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Identification
NameEpinastine
Accession NumberDB00751  (APRD00043)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionEpinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
Structure
Thumb
Synonyms
(+-)-Epinastine
3-amino-9,13b-dihydro-1H-Dibenz(c,F)imidazo(1,5-a)azepine
Epinastin
Epinastina
Epinastine
Epinastinum
External Identifiers
  • WAL 801 Cl
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ElestatSolution / drops.5 mg/mLOphthalmicAllergan, Inc.2004-01-19Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicPerrigo Company2011-11-012016-10-13Us
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicSomerset Therapeutics, Llc2016-09-14Not applicableUs
Epinastine HydrochlorideSolution.5 mg/mLOphthalmicApotex Corp.2011-10-31Not applicableUs
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicA S Medication Solutions2013-11-05Not applicableUs
Epinastine HydrochlorideSolution.5 mg/mLOphthalmicSun Pharmaceutical Industries Limited2011-11-01Not applicableUs
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicBreckenridge Pharmaceutical, Inc.2013-11-05Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlegainKyorin Rimedio
AlenapionChoseido Pharmaceutical
AlesionBoehringer Ingelheim
AlesiotecNihon Yakuhin Kogyo
AlketPoen
AllernothinMorishita Jintan
AllerstinDong Koo
AlpeedDaito
AplatinTaiyo Pharmaceutical
ArestenIl Sung
AsmotTatsumi Kagaku
AtergitRoemmers
AzusaleonShiono Kemikaru
ElpinanTowa Yakuhin
EpinastineKotobuki Seiyaku
EpinazionMedisa Shinyaku
EpioftalFarmindustria
FlurinolBoehringer Ingelheim
HelvottzYoshindo
Kai lai ZhiCarelife Pharmaceutical Co Ltd
PinasionTaisho Yakuhin
PurivistAllergan
RelenastineLansier
RelestatAllergan
TalercAché
TimkentNisshin Seiyaku
YupitelIwaki Seiyaku
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Epinastine Hydrochloride
ThumbNot applicableDBSALT000961
Categories
UNIIQ13WX941EF
CAS number80012-43-7
WeightAverage: 249.3104
Monoisotopic: 249.126597495
Chemical FormulaC16H15N3
InChI KeyWHWZLSFABNNENI-UHFFFAOYSA-N
InChI
InChI=1S/C16H15N3/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16/h1-8,15H,9-10H2,(H2,17,18)
IUPAC Name
2,4-diazatetracyclo[12.4.0.0²,⁶.0⁷,¹²]octadeca-1(18),3,7,9,11,14,16-heptaen-3-amine
SMILES
NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21
Pharmacology
IndicationFor the prevention of itching associated with allergic conjunctivitis.
Structured Indications
PharmacodynamicsEpinastine is an antihistamine and an inhibitor of histamine release from the mast cell for topical administration to the eyes. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for the histamine H2 receptor. Epinastine also possesses affinity for the a1-, a2-, and 5-HT2 -receptors. Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system.
Mechanism of actionEpinastine has a multiaction effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.
TargetKindPharmacological actionActionsOrganismUniProt ID
Histamine H1 receptorProteinyes
antagonist
HumanP35367 details
Histamine H2 receptorProteinyes
antagonist
HumanP25021 details
Alpha-1A adrenergic receptorProteinunknown
unknown
HumanP35348 details
Alpha-2A adrenergic receptorProteinunknown
unknown
HumanP08913 details
5-hydroxytryptamine receptor 2AProteinunknown
antagonist
HumanP28223 details
5-hydroxytryptamine receptor 7Proteinunknown
antagonist
HumanP34969 details
Related Articles
AbsorptionThe absolute bioavailability of epinastine is about 40%.
Volume of distributionNot Available
Protein binding64%
Metabolism

Mainly excreted unchanged, less than 10% metabolized.

Route of eliminationEpinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.
