Stem definition | Drug id | CAS RN |
---|---|---|
antihistaminics | 1027 | 80012-43-7 |
None
Property | Value | Reference |
---|---|---|
MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.15 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Date | Agency | Company | Orphan |
---|---|---|---|
Oct. 16, 2003 | FDA | ALLERGAN | |
Sept. 20, 2019 | PMDA | Santen Pharmaceutical Co., Ltd. |
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 | 170.03 | 26.77 | 80 | 1311 | 137557 | 50466176 |
Platelet count decreased | 35.20 | 26.77 | 26 | 1365 | 100700 | 50503033 |
Hepatic function abnormal | 33.98 | 26.77 | 17 | 1374 | 32664 | 50571069 |
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 | 99.03 | 30.63 | 43 | 1293 | 36896 | 29536295 |
Hepatic function abnormal | 71.58 | 30.63 | 35 | 1301 | 39224 | 29533967 |
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 |
---|---|---|---|---|---|---|
Hepatic function abnormal | 92.12 | 23.12 | 47 | 2555 | 64266 | 64431864 |
Platelet count decreased | 43.54 | 23.12 | 43 | 2559 | 167668 | 64328462 |
Drug eruption | 36.55 | 23.12 | 21 | 2581 | 36115 | 64460015 |
Pyrexia | 35.83 | 23.12 | 73 | 2529 | 558571 | 63937559 |
Interstitial lung disease | 32.93 | 23.12 | 29 | 2573 | 97703 | 64398427 |
Decreased appetite | 27.18 | 23.12 | 44 | 2558 | 281245 | 64214885 |
Neutrophil count decreased | 26.18 | 23.12 | 23 | 2579 | 77173 | 64418957 |
None
Source | Code | Description |
---|---|---|
ATC | R06AX24 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use |
ATC | S01GX10 | SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics |
FDA MoA | N0000000122 | Adrenergic Agonists |
FDA MoA | N0000000190 | Histamine H1 Receptor Antagonists |
FDA EPC | N0000175519 | Histamine-1 Receptor Inhibitor |
MeSH PA | D018494 | Histamine Agents |
MeSH PA | D006633 | Histamine Antagonists |
MeSH PA | D006634 | Histamine H1 Antagonists |
MeSH PA | D018377 | Neurotransmitter Agents |
FDA PE | N0000175628 | Decreased Histamine Release |
FDA EPC | N0000175883 | Adrenergic Receptor Agonist |
CHEBI has role | CHEBI:37955 | H1 receptor antagonists |
CHEBI has role | CHEBI:37956 | antihistamines |
CHEBI has role | CHEBI:50857 | anti-allergic drugs |
CHEBI has role | CHEBI:66981 | ophthalmology drugs |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
Ocular Itching | indication |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 9.94 | 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 | 8.90 | WOMBAT-PK | CHEMBL | |||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4 | WOMBAT-PK | |||||
Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
5-hydroxytryptamine receptor 2A | GPCR | WOMBAT-PK | |||||||
Alpha-1A adrenergic receptor | GPCR | WOMBAT-PK | |||||||
Histamine H2 receptor | GPCR | WOMBAT-PK | |||||||
Solute carrier family 22 member 2 | Transporter | IC50 | 5.37 | CHEMBL | |||||
Multidrug and toxin extrusion protein 1 | Transporter | IC50 | 5.96 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | WOMBAT-PK | |||||||
Multidrug and toxin extrusion protein 2 | Transporter | IC50 | 4.53 | CHEMBL | |||||
Histamine H1 receptor | GPCR | IC50 | 8.80 | CHEMBL |
ID | Source |
---|---|
4021466 | VUID |
N0000148850 | NUI |
D01713 | KEGG_DRUG |
108929-04-0 | SECONDARY_CAS_RN |
4021466 | VANDF |
C0078442 | UMLSCUI |
CHEBI:51032 | CHEBI |
CHEMBL1106 | ChEMBL_ID |
DB00751 | DRUGBANK_ID |
CHEMBL1200491 | ChEMBL_ID |
C053090 | MESH_SUPPLEMENTAL_RECORD_UI |
3241 | PUBCHEM_CID |
7176 | IUPHAR_LIGAND_ID |
5953 | INN_ID |
Q13WX941EF | UNII |
236961 | RXNORM |
17645 | MMSL |
181234 | MMSL |
007311 | NDDF |
007312 | NDDF |
407068009 | SNOMEDCT_US |
407069001 | SNOMEDCT_US |
427671005 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Epinastine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-911 | SOLUTION/ DROPS | 0.50 mg | OPHTHALMIC | ANDA | 22 sections |
Epinastine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51991-836 | SOLUTION/ DROPS | 0.50 mg | OPHTHALMIC | ANDA | 26 sections |
EPINASTINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 62756-329 | SOLUTION | 0.50 mg | OPHTHALMIC | ANDA | 22 sections |
EPINASTINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70069-008 | SOLUTION/ DROPS | 0.50 mg | OPHTHALMIC | ANDA | 20 sections |