epinastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics 1027 80012-43-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alesion
  • epinastine
  • (+/-)-Epinastine
  • epinastine hydrochloride
  • epinastine HCl
direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell, indicated for the prevention of itching associated with allergic conjunctivitis
  • Molecular weight: 249.32
  • Formula: C16H15N3
  • CLOGP: 2.15
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 41.62
  • ALOGS: -3.18
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.15 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility) 38 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Oct. 16, 2003 FDA ALLERGAN
Sept. 20, 2019 PMDA Santen Pharmaceutical Co., Ltd.

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 150.71 25.67 80 1472 198963 63288507
Platelet count decreased 36.85 25.67 27 1525 116095 63371375
Hepatic function abnormal 36.77 25.67 18 1534 37124 63450346

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 89.81 28.09 43 1516 46654 34908718
Hepatic function abnormal 70.80 28.09 36 1523 44327 34911045
Drug eruption 28.36 28.09 15 1544 19883 34935489

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
Hepatic function abnormal 95.34 22.94 49 2944 73058 79668337
Platelet count decreased 48.06 22.94 47 2946 194617 79546778
Drug eruption 39.34 22.94 23 2970 43912 79697483
Pyrexia 37.53 22.94 80 2913 678629 79062766
Interstitial lung disease 35.12 22.94 31 2962 112569 79628826
Decreased appetite 29.65 22.94 49 2944 342369 79399026
Neutrophil count decreased 23.72 22.94 23 2970 93936 79647459
Cardiac failure 23.52 22.94 29 2964 154813 79586582

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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

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

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204
Ocular Itching indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.94 Basic

Orange Book patent data (new drug applications)

None

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 8.90 WOMBAT-PK CHEMBL
Alpha-1A adrenergic receptor GPCR WOMBAT-PK
Alpha-2A adrenergic receptor GPCR WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4 WOMBAT-PK
Multidrug resistance protein 1 Transporter 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
5-hydroxytryptamine receptor 2A GPCR WOMBAT-PK
Multidrug and toxin extrusion protein 2 Transporter IC50 4.53 CHEMBL
Histamine H1 receptor GPCR IC50 8.80 CHEMBL

External reference:

IDSource
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 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