azelastine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics 271 58581-89-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • azelastine
  • azelastine hydrochloride
  • azelastine HCl
Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine Hydrochloride is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity.
  • Molecular weight: 381.90
  • Formula: C22H24ClN3O
  • CLOGP: 4.01
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 35.91
  • ALOGS: -4.62
  • ROTB: 3

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.56 mg N
4 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.30 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 15 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.17 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 22 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 1, 1996 FDA MEDA PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 339.96 15.22 252 9696 137385 50457791
Sinusitis 143.74 15.22 172 9776 170386 50424790
Product dose omission issue 59.31 15.22 119 9829 183719 50411457
Asthma 59.06 15.22 80 9868 89257 50505919
Infusion site swelling 45.45 15.22 24 9924 7152 50588024
Headache 44.65 15.22 207 9741 506328 50088848
Infusion site erythema 43.72 15.22 25 9923 8702 50586474
Bronchitis 33.01 15.22 67 9881 104092 50491084
Toxicity to various agents 30.95 15.22 3 9945 212496 50382680
Sinus disorder 30.85 15.22 27 9921 18431 50576745
Cough 30.17 15.22 110 9838 241154 50354022
Infusion site extravasation 27.18 15.22 17 9931 6959 50588217
COVID-19 23.82 15.22 37 9911 46625 50548551
Infusion site pain 22.54 15.22 19 9929 12327 50582849
Pre-existing condition improved 22.03 15.22 15 9933 7082 50588094
Multiple allergies 21.89 15.22 16 9932 8447 50586729
Nasal discomfort 21.77 15.22 12 9936 3892 50591284
Infusion site pruritus 21.67 15.22 12 9936 3925 50591251
Fatigue 20.29 15.22 220 9728 707381 49887795
Infusion site haemorrhage 18.89 15.22 10 9938 2994 50592182
Systemic lupus erythematosus 18.01 15.22 3 9945 140619 50454557
Product quality issue 17.93 15.22 26 9922 30832 50564344
Product taste abnormal 17.54 15.22 8 9940 1737 50593439
Hepatic enzyme increased 17.44 15.22 3 9945 137377 50457799
Upper respiratory tract infection 16.97 15.22 39 9909 65859 50529317
Ear infection 16.74 15.22 23 9925 25947 50569229
Sleep apnoea syndrome 16.70 15.22 22 9926 23846 50571330
Therapy interrupted 16.36 15.22 20 9928 20132 50575044
Nasal congestion 16.31 15.22 33 9915 51087 50544089
General physical health deterioration 16.25 15.22 4 9944 142430 50452746
Drug intolerance 15.79 15.22 12 9936 219092 50376084
Upper-airway cough syndrome 15.28 15.22 13 9935 8537 50586639
Choroidal effusion 15.22 15.22 5 9943 449 50594727

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Treatment failure 250.98 18.87 116 4043 36823 29533545
Sinusitis 69.59 18.87 49 4110 34301 29536067
Transferrin increased 35.89 18.87 5 4154 5 29570363
Chorioretinopathy 33.34 18.87 11 4148 1405 29568963
Oesophageal injury 30.40 18.87 5 4154 25 29570343

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sinusitis 81.25 14.78 106 9826 145822 64342978
Asthma 49.60 14.78 67 9865 95158 64393642
Product dose omission issue 47.08 14.78 97 9835 194650 64294150
Headache 44.58 14.78 180 9752 529287 63959513
Toxicity to various agents 44.34 14.78 3 9929 363510 64125290
Fatigue 31.67 14.78 210 9722 748520 63740280
Transferrin increased 29.94 14.78 5 9927 25 64488775
Chorioretinopathy 27.64 14.78 11 9921 2186 64486614
Cough 25.54 14.78 103 9829 302045 64186755
Oesophageal injury 25.17 14.78 5 9927 73 64488727
Product quality issue 23.71 14.78 26 9906 29773 64459027
Infusion site erythema 23.22 14.78 14 9918 6859 64481941
Bronchitis 22.60 14.78 51 9881 108692 64380108
General physical health deterioration 21.47 14.78 3 9929 204422 64284378
Sinus disorder 21.38 14.78 19 9913 16889 64471911
Infusion site swelling 20.74 14.78 12 9920 5453 64483347
Acute respiratory failure 19.94 14.78 31 9901 49903 64438897
Upper-airway cough syndrome 17.80 14.78 13 9919 8757 64480043
Therapy interrupted 16.84 14.78 18 9914 20018 64468782
Nasal operation 16.07 14.78 4 9928 169 64488631
Dermatitis atopic 16.02 14.78 9 9923 3867 64484933
Infusion site pain 15.83 14.78 13 9919 10384 64478416
Flushing 15.36 14.78 36 9896 78612 64410188
Drug interaction 15.32 14.78 20 9912 362063 64126737
Psoriasis 15.31 14.78 34 9898 71669 64417131
Dyspnoea 15.16 14.78 173 9759 718501 63770299
Nasal discomfort 15.10 14.78 9 9923 4319 64484481
Choroidal effusion 14.95 14.78 5 9927 607 64488193