Half life12 hours
Clearance
  • 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Epinastine.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Epinastine.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Epinastine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Epinastine.Experimental, Illicit
AbciximabEpinastine may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Epinastine can be increased when it is combined with Abiraterone.Approved
AcenocoumarolEpinastine may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Epinastine can be increased when it is combined with Acetaminophen.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Epinastine is combined with Acetylsalicylic acid.Approved, Vet Approved
AfatinibThe serum concentration of Epinastine can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Epinastine can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Epinastine can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Epinastine can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Epinastine can be increased when it is combined with Alfentanil.Approved, Illicit
AlprostadilEpinastine may increase the antiplatelet activities of Alprostadil.Approved, Investigational
AlteplaseEpinastine may increase the anticoagulant activities of Alteplase.Approved
ALX-0081Epinastine may increase the anticoagulant activities of ALX-0081.Investigational
AmantadineThe serum concentration of Epinastine can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Epinastine can be increased when it is combined with Aminohippuric acid.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Epinastine is combined with Aminosalicylic Acid.Approved
AmiodaroneThe metabolism of Epinastine can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Epinastine can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Epinastine can be increased when it is combined with Amlodipine.Approved
AmphetamineAmphetamine may decrease the sedative activities of Epinastine.Approved, Illicit
AmprenavirThe serum concentration of Epinastine can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Epinastine can be increased when it is combined with Amsacrine.Approved
AnagrelideEpinastine may increase the anticoagulant activities of Anagrelide.Approved
AncrodEpinastine may increase the anticoagulant activities of Ancrod.Investigational
AnistreplaseEpinastine may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanEpinastine may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Epinastine is combined with Apixaban.Approved
AprepitantThe serum concentration of Epinastine can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinEpinastine may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanEpinastine may increase the anticoagulant activities of Argatroban.Approved, Investigational
ArtemetherThe metabolism of Epinastine can be decreased when combined with Artemether.Approved
AstaxanthinEpinastine may increase the anticoagulant activities of Astaxanthin.Investigational
AstemizoleThe serum concentration of Epinastine can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Epinastine.Approved, Investigational
AtenololThe serum concentration of Epinastine can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Epinastine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Epinastine can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Epinastine can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Epinastine can be increased when it is combined with Azithromycin.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Epinastine is combined with Balsalazide.Approved, Investigational
BatroxobinEpinastine may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminEpinastine may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinEpinastine may increase the anticoagulant activities of Bemiparin.Approved
BenzocaineThe serum concentration of Epinastine can be increased when it is combined with Benzocaine.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Epinastine.Approved, Illicit
Benzylpenicilloyl PolylysineEpinastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BepridilThe serum concentration of Epinastine can be increased when it is combined with Bepridil.Approved, Withdrawn
BeraprostEpinastine may increase the anticoagulant activities of Beraprost.Investigational
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Epinastine.Approved
BetaxololThe metabolism of Epinastine can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Epinastine can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Epinastine can be increased when it is combined with Biperiden.Approved
BivalirudinEpinastine may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Epinastine can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Epinastine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Epinastine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Epinastine.Approved
BromocriptineThe serum concentration of Epinastine can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Epinastine can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Epinastine can be decreased when combined with Bupropion.Approved
BuspironeThe serum concentration of Epinastine can be increased when it is combined with Buspirone.Approved, Investigational
ButylphthalideEpinastine may increase the antiplatelet activities of Butylphthalide.Investigational
CabazitaxelThe serum concentration of Epinastine can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Epinastine can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Epinastine can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Epinastine can be increased when it is combined with Candesartan.Approved
CangrelorEpinastine may increase the anticoagulant activities of Cangrelor.Approved
CaptoprilThe serum concentration of Epinastine can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Epinastine can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Epinastine can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Epinastine can be increased when it is combined with Caspofungin.Approved
CefditorenThe serum concentration of Cefditoren can be decreased when it is combined with Epinastine.Approved
CefpodoximeEpinastine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Vet Approved
