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

Stem definition	Drug id	CAS RN
antihistaminics	1027	80012-43-7

Description:

Molecule	Description
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

Molecule

Description

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:

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Property	Value	Reference
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
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.15 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Oct. 16, 2003	FDA	ALLERGAN
Sept. 20, 2019	PMDA	Santen Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

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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	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

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FDA Adverse Event Reporting System (Male)

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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	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

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FDA Adverse Event Reporting System (Geriatric)

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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	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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
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
FDA EPC	N0000175519	Histamine-1 Receptor Inhibitor
FDA EPC	N0000175883	Adrenergic Receptor Agonist
FDA MoA	N0000000122	Adrenergic Agonists
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists

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

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	9.94	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8.90	WOMBAT-PK	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN				WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN				WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN				WOMBAT-PK
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.37	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.96	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN				WOMBAT-PK
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	4.53	CHEMBL

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External reference:

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ID	Source
007311	NDDF
007312	NDDF
108929-04-0	SECONDARY_CAS_RN
17645	MMSL
181234	MMSL
236961	RXNORM
3241	PUBCHEM_CID
4021466	VUID
4021466	VANDF
407068009	SNOMEDCT_US

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Pharmaceutical products:

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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	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

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