azelastine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics | 271 | 58581-89-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.56 | mg | N |
| 4 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 1, 1996 | FDA | MEDA PHARMS |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Treatment failure | 403.68 | 15.17 | 252 | 10017 | 92835 | 46582958 |
| Sinusitis | 157.50 | 15.17 | 167 | 10102 | 129601 | 46546192 |
| Asthma | 82.33 | 15.17 | 101 | 10168 | 91441 | 46584352 |
| Headache | 45.91 | 15.17 | 217 | 10052 | 478135 | 46197658 |
| Product dose omission issue | 36.51 | 15.17 | 100 | 10169 | 168420 | 46507373 |
| Toxicity to various agents | 35.45 | 15.17 | 3 | 10266 | 211763 | 46464030 |
| Nasal discomfort | 35.33 | 15.17 | 17 | 10252 | 3721 | 46672072 |
| Infusion site swelling | 33.92 | 15.17 | 19 | 10250 | 5680 | 46670113 |
| Bronchitis | 33.76 | 15.17 | 73 | 10196 | 105906 | 46569887 |
| Infusion site erythema | 31.23 | 15.17 | 20 | 10249 | 7622 | 46668171 |
| Nasal congestion | 29.34 | 15.17 | 44 | 10225 | 48069 | 46627724 |
| Cough | 28.52 | 15.17 | 113 | 10156 | 230136 | 46445657 |
| Sinus disorder | 26.82 | 15.17 | 25 | 10244 | 16538 | 46659255 |
| Upper-airway cough syndrome | 25.94 | 15.17 | 18 | 10251 | 7829 | 46667964 |
| Ear infection | 24.98 | 15.17 | 28 | 10241 | 22985 | 46652808 |
| Ear discomfort | 23.51 | 15.17 | 16 | 10253 | 6745 | 46669048 |
| Sneezing | 20.18 | 15.17 | 19 | 10250 | 12722 | 46663071 |
| Pre-existing condition improved | 19.17 | 15.17 | 14 | 10255 | 6598 | 46669195 |
| Wheezing | 18.40 | 15.17 | 38 | 10231 | 53348 | 46622445 |
| Drug interaction | 16.95 | 15.17 | 12 | 10257 | 203082 | 46472711 |
| Rheumatoid arthritis | 16.62 | 15.17 | 17 | 10252 | 240198 | 46435595 |
| General physical health deterioration | 16.07 | 15.17 | 3 | 10266 | 115766 | 46560027 |
| Sleep apnoea syndrome | 16.01 | 15.17 | 22 | 10247 | 22179 | 46653614 |
| Product taste abnormal | 15.79 | 15.17 | 8 | 10261 | 1955 | 46673838 |
| Multiple allergies | 15.69 | 15.17 | 13 | 10256 | 7358 | 46668435 |
| Fatigue | 15.61 | 15.17 | 203 | 10066 | 608494 | 46067299 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Treatment failure | 262.43 | 18.23 | 116 | 3933 | 34563 | 29913866 |
| Sinusitis | 51.99 | 18.23 | 40 | 4009 | 33305 | 29915124 |
| Transferrin increased | 36.08 | 18.23 | 5 | 4044 | 5 | 29948424 |
| Chorioretinopathy | 33.50 | 18.23 | 11 | 4038 | 1441 | 29946988 |
| Oesophageal injury | 31.12 | 18.23 | 5 | 4044 | 22 | 29948407 |
| Amaurosis fugax | 24.61 | 18.23 | 7 | 4042 | 566 | 29947863 |
| Headache | 19.10 | 18.23 | 61 | 3988 | 182245 | 29766184 |
| Merycism | 18.90 | 18.23 | 3 | 4046 | 12 | 29948417 |
| Eosinophilic granulomatosis with polyangiitis | 18.90 | 18.23 | 7 | 4042 | 1308 | 29947121 |
| Oesophageal ulcer | 18.56 | 18.23 | 9 | 4040 | 3268 | 29945161 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 agents |
| CHEBI has role | CHEBI:37955 | h1-receptor blockers |
| CHEBI has role | CHEBI:49167 | anti-asthmatic agents |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitors |
| CHEBI has role | CHEBI:50857 | anti-allergic agents |
| CHEBI has role | CHEBI:64964 | 5-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 (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.91 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 8.17 | WOMBAT-PK | CHEMBL | |||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7.30 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 7.30 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 7 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 6.83 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| ZQI909440X | UNII |
| 4024042 | VUID |
| N0000022047 | NUI |