CefuroximeEpinastine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CelecoxibThe metabolism of Epinastine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Epinastine can be increased when it is combined with Ceritinib.Approved
CertoparinEpinastine may increase the anticoagulant activities of Certoparin.Approved
ChloroquineThe serum concentration of Epinastine can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Epinastine.Illicit, Withdrawn
ChlorpromazineThe serum concentration of Epinastine can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Epinastine can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Epinastine can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholecalciferolThe metabolism of Epinastine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Epinastine can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Epinastine can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Epinastine can be increased when it is combined with Cilazapril.Approved
CilostazolEpinastine may increase the anticoagulant activities of Cilostazol.Approved
CimetidineThe serum concentration of Epinastine can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Epinastine can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Epinastine can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Epinastine can be increased when it is combined with Citalopram.Approved
Citric AcidEpinastine may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Epinastine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Epinastine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Epinastine can be decreased when combined with Clobazam.Approved, Illicit
ClofazimineThe serum concentration of Epinastine can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Epinastine can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClopidogrelThe metabolism of Epinastine can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Epinastine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Epinastine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Epinastine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Epinastine can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Epinastine can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Epinastine can be increased when it is combined with Colforsin.Experimental
CollagenaseThe risk or severity of adverse effects can be increased when Epinastine is combined with Collagenase.Approved
ConivaptanThe serum concentration of Epinastine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Epinastine can be decreased when combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Epinastine can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Epinastine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CysteamineThe therapeutic efficacy of Cysteamine can be decreased when used in combination with Epinastine.Approved, Investigational
Dabigatran etexilateEpinastine may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Epinastine can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Epinastine can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Epinastine can be increased when it is combined with Dactinomycin.Approved
DalteparinEpinastine may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidEpinastine may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarifenacinThe metabolism of Epinastine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Epinastine can be increased when it is combined with Darunavir.Approved
DasatinibEpinastine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
DaunorubicinThe serum concentration of Epinastine can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Epinastine can be decreased when it is combined with Deferasirox.Approved, Investigational
DefibrotideEpinastine may increase the anticoagulant activities of Defibrotide.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Epinastine.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Epinastine is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Epinastine is combined with dersalazine.Investigational
DesipramineThe serum concentration of Epinastine can be increased when it is combined with Desipramine.Approved
DesirudinEpinastine may increase the anticoagulant activities of Desirudin.Approved
DesloratadineThe serum concentration of Epinastine can be increased when it is combined with Desloratadine.Approved, Investigational
DesmoteplaseEpinastine may increase the anticoagulant activities of Desmoteplase.Investigational
DexamethasoneThe serum concentration of Epinastine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexmethylphenidateEpinastine can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved
DextranEpinastine may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Epinastine may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Epinastine may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Epinastine may increase the anticoagulant activities of Dextran 75.Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Epinastine.Approved, Illicit
DextromethorphanThe serum concentration of Epinastine can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Epinastine can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolEpinastine may increase the anticoagulant activities of Dicoumarol.Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Epinastine.Approved, Illicit
DiflunisalThe risk or severity of adverse effects can be increased when Epinastine is combined with Diflunisal.Approved
DigoxinThe serum concentration of Epinastine can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe metabolism of Epinastine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Epinastine can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Epinastine can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Epinastine can be increased when it is combined with Dipyridamole.Approved
DitazoleEpinastine may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DoxazosinThe serum concentration of Epinastine can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Epinastine can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Epinastine can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Epinastine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Epinastine can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Epinastine can be decreased when combined with Dronedarone.Approved
