Stem definition | Drug id | CAS RN |
---|---|---|
antihistaminics | 271 | 58581-89-8 |
Dose | Unit | Route |
---|---|---|
0.56 | mg | N |
4 | mg | O |
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 1, 1996 | FDA | MEDA PHARMS |
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 |
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 |
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 |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.91 | Basic |
None
None
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 |
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 |
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 |