• Molecular NameClozapine
  • SynonymClozapin
  • Weight326.831
  • Drugbank_IDDB00363
  • ACS_NO5786-21-0
  • Show 3D model
  • LogP (experiment)3.32
  • LogP (predicted, AB/LogP v2.0)3.09
  • pka3.70, 7.60
  • LogD (pH=7, predicted)2.25
  • Solubility (experiment)Insoluble
  • LogS (predicted, ACD/Labs)(ph=7)-3.22
  • LogSw (predicted, AB/LogsW2.0)0.02
  • Sw (mg/ml) (predicted, ACD/Labs)0.04
  • No.of HBond Donors1
  • No.of HBond Acceptors4
  • No.of Rotatable Bonds1
  • TPSA30.87
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyAn antipsychotic medication used in the treatment of schizophrenia. The first of the atypical antipsychotics to be developed
  • Absorption_value100.0
  • Absorption (description)Rapid and almost complete
  • Caco_2N/A
  • Bioavailability55.0
  • Protein binding95.0
  • Volume of distribution (VD)5.4 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmHepatic, by several CYP isozymes. Clozapine undergoes a moderate first-pass metabolism and is almost completely metabolised before excretion via N-demethylation, N-oxidation, oxidation of the chlorine-containing ring, and thiomethyl conjugation. Metabolism is catalysed by cytochrome P450 isoenzyme CYP1A2. Only the desmethyl metabolite (norclozapine) shows any pharmacological actions but these are considerably weaker and of shorter duration than the parent drug.
  • Half life8 h (range 4-12 hours)
  • ExcretionOnly trace amounts of unchanged drug are detected in the urine and faeces. Approx. 50% of the administered dose are excreted as metabolites in the urine and 30% in the faeces.
  • Urinary Excretion<1
  • Clerance6.1 ml/min/kg
  • ToxicityAdverse events observed in association with the use of Clozapine in clinical trials at an incidence of greater than 5% were: central nervous system complaints, including drowsiness/sedation, dizziness/vertigo, headache and tremor; autonomic nervous system complaints, including salivation, sweating, dry mouth and visual disturbances; cardiovascular findings, including tachycardia, hypotension and syncope; gastrointestinal complaints, including constipation and nausea; fever.
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=160