Drotrecogin alfaEpinastine may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
DuloxetineThe metabolism of Epinastine can be decreased when combined with Duloxetine.Approved
Edetic AcidEpinastine may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanEpinastine may increase the anticoagulant activities of Edoxaban.Approved
EfavirenzThe serum concentration of Epinastine can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Epinastine can be increased when it is combined with Elbasvir.Approved
EliglustatThe metabolism of Epinastine can be decreased when combined with Eliglustat.Approved
EnalaprilThe serum concentration of Epinastine can be increased when it is combined with Enalapril.Approved, Vet Approved
EnoxaparinEpinastine may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Epinastine can be decreased when it is combined with Enzalutamide.Approved
eplivanserineEpinastine may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Epinastine.Approved
EptifibatideEpinastine may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
ErgonovineThe serum concentration of Epinastine can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Epinastine can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Epinastine.Approved, Investigational
ErythromycinThe metabolism of Epinastine can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Epinastine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Epinastine can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Epinastine can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Epinastine can be decreased when it is combined with Estrone.Approved
Ethyl biscoumacetateEpinastine may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Epinastine can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Epinastine can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Epinastine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Epinastine can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
Ferric CarboxymaltoseEpinastine can cause a decrease in the absorption of Ferric Carboxymaltose resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ferric CitrateEpinastine can cause a decrease in the absorption of Ferric Citrate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ferric pyrophosphateEpinastine can cause a decrease in the absorption of Ferric pyrophosphate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Epinastine.Approved
FexofenadineThe serum concentration of Epinastine can be increased when it is combined with Fexofenadine.Approved
FibrinolysinEpinastine may increase the anticoagulant activities of Fibrinolysin.Approved
FidaxomicinThe serum concentration of Epinastine can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe metabolism of Epinastine can be decreased when combined with Fluconazole.Approved
FluindioneEpinastine may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe metabolism of Epinastine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Epinastine can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Epinastine can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Epinastine can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Epinastine can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxEpinastine may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumEpinastine may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe serum concentration of Fosamprenavir can be decreased when it is combined with Epinastine.Approved
FosaprepitantThe serum concentration of Epinastine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Epinastine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Epinastine can be increased when it is combined with Fusidic Acid.Approved
GabexateEpinastine may increase the anticoagulant activities of Gabexate.Investigational
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Epinastine.Approved, Investigational
GenisteinThe serum concentration of Epinastine can be increased when it is combined with Genistein.Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Epinastine.Approved
GlyburideThe serum concentration of Epinastine can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Epinastine can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Epinastine can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Epinastine can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Epinastine can be increased when it is combined with Haloperidol.Approved
HeparinEpinastine may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineEpinastine may increase the anticoagulant activities of Higenamine.Investigational
HirulogEpinastine may increase the anticoagulant activities of Hirulog.Experimental
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Epinastine.Approved, Investigational
HydrocortisoneThe serum concentration of Epinastine can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Epinastine.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Epinastine is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Epinastine.Approved
IbudilastEpinastine may increase the antiplatelet activities of Ibudilast.Approved, Investigational
Icosapent ethylEpinastine may increase the antiplatelet activities of Icosapent ethyl.Approved, Nutraceutical
IdelalisibThe serum concentration of Epinastine can be increased when it is combined with Idelalisib.Approved
idraparinuxEpinastine may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilEpinastine may increase the antiplatelet activities of Ifenprodil.Approved, Withdrawn
IloprostIloprost may increase the antiplatelet activities of Epinastine.Approved, Investigational
ImatinibThe metabolism of Epinastine can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Epinastine can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Epinastine.Approved
IndobufenEpinastine may increase the anticoagulant activities of Indobufen.Investigational
IndomethacinThe serum concentration of Epinastine can be increased when it is combined with Indomethacin.Approved, Investigational
IronEpinastine can cause a decrease in the absorption of Iron resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Iron DextranEpinastine can cause a decrease in the absorption of Iron Dextran resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Vet Approved