| D00659 | KEGG_DRUG |
| 79307-93-0 | SECONDARY_CAS_RN |
| 4021001 | VANDF |
| 4024042 | VANDF |
| C0052762 | UMLSCUI |
| CHEBI:2951 | CHEBI |
| CHEMBL639 | ChEMBL_ID |
| CHEMBL1200809 | ChEMBL_ID |
| DB00972 | DRUGBANK_ID |
| 2267 | PUBCHEM_CID |
| 4074 | INN_ID |
| C020976 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7121 | IUPHAR_LIGAND_ID |
| 18603 | RXNORM |
| 169403 | MMSL |
| 4237 | MMSL |
| 8899 | MMSL |
| 003931 | NDDF |
| 003932 | NDDF |
| 108644000 | SNOMEDCT_US |
| 108646003 | SNOMEDCT_US |
| 372520005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| DYMISTA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0037-0245 | SPRAY, METERED | 137 ug | NULLSAL | NDA | 28 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0293 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 27 sections |
| Azelastine Hydrochloride and Fluticasone Propionate | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0378-3458 | SPRAY, METERED | 137 ug | NULLSAL | 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 | NULLSAL | ANDA | 27 sections |
| azelastine hcl nasal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 45802-026 | SPRAY | 205.50 ug | NULLSAL | ANDA | 27 sections |
| AZELASTINE HYDROCHLORIDE AND FLUTICASONE PROPIONULLTE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 45802-066 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 26 sections |
| Azelastine Hydrochloride | Human Prescription Drug Label | 1 | 47335-779 | SPRAY, METERED | 137 ug | NULLSAL | 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 | NULLSAL | ANDA | 19 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3833 | SPRAY, METERED | 1 mg | NULLSAL | ANDA | 27 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50383-738 | SPRAY, METERED | 1 mg | NULLSAL | ANDA | 25 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50383-942 | SPRAY, METERED | 1.50 mg | NULLSAL | ANDA | 25 sections |
| AZELASTINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51991-814 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 28 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53002-1279 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 19 sections |
| Astelin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5072 | SPRAY, METERED | 137 ug | NULLSAL | NDA | 22 sections |
| Azelastine Hydrochloride | Human prescription drug label | 1 | 54868-6131 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 19 sections |
| AZELASTINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 59651-214 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 26 sections |
| AZELASTINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 59651-215 | SPRAY, METERED | 205.50 ug | NULLSAL | 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 | NULLSAL | ANDA | 19 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-0848 | SPRAY, METERED | 205.50 ug | NULLSAL | ANDA | 26 sections |
| Azelastine hydrochloride and Fluticasone propionate | HUMAN PRESCRIPTION DRUG LABEL | 2 | 60505-0953 | SPRAY, METERED | 137 ug | NULLSAL | 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 | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2057 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 27 sections |
| azelastine hcl nasal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2519 | SPRAY | 205.50 ug | NULLSAL | ANDA | 27 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-676 | SPRAY, METERED | 1 mg | NULLSAL | ANDA | 27 sections |
| Azelastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-706 | SPRAY, METERED | 205.50 ug | NULLSAL | ANDA | 19 sections |
| Azelastine | Human Prescription Drug Label | 1 | 67877-477 | SPRAY, METERED | 137 ug | NULLSAL | ANDA | 25 sections |