• Molecular NameCilazapril
  • SynonymInhibace
  • Weight417.506
  • Drugbank_IDDB01340
  • ACS_NO92077-78-6
  • Show 3D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)-0.17
  • pkaN/A
  • LogD (pH=7, predicted)-3.57
  • Solubility (experiment)5.02 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)-1.48
  • LogSw (predicted, AB/LogsW2.0)25.67
  • Sw (mg/ml) (predicted, ACD/Labs)0.35
  • No.of HBond Donors2
  • No.of HBond Acceptors8
  • No.of Rotatable Bonds9
  • TPSA99.18
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure.
  • Absorption_value59.0
  • Absorption (description)After oral administration and rapid absorption; The absolute bioavailability of cilazaprilat after oral administration of cilazapril is 57% based on urinary recovery data.
  • Caco_2N/A
  • Bioavailability60.0
  • Protein binding24.0
  • Volume of distribution (VD)29 to 46 L
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • Metabollsmcilazapril is hydrolysed in the liver to its diacid, cilazaprilate (active ACE inhibitor), and no further metabolism occurs.
  • Half lifeInitial half-life of 1.3 to 1.8 h and a terminal phase elimination half-life of 40 to 50 h for cilazaprilate. Effective half-life (steady state reached) is approx. 9 h.
  • ExcretionExcretion is biphasic and occurs almost exclusively in the kidneys with approx. 53% cilazaprilate being recovered in urine after oral administration of cilazapril. Rapid elimination of cilazaprilate occurs with unbound drug eliminated within 8 h. Both cilazapril and cilazaprilate are removed to a limited extent by haemodialysis.
  • Urinary ExcretionN/A
  • Clerancecilazaprilate is 14~24 L/h, after a single oral dose of 2.5 to 10 mg cilazapril, and in patients with moderate essential hypertension clearance is 14~16 L/h, after a single oral dose of 5 to 20 mg.
  • ToxicitySkin rashes and allergies have been noted in women administered the low toxic dose of 15 mg/kg at 22 week intervals. It is a poison by intravenous routes and moderately toxic by subcutaneous and intraperitoneal routes.
  • LD50 (rat)> 4 g/kg (rats, marmosets)
  • LD50 (mouse)Oral LD50 >2.5 g/kg