Iron saccharateEpinastine can cause a decrease in the absorption of Iron saccharate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
IsavuconazoniumThe metabolism of Epinastine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Epinastine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Epinastine can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Epinastine.Approved, Investigational
IvacaftorThe serum concentration of Epinastine can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Epinastine can be increased when it is combined with Ivermectin.Approved, Vet Approved
Kct 0809Epinastine may increase the anticoagulant activities of Kct 0809.Investigational
KetamineThe serum concentration of Epinastine can be increased when it is combined with Ketamine.Approved, Vet Approved
KetanserinEpinastine may increase the antiplatelet activities of Ketanserin.Investigational
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Epinastine.Approved, Investigational
KetoconazoleThe metabolism of Epinastine can be decreased when combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Epinastine can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Epinastine can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Epinastine.Approved
LepirudinEpinastine may increase the anticoagulant activities of Lepirudin.Approved
LevofloxacinThe serum concentration of Epinastine can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Epinastine can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Epinastine can be increased when it is combined with Lidocaine.Approved, Vet Approved
LimaprostLimaprost may increase the antiplatelet activities of Epinastine.Approved
LiothyronineThe serum concentration of Epinastine can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Epinastine can be decreased when it is combined with Liotrix.Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Epinastine.Approved, Investigational
LisinoprilThe serum concentration of Epinastine can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Epinastine can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Epinastine can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Epinastine can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Epinastine can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Epinastine can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Epinastine can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Epinastine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Epinastine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Epinastine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Epinastine can be decreased when combined with Lumefantrine.Approved
MaprotilineThe serum concentration of Epinastine can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Epinastine can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Epinastine can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Epinastine can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MephedroneMephedrone may decrease the sedative activities of Epinastine.Investigational
MephentermineMephentermine may decrease the sedative activities of Epinastine.Approved
MeprobamateThe serum concentration of Epinastine can be increased when it is combined with Meprobamate.Approved, Illicit
MesalazineThe therapeutic efficacy of Mesalazine can be decreased when used in combination with Epinastine.Approved
MethadoneThe serum concentration of Epinastine can be increased when it is combined with Methadone.Approved
MethamphetamineMethamphetamine may decrease the sedative activities of Epinastine.Approved, Illicit
MethotrimeprazineThe metabolism of Epinastine can be decreased when combined with Methotrimeprazine.Approved
MethylphenidateEpinastine can cause an increase in the absorption of Methylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Epinastine.Approved, Investigational
MibefradilThe serum concentration of Epinastine can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Epinastine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Epinastine can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Epinastine can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the antiplatelet activities of Epinastine.Approved
MirabegronThe metabolism of Epinastine can be decreased when combined with Mirabegron.Approved
MitomycinThe serum concentration of Epinastine can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Epinastine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Epinastine can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MMDAMMDA may decrease the sedative activities of Epinastine.Experimental, Illicit
ModafinilThe serum concentration of Epinastine can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Epinastine can be increased when it is combined with Morphine.Approved, Investigational
NadroparinEpinastine may increase the anticoagulant activities of Nadroparin.Approved
NafamostatEpinastine may increase the anticoagulant activities of Nafamostat.Investigational
NafcillinThe serum concentration of Epinastine can be decreased when it is combined with Nafcillin.Approved
NaftopidilEpinastine may increase the antiplatelet activities of Naftopidil.Investigational
NaltrexoneThe serum concentration of Epinastine can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Epinastine can be increased when it is combined with Naringenin.Experimental
NCX 4016The risk or severity of adverse effects can be increased when Epinastine is combined with NCX 4016.Investigational
NefazodoneThe metabolism of Epinastine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Epinastine.Approved
NeostigmineThe serum concentration of Epinastine can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Epinastine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Epinastine can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Epinastine can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Epinastine can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Epinastine.Approved, Investigational
NimesulideEpinastine may increase the antiplatelet activities of Nimesulide.Approved, Withdrawn
NisoldipineThe serum concentration of Epinastine can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Epinastine can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Epinastine can be increased when it is combined with Nitrendipine.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Epinastine is combined with Nitroaspirin.Investigational
