Identification

Name
Epinastine
Accession Number
DB00751  (APRD00043)
Type
Small Molecule
Groups
Approved, Investigational
Description

Epinastine 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 IDs
WAL 801 Cl
Product Ingredients
IngredientUNIICASInChI Key
Epinastine HydrochlorideGFM415S5XL108929-04-0VKXSGUIOOQPGAF-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ElestatSolution / drops.5 mg/mLOphthalmicAllergan2004-01-19Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EpinastineSolution / drops.5 mg/mLOphthalmicAkorn2017-05-05Not applicableUs
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicPerrigo International2011-11-012016-10-13Us
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicSomerset Therapeutics, Llc2016-09-14Not applicableUs
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicBreckenridge Pharmaceutical, Inc.2013-11-05Not applicableUs
Epinastine HydrochlorideSolution.5 mg/mLOphthalmicSun Pharmaceutical Industries Limited2011-11-01Not applicableUs
Epinastine HydrochlorideSolution / drops.5 mg/mLOphthalmicA S Medication Solutions2013-11-052017-06-20Us
Epinastine HydrochlorideSolution.5 mg/mLOphthalmicApotex Corporation2011-10-31Not applicableUs
International/Other Brands
Alegain (Kyorin Rimedio) / Alenapion (Choseido Pharmaceutical) / Alesion (Boehringer Ingelheim) / Alesiotec (Nihon Yakuhin Kogyo) / Alket (Poen) / Allernothin (Morishita Jintan) / Allerstin (Dong Koo) / Alpeed (Daito) / Aplatin (Taiyo Pharmaceutical) / Aresten (Il Sung) / Asmot (Tatsumi Kagaku) / Atergit (Roemmers) / Azusaleon (Shiono Kemikaru) / Elpinan (Towa Yakuhin) / Epinastine (Kotobuki Seiyaku) / Epinazion (Medisa Shinyaku) / Epioftal (Farmindustria) / Flurinol (Boehringer Ingelheim) / Helvottz (Yoshindo) / Kai lai Zhi (Carelife Pharmaceutical Co Ltd) / Pinasion (Taisho Yakuhin) / Purivist (Allergan) / Relenastine (Lansier) / Relestat (Allergan) / Talerc (Aché) / Timkent (Nisshin Seiyaku) / Yupitel (Iwaki Seiyaku)
Categories
UNII
Q13WX941EF
CAS number
80012-43-7
Weight
Average: 249.3104
Monoisotopic: 249.126597495
Chemical Formula
C16H15N3
InChI Key
WHWZLSFABNNENI-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

Indication

For the prevention of itching associated with allergic conjunctivitis.

Associated Conditions
Pharmacodynamics

Epinastine 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 action

Epinastine 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.

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Human
AHistamine H2 receptor
antagonist
Human
UAlpha-1A adrenergic receptor
unknown
Human
UAlpha-2A adrenergic receptor
unknown
Human
U5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
Absorption

The absolute bioavailability of epinastine is about 40%.

Volume of distribution
Not Available
Protein binding

64%

Metabolism

Mainly excreted unchanged, less than 10% metabolized.

Route of elimination

Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.