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R01AC03 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Antiallergic agents, excl. corticosteroids
ATC R06AX19 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
ATC S01GX07 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Other antiallergics
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
CHEBI has role CHEBI:35523 bronchodilator
CHEBI has role CHEBI:37955 H1 receptor antagonists
CHEBI has role CHEBI:49167 anti-asthmatic drugs
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:50857 anti-allergic drugs
CHEBI has role CHEBI:64964 5delta-lipoxygenase inhibitor
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
MeSH PA D016859 Lipoxygenase Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Vasomotor rhinitis indication 8229003 DOID:4730
Allergic rhinitis indication 61582004
Seasonal allergic rhinitis indication 367498001
Allergic conjunctivitis indication 473460002 DOID:11204
Kidney disease contraindication 90708001 DOID:557
Drowsy contraindication 271782001
Ocular Irritation contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.91 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 9259428 June 13, 2023 TREATMENT OF SEASONAL ALLERGIC RHINITIS
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 8163723 Aug. 29, 2023 ALLERGIC RHINITIS
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 8163723 Aug. 29, 2023 RELIEF OF SYMPTOMS ASSOCIATED WITH SEASONAL ALLERGIC RHINITIS
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 8163723 Aug. 29, 2023 TREATMENT OF ALLERGIC RHINITIS, INCLUDING SEASONAL ALLERGIC RHINITIS
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 8163723 Aug. 29, 2023 TREATMENT OF SEASONAL ALLERGIC RHINITIS
0.137MG/SPRAY;0.05MG/SPRAY DYMISTA MYLAN SPECIALITY LP N202236 May 1, 2012 RX SPRAY, METERED NASAL 8163723 Aug. 29, 2023 TREATMENT OF SYMPTOMS OF SEASONAL ALLERGIC RHINITIS
0.137MG/SPRAY ASTEPRO MYLAN SPECIALITY LP N022203 Oct. 15, 2008 DISCN SPRAY, METERED NASAL 8518919 Nov. 22, 2025 TREATMENT OF ALLERGIC RHINITIS, INCLUDING SEASONAL AND PERENNIAL ALLERGIC RHINITIS
0.2055MG/SPRAY ASTEPRO MYLAN SPECIALITY LP N022203 Aug. 31, 2009 DISCN SPRAY, METERED NASAL 8518919 Nov. 22, 2025 TREATMENT OF ALLERGIC RHINITIS, INCLUDING SEASONAL AND PERENNIAL ALLERGIC RHINITIS
0.2055MG/SPRAY ASTEPRO ALLERGY BAYER HLTHCARE N213872 June 17, 2021 OTC SPRAY, METERED NASAL 8518919 Nov. 22, 2025 OTC USE: ALLERGY SYMPTOM RELIEVER; TEMPORARY RELIEF OF THESE SYMPTOMS DUE TO HAY FEVER OR OTHER UPPER RESPIRATORY ALLERGIES: NASAL CONGESTION, RUNNY NOSE, SNEEZING AND ITCHY NOSE
0.2055MG/SPRAY CHILDRENS ASTEPRO ALLERGY BAYER HLTHCARE N213872 June 17, 2021 OTC SPRAY, METERED NASAL 8518919 Nov. 22, 2025 OTC USE: ALLERGY SYMPTOM RELIEVER; TEMPORARY RELIEF OF THESE SYMPTOMS DUE TO HAY FEVER OR OTHER UPPER RESPIRATORY ALLERGIES: NASAL CONGESTION, RUNNY NOSE, SNEEZING AND ITCHY NOSE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 8.17 WOMBAT-PK CHEMBL
Multidrug resistance protein 1 Transporter WOMBAT-PK
5-hydroxytryptamine receptor 2B GPCR Ki 7.70 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 6.30 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.30 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR IC50 5.20 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 7.30 CHEMBL
Histamine H3 receptor GPCR Ki 6.83 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.30 CHEMBL

External reference:

IDSource
4024042 VUID
N0000022047 NUI
D00659 KEGG_DRUG
79307-93-0 SECONDARY_CAS_RN
18603 RXNORM
C0052762 UMLSCUI
CHEBI:2951 CHEBI
CHEMBL639 ChEMBL_ID
DB00972 DRUGBANK_ID
CHEMBL1200809 ChEMBL_ID
C020976 MESH_SUPPLEMENTAL_RECORD_UI
2267 PUBCHEM_CID
7121 IUPHAR_LIGAND_ID
4074 INN_ID
ZQI909440X UNII
169403 MMSL
4237 MMSL
8899 MMSL
003931 NDDF
003932 NDDF
4021001 VANDF
4024042 VANDF
108644000 SNOMEDCT_US
108646003 SNOMEDCT_US
372520005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DYMISTA HUMAN PRESCRIPTION DRUG LABEL 2 0037-0245 SPRAY, METERED 137 ug NASAL NDA 28 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0293 SPRAY, METERED 137 ug NASAL ANDA 27 sections
Azelastine Hydrochloride and Fluticasone Propionate HUMAN PRESCRIPTION DRUG LABEL 2 0378-3458 SPRAY, METERED 137 ug NASAL NDA authorized generic 29 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-718 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 10 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-094 SPRAY, METERED 1 mg NASAL ANDA 27 sections
azelastine hcl nasal HUMAN PRESCRIPTION DRUG LABEL 1 45802-026 SPRAY 205.50 ug NASAL ANDA 27 sections
AZELASTINE HYDROCHLORIDE AND FLUTICASONE PROPIONATE HUMAN PRESCRIPTION DRUG LABEL 2 45802-066 SPRAY, METERED 137 ug NASAL ANDA 28 sections
AZELASTINE HYDROCHLORIDE AND FLUTICASONE PROPIONATE HUMAN PRESCRIPTION DRUG LABEL 2 45802-066 SPRAY, METERED 137 ug NASAL ANDA 28 sections
Azelastine Hydrochloride Human Prescription Drug Label 1 47335-779 SPRAY, METERED 137 ug NASAL ANDA 25 sections
Azelastine Hydrochloride Human Prescription Drug Label 1 47335-938 SOLUTION/ DROPS 0.50 mg INTRAOCULAR ANDA 17 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-2330 SPRAY, METERED 137 ug NASAL ANDA 19 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-3833 SPRAY, METERED 1 mg NASAL ANDA 27 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50383-738 SPRAY, METERED 1 mg NASAL ANDA 25 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50383-942 SPRAY, METERED 1.50 mg NASAL ANDA 25 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50383-942 SPRAY, METERED 1.50 mg NASAL ANDA 25 sections
AZELASTINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51991-814 SPRAY, METERED 137 ug NASAL ANDA 28 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 53002-1279 SPRAY, METERED 137 ug NASAL ANDA 19 sections
Azelastine Hydrochloride Human Prescription Drug Label 1 53002-2279 SPRAY, METERED 137 ug NASAL ANDA 25 sections
Astelin HUMAN PRESCRIPTION DRUG LABEL 1 54868-5072 SPRAY, METERED 137 ug NASAL NDA 22 sections
Azelastine Hydrochloride Human prescription drug label 1 54868-6131 SPRAY, METERED 137 ug NASAL ANDA 19 sections
AZELASTINE HYDROCHLORIDE Human Prescription Drug Label 1 59651-214 SPRAY, METERED 137 ug NASAL ANDA 26 sections
AZELASTINE HYDROCHLORIDE Human Prescription Drug Label 1 59651-214 SPRAY, METERED 137 ug NASAL ANDA 26 sections
AZELASTINE HYDROCHLORIDE Human Prescription Drug Label 1 59651-215 SPRAY, METERED 205.50 ug NASAL ANDA 26 sections
AZELASTINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 60505-0578 SOLUTION/ DROPS 0.50 mg INTRAOCULAR ANDA 17 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60505-0833 SPRAY, METERED 137 ug NASAL ANDA 19 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60505-0848 SPRAY, METERED 205.50 ug NASAL ANDA 26 sections
Azelastine hydrochloride and Fluticasone propionate HUMAN PRESCRIPTION DRUG LABEL 2 60505-0953 SPRAY, METERED 137 ug NASAL ANDA 27 sections
Azelastine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61314-308 SOLUTION/ DROPS 0.50 mg INTRAOCULAR ANDA 16 sections
Azelastine Hydrochloride Ophthalmic Solution 0.05% Human Prescription Drug Label 1 62332-506 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 16 sections
Azelastine Hydrochloride Ophthalmic Solution 0.05% Human Prescription Drug Label 1 62332-506 SOLUTION/ DROPS 0.50 mg OPHTHALMIC ANDA 16 sections