NorethisteroneThe serum concentration of Epinastine can be decreased when it is combined with Norethisterone.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Epinastine is combined with Obinutuzumab.Approved
OlaparibThe metabolism of Epinastine can be decreased when combined with Olaparib.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Epinastine is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Epinastine.Approved
OmeprazoleThe serum concentration of Epinastine can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Epinastine can be increased when it is combined with Osimertinib.Approved
OtamixabanEpinastine may increase the anticoagulant activities of Otamixaban.Investigational
P-NitrophenolThe serum concentration of Epinastine can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Epinastine can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Epinastine can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Epinastine can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe serum concentration of Epinastine can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Epinastine can be increased when it is combined with Pantoprazole.Approved
ParnaparinEpinastine may increase the anticoagulant activities of Parnaparin.Approved
ParoxetineThe metabolism of Epinastine can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Epinastine.Approved
Peginterferon alfa-2bThe serum concentration of Epinastine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Epinastine can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Epinastine.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Epinastine.Approved, Investigational
PerindoprilThe serum concentration of Epinastine can be increased when it is combined with Perindopril.Approved
PhenindioneEpinastine may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Epinastine can be increased when combined with Phenobarbital.Approved
PhenprocoumonEpinastine may increase the anticoagulant activities of Phenprocoumon.Approved
PhenterminePhentermine may decrease the sedative activities of Epinastine.Approved, Illicit
PhenytoinThe metabolism of Epinastine can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Epinastine can be increased when it is combined with Pimozide.Approved
PlasminEpinastine may increase the anticoagulant activities of Plasmin.Investigational
Platelet Activating FactorThe serum concentration of Epinastine can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Epinastine can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Posaconazole can be decreased when it is combined with Epinastine.Approved, Investigational, Vet Approved
PrasugrelEpinastine may increase the anticoagulant activities of Prasugrel.Approved
PravastatinThe serum concentration of Epinastine can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Epinastine can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Epinastine can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Epinastine can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Epinastine can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Epinastine can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Epinastine can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Epinastine can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Epinastine can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Epinastine can be increased when it is combined with Propranolol.Approved, Investigational
Protein CEpinastine may increase the anticoagulant activities of Protein C.Approved
Protein S humanEpinastine may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeEpinastine may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineThe serum concentration of Epinastine can be increased when it is combined with Protriptyline.Approved
PseudoephedrinePseudoephedrine may decrease the sedative activities of Epinastine.Approved
QuazepamThe serum concentration of Epinastine can be increased when it is combined with Quazepam.Approved, Illicit
QuercetinThe serum concentration of Epinastine can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Epinastine can be increased when it is combined with Quinacrine.Approved
QuinidineThe metabolism of Epinastine can be decreased when combined with Quinidine.Approved
QuinineThe serum concentration of Epinastine can be increased when it is combined with Quinine.Approved
RamatrobanEpinastine may increase the antiplatelet activities of Ramatroban.Investigational
RanitidineThe serum concentration of Epinastine can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Epinastine can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Epinastine can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Epinastine can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Epinastine can be decreased when it is combined with Reserpine.Approved
ResveratrolEpinastine may increase the antiplatelet activities of Resveratrol.Experimental, Investigational
ReteplaseEpinastine may increase the anticoagulant activities of Reteplase.Approved
ReviparinEpinastine may increase the anticoagulant activities of Reviparin.Approved
RidogrelEpinastine may increase the antiplatelet activities of Ridogrel.Approved
RifabutinThe metabolism of Epinastine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Epinastine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Epinastine can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Epinastine.Approved
RisedronateThe serum concentration of Risedronate can be increased when it is combined with Epinastine.Approved, Investigational
RitobegronRitobegron may decrease the sedative activities of Epinastine.Investigational
RitonavirThe metabolism of Epinastine can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanEpinastine may increase the anticoagulant activities of Rivaroxaban.Approved
RolapitantThe serum concentration of Epinastine can be increased when it is combined with Rolapitant.Approved
RopiniroleThe metabolism of Epinastine can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneEpinastine may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Epinastine is combined with Salicylic acid.Approved, Vet Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Epinastine.Approved, Investigational
