBond Acceptors6
  • No.of Rotatable Bonds3
  • TPSA63.91
  • StatusFDA approved
  • AdministrationIntravenously normally
  • PharmacologyA benzodiazepine antagonist.
  • Absorption_value95.0
  • Absorption (description)Flumazenil is rapidly and well absorbed after oral administration
  • Caco_2N/A
  • Bioavailability16.0
  • Protein binding40.0
  • Volume of distribution (VD)0.63 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)Blood:plasma ratio is 0.8 to 1.3.
  • Metabollsmundergoes extensive first-pass hepatic metabolism. It is therefore given by intravenous administration. It is rapidly distributed into the brain. Flumazenil is extensively metabolised in the liver to an inactive carboxylic acid form and excreted predominantly in urine (less than 1% is excreted unchanged). Metabolites include N-desmethylflumazenil, N-desmethylflumazenil acid and flumazenil acid.
  • Half life0.9 h
  • Excretionurine (less than 1% is excreted unchanged). Some (5 to 10%) is excreted via bile in faeces.
  • Urinary Excretion<0.2
  • Clerance9.9 ml/min/kg
  • ToxicityIn clinical studies, most adverse reactions to flumazenil were an extension of the pharmacologic effects of the drug in reversing benzodiazepine effects.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A