• Molecular NameAzelastine
  • SynonymAzelastina [INN-Spanish]; Azelastine Hydrochloride; Azelastinum [INN-Latin]
  • Weight383.923
  • Drugbank_IDDB00972
  • ACS_NO58581-89-8
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  • LogP (experiment)4.961
  • LogP (predicted, AB/LogP v2.0)4.03
  • pka9.54
  • LogD (pH=7, predicted)1.97
  • Solubility (experiment)N/A
  • LogS (predicted, ACD/Labs)(ph=7)-2.27
  • LogSw (predicted, AB/LogsW2.0)0.02
  • Sw (mg/ml) (predicted, ACD/Labs)0.02
  • No.of HBond Donors1
  • No.of HBond Acceptors4
  • No.of Rotatable Bonds3
  • TPSA35.58
  • StatusFDA approved
  • AdministrationIntranasal, ocular
  • PharmacologyAn antihistamine and mast cell stabilizer available as a nasal spray (Astelin or Astepro) for hay fever and as eye drops (Optivar) for allergic conjunctivitis.
  • Absorption_valueN/A
  • Absorption (description)Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
  • Caco_2N/A
  • BioavailabilityN/A
  • Protein binding88.0
  • Volume of distribution (VD)15
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmAzelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.
  • Half life22 h
  • ExcretionN/A
  • Urinary ExcretionN/A
  • CleranceN/A
  • ToxicityN/A
  • LD50 (rat)N/A
  • LD50 (mouse)N/A