SCH-530348Epinastine may increase the antiplatelet activities of SCH-530348.Investigational
ScopolamineThe serum concentration of Epinastine can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Epinastine can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagEpinastine may increase the anticoagulant activities of Selexipag.Approved
SertralineThe serum concentration of Epinastine can be increased when it is combined with Sertraline.Approved
SevofluraneEpinastine may increase the antiplatelet activities of Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Epinastine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Epinastine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Epinastine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Epinastine can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Epinastine can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Epinastine can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Epinastine can be increased when it is combined with Spironolactone.Approved
SRT501Epinastine may increase the antiplatelet activities of SRT501.Investigational
St. John's WortThe serum concentration of Epinastine can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Epinastine can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Epinastine can be increased when it is combined with Stiripentol.Approved
StreptokinaseEpinastine may increase the anticoagulant activities of Streptokinase.Approved
StreptozocinThe serum concentration of Epinastine can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Epinastine can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Epinastine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideEpinastine may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SumatriptanThe serum concentration of Epinastine can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Epinastine can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Epinastine can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Epinastine can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Epinastine can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Epinastine can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe metabolism of Epinastine can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Epinastine can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Epinastine can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Epinastine can be increased when it is combined with Temsirolimus.Approved
TenecteplaseEpinastine may increase the anticoagulant activities of Tenecteplase.Approved
TerazosinThe serum concentration of Epinastine can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Epinastine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Epinastine can be increased when it is combined with Terfenadine.Withdrawn
TesmilifeneThe serum concentration of Epinastine can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Epinastine can be increased when it is combined with Testosterone.Approved, Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Epinastine.Approved
ThiotepaThe metabolism of Epinastine can be decreased when combined with Thiotepa.Approved
TicagrelorThe serum concentration of Epinastine can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Epinastine can be decreased when combined with Ticlopidine.Approved
TinzaparinEpinastine may increase the anticoagulant activities of Tinzaparin.Approved
TipranavirTipranavir may increase the antiplatelet activities of Epinastine.Approved, Investigational
TirofibanEpinastine may increase the anticoagulant activities of Tirofiban.Approved
TocilizumabThe serum concentration of Epinastine can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Epinastine can be increased when it is combined with Tolvaptan.Approved
TositumomabThe risk or severity of adverse effects can be increased when Epinastine is combined with Tositumomab.Approved
TranilastEpinastine may increase the antiplatelet activities of Tranilast.Approved, Investigational
TranylcypromineThe metabolism of Epinastine can be decreased when combined with Tranylcypromine.Approved
TrapidilEpinastine may increase the antiplatelet activities of Trapidil.Approved
TrazodoneThe serum concentration of Epinastine can be decreased when it is combined with Trazodone.Approved, Investigational
TreprostinilTreprostinil may increase the antiplatelet activities of Epinastine.Approved, Investigational
TrifluoperazineThe serum concentration of Epinastine can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Epinastine can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TriflusalEpinastine may increase the anticoagulant activities of Triflusal.Approved
TrimethoprimThe serum concentration of Epinastine can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Epinastine can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Epinastine can be increased when it is combined with Troleandomycin.Approved
UrokinaseEpinastine may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Epinastine.Approved, Investigational
VenlafaxineThe metabolism of Epinastine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Epinastine can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Epinastine can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Epinastine can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Epinastine can be increased when it is combined with Vinorelbine.Approved, Investigational
Vitamin EVitamin E may increase the antiplatelet activities of Epinastine.Approved, Nutraceutical, Vet Approved
VorapaxarEpinastine may increase the anticoagulant activities of Vorapaxar.Approved
VoriconazoleThe metabolism of Epinastine can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinEpinastine may increase the anticoagulant activities of Warfarin.Approved
XimelagatranEpinastine may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Ym150Epinastine may increase the anticoagulant activities of Ym150.Investigational
ZimelidineThe serum concentration of Epinastine can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Epinastine can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis Reference

Akiharu Isowaki, Tomoko Nakajima, Akira Ohtori, “Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine.” U.S. Patent US20090143359, issued June 04, 2009.

