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Substance Name: Azelastine hydrochloride [USAN:JAN]
RN: 79307-93-0
UNII: 0L591QR10I
InChIKey: YEJAJYAHJQIWNU-UHFFFAOYSA-N

Note

  • Azeptin is azelastine hydrochloride; eye drop formulation effective in relieving symptoms of allergic conjunctivitis.

Molecular Formula

  • C22-H24-Cl-N3-O.Cl-H

Molecular Weight

  • 418.366
 

Classification Codes

  • Anti-Allergic
  • Anti-Allergic Agents
  • Anti-Asthmatic
  • Bronchodilator Agents
  • Drug / Therapeutic Agent
  • Histamine H1 Antagonists, Non-Sedating
  • Lipoxygenase Inhibitors
  • Reproductive Effect

Names and Synonyms

Name of Substance

  • Azelastine hydrochloride [USAN:JAN]

Synonyms

  • 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride
  • 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone monohydrochloride
  • A 5610
  • A-5610
  • Allergodil
  • Astelin
  • Astepro
  • Azelastine HCl
  • Azelastine hydrochloride
  • Azeptin
  • E-0659
  • Optivar
  • Rhinolast
  • UNII-0L591QR10I
  • W- 979M
  • W-2979M
  • Zalastine

Systematic Name

  • 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride

Registry Numbers

CAS Registry Number

  • 79307-93-0

FDA UNII

  • 0L591QR10I

Related Registry Number

  • 58581-89-8 (Parent)

System Generated Number

  • 0079307930

Molecular Formulas

Molecular Formula

  • C22-H24-Cl-N3-O.Cl-H

Molecular Formula Fragments

  • C22-H24-Cl-N3-O
  • Cl-H
  • COMPONENT

Structure Descriptors

InChI

1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H

InChIKey

YEJAJYAHJQIWNU-UHFFFAOYSA-N

Smiles

c12c(nn([C@@H]3CCC[N@@](CC3)C)c(c1cccc2)=O)Cc1ccc(Cl)cc1.Cl

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
dog LD50 oral 107mg/kg (107mg/kg) GASTROINTESTINAL: NAUSEA OR VOMITING

BEHAVIORAL: ATAXIA

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5235, 1986.
guinea pig LD50 intramuscular 46200ug/kg (46.2mg/kg) BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
guinea pig LD50 intravenous 23mg/kg (23mg/kg) BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
guinea pig LD50 oral 126mg/kg (126mg/kg) BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
guinea pig LD50 subcutaneous 37300ug/kg (37.3mg/kg) BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
mouse LD50 intramuscular 57200ug/kg (57.2mg/kg) BEHAVIORAL: ATAXIA

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
mouse LD50 intravenous 25400ug/kg (25.4mg/kg) BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
mouse LD50 oral 143mg/kg (143mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
mouse LD50 subcutaneous 59600ug/kg (59.6mg/kg) GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS

BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
rat LD50 intramuscular 115mg/kg (115mg/kg) BEHAVIORAL: TREMOR

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
rat LD50 intravenous 24600ug/kg (24.6mg/kg) BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
rat LD50 oral 580mg/kg (580mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: TREMOR

BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.
rat LD50 subcutaneous 80500ug/kg (80.5mg/kg) BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX)

BEHAVIORAL: TREMOR

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Kiso to Rinsho. Clinical Report. Vol. 20, Pg. 5231, 1986.