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 | 158.74 | 26.54 | 80 | 1368 | 170312 | 56120307 |
Platelet count decreased | 35.46 | 26.54 | 26 | 1422 | 106357 | 56184262 |
Hepatic function abnormal | 34.15 | 26.54 | 17 | 1431 | 34541 | 56256078 |
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 | 94.34 | 29.22 | 43 | 1408 | 40749 | 31655144 |
Hepatic function abnormal | 69.48 | 29.22 | 35 | 1416 | 41187 | 31654706 |
Drug eruption | 29.27 | 29.22 | 15 | 1436 | 18172 | 31677721 |
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 | 91.00 | 23.44 | 47 | 2727 | 67949 | 70857721 |
Platelet count decreased | 42.45 | 23.44 | 43 | 2731 | 178179 | 70747491 |
Drug eruption | 40.74 | 23.44 | 23 | 2751 | 39473 | 70886197 |
Pyrexia | 36.68 | 23.44 | 76 | 2698 | 606876 | 70318794 |
Interstitial lung disease | 33.96 | 23.44 | 30 | 2744 | 104655 | 70821015 |
Decreased appetite | 28.25 | 23.44 | 46 | 2728 | 304734 | 70620936 |
Alopecia areata | 25.94 | 23.44 | 7 | 2767 | 1629 | 70924041 |
Neutrophil count decreased | 25.22 | 23.44 | 23 | 2751 | 83533 | 70842137 |
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 |
CHEMBL1200491 | ChEMBL_ID |
DB00751 | DRUGBANK_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 |