US20090143359
General References
  1. Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6. [PubMed:1972625 ]
  2. Schilling JC, Adamus WS, Kuthan H: Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1990 Dec;28(12):493-7. [PubMed:1982280 ]
External Links
ATC CodesR06AX24S01GX10
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (113 KB)
MSDSDownload (57 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9923
Blood Brain Barrier+0.9787
Caco-2 permeable+0.5766
P-glycoprotein substrateSubstrate0.5665
P-glycoprotein inhibitor INon-inhibitor0.8193
P-glycoprotein inhibitor IINon-inhibitor0.5736
Renal organic cation transporterInhibitor0.7994
CYP450 2C9 substrateNon-substrate0.8676
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.5422
CYP450 1A2 substrateNon-inhibitor0.5686
CYP450 2C9 inhibitorNon-inhibitor0.9243
CYP450 2D6 inhibitorNon-inhibitor0.5228
CYP450 2C19 inhibitorNon-inhibitor0.8702
CYP450 3A4 inhibitorNon-inhibitor0.6566
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.726
Ames testAMES toxic0.5689
CarcinogenicityNon-carcinogens0.9144
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7509 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9353
hERG inhibition (predictor II)Non-inhibitor0.8419
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Allergan inc
Packagers
Dosage forms
FormRouteStrength
SolutionOphthalmic.5 mg/mL
Solution / dropsOphthalmic.5 mg/mL
Prices
Unit descriptionCostUnit
Elestat 0.05% Solution 5ml Bottle116.58USD bottle
Elestat 0.05% eye drops22.94USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7429602 No2000-11-292020-11-29Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point205-208 °CNot Available
logP3.51BIOBYTE (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.163 mg/mLALOGPS
logP2.53ALOGPS
logP3.07ChemAxon
logS-3.2ALOGPS
pKa (Strongest Basic)8.77ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area41.62 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity76.9 m3·mol-1ChemAxon
Polarizability27.33 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzazepines. These are compounds with two benzene rings connected by an azepine ring. Azepine is an unsaturated seven-member heterocycle with one nitrogen atom replacing a carbon atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzazepines
Sub ClassDibenzazepines
Direct ParentDibenzazepines
Alternative Parents
Substituents
  • Dibenzazepine
  • Azepine
  • Benzenoid
  • 2-imidazoline
  • Tertiary amine
  • Guanidine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Tsujii T, Yamamoto E, Ohira T, Saito N, Watanabe S: Effects of sedative and non-sedative H1 antagonists on cognitive tasks: behavioral and near-infrared spectroscopy (NIRS) examinations. Psychopharmacology (Berl). 2007 Sep;194(1):83-91. Epub 2007 May 30. [PubMed:17534605 ]
  2. Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6. [PubMed:1972625 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) si...
Gene Name:
HRH2
Uniprot ID:
P25021
Molecular Weight:
40097.65 Da
References
  1. Bielory L, Ghafoor S: Histamine receptors and the conjunctiva. Curr Opin Allergy Clin Immunol. 2005 Oct;5(5):437-40. [PubMed:16131920 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
unknown
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [PubMed:8836655 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
unknown
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [PubMed:8836655 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Dupont LJ, Pype JL, Meade CJ, DeLeyn P, Deneffe G, Demedts MG, Verleden GM: Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro. Eur Respir J. 1999 Nov;14(5):1068-75. [PubMed:10596692 ]
  2. Dupont LJ, Meade CJ, Demedts MG, Verleden GM: Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor. Eur Respir J. 1996 Jul;9(7):1433-8. [PubMed:8836655 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Dupont LJ, Pype JL, Meade CJ, DeLeyn P, Deneffe G, Demedts MG, Verleden GM: Epinastine (WAL 801CL) inhibits the electrical field stimulation-induced cholinergic contraction in guinea pig and human airways in vitro. Eur Respir J. 1999 Nov;14(5):1068-75. [PubMed:10596692 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Ishiguro N, Nozawa T, Tsujihata A, Saito A, Kishimoto W, Yokoyama K, Yotsumoto T, Sakai K, Igarashi T, Tamai I: Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metab Dispos. 2004 May;32(5):519-24. [PubMed:15100174 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23