Half life

12 hours

Clearance
  • 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Epinastine H1-Antihistamine ActionDrug action
Epinastine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Epinastine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Epinastine.Experimental
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine 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, Investigational
AcepromazineAcepromazine may decrease the vasoconstricting activities of Epinastine.Approved, Vet Approved
AcetaminophenThe serum concentration of Epinastine can be increased when it is combined with Acetaminophen.Approved
Acetyl sulfisoxazoleThe metabolism of Epinastine can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Epinastine is combined with Acetylsalicylic acid.Approved, Vet Approved
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
AloxiprinThe risk or severity of adverse effects can be increased when Epinastine is combined with Aloxiprin.Experimental
AlprostadilEpinastine may increase the antiplatelet activities of Alprostadil.Approved, Investigational
AlteplaseEpinastine may increase the anticoagulant activities of Alteplase.Approved
AmikacinThe risk or severity of adverse effects can be increased when Amikacin is combined with Epinastine.Approved, Investigational, Vet Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Epinastine is combined with Aminosalicylic Acid.Approved
AmiodaroneThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may decrease the vasoconstricting activities of Epinastine.Approved
AmlodipineThe serum concentration of Epinastine can be increased when it is combined with Amlodipine.Approved
AmoxapineAmoxapine may decrease the vasoconstricting activities of Epinastine.Approved
AmphetamineAmphetamine may decrease the sedative activities of Epinastine.Approved, Illicit, Investigational
AnagrelideEpinastine may increase the anticoagulant activities of Anagrelide.Approved
AncrodEpinastine may increase the anticoagulant activities of Ancrod.Approved, Investigational
AndrographolideEpinastine may increase the antiplatelet activities of Andrographolide.Investigational
AnistreplaseEpinastine may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanEpinastine may increase the anticoagulant activities of Antithrombin III human.Approved
ApalutamideThe serum concentration of Epinastine can be decreased when it is combined with Apalutamide.Approved, Investigational
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, Investigational, Withdrawn
ArgatrobanEpinastine may increase the anticoagulant activities of Argatroban.Approved, Investigational
AripiprazoleAripiprazole may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
ArtemetherThe metabolism of Epinastine can be decreased when combined with Artemether.Approved
AsenapineAsenapine may decrease the vasoconstricting activities of Epinastine.Approved
AstaxanthinEpinastine may increase the anticoagulant activities of Astaxanthin.Investigational
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Epinastine.Approved, Investigational
AtomoxetineThe metabolism of Epinastine can be decreased when combined with Atomoxetine.Approved
AzelastineEpinastine may increase the antiplatelet activities of Azelastine.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, Investigational
BenzatropineThe risk or severity of QTc prolongation can be increased when Benzatropine is combined with Epinastine.Approved
BenzphetamineBenzphetamine may decrease the sedative and stimulatory activities of Epinastine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Epinastine.Approved
Benzylpenicilloyl PolylysineEpinastine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BepridilThe risk or severity of QTc prolongation can be increased when Epinastine 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, Investigational
BetaxololThe metabolism of Epinastine can be decreased when combined with Betaxolol.Approved, Investigational
BevantololBevantolol may decrease the vasoconstricting activities of Epinastine.Approved
BivalirudinEpinastine may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Epinastine can be decreased when combined with Boceprevir.Approved, Withdrawn
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
BrexpiprazoleBrexpiprazole may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
BrinaseEpinastine may increase the anticoagulant activities of Brinase.Experimental
BromocriptineBromocriptine may increase the hypertensive and vasoconstricting activities of Epinastine.Approved, Investigational
BrompheniramineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Brompheniramine.Approved
BucindololBucindolol may decrease the vasoconstricting activities of Epinastine.Investigational
BuflomedilEpinastine may increase the antiplatelet activities of Buflomedil.Experimental
BunazosinBunazosin may decrease the vasoconstricting activities of Epinastine.Investigational
BupropionThe risk or severity of adverse effects can be increased when Bupropion is combined with Epinastine.Approved
ButylphthalideEpinastine may increase the antiplatelet activities of Butylphthalide.Investigational
CabergolineCabergoline may increase the hypertensive and vasoconstricting activities of Epinastine.Approved
CaffeineThe serum concentration of Epinastine can be increased when it is combined with Caffeine.Approved
CangrelorEpinastine may increase the anticoagulant activities of Cangrelor.Approved
CaplacizumabEpinastine may increase the anticoagulant activities of Caplacizumab.Investigational
CarbamazepineThe metabolism of Epinastine can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Epinastine is combined with Carbaspirin calcium.Experimental, Investigational
CarvedilolThe serum concentration of Epinastine can be increased when it is combined with Carvedilol.Approved, Investigational
CefditorenThe serum concentration of Cefditoren can be decreased when it is combined with Epinastine.Approved, Investigational
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, Investigational
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Epinastine.Approved
ChloroquineThe metabolism of Epinastine can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorphenamineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Chlorphenamine.Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Epinastine.Illicit, Withdrawn
ChlorpromazineThe metabolism of Epinastine can be decreased when combined with Chlorpromazine.Approved, Investigational, Vet Approved
CholecalciferolThe metabolism of Epinastine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolEpinastine may increase the anticoagulant activities of Cilostazol.Approved, Investigational
CinacalcetThe metabolism of Epinastine can be decreased when combined with Cinacalcet.Approved
CinnarizineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Cinnarizine.Approved, Investigational
CiprofloxacinThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe metabolism of Epinastine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Epinastine can be decreased when combined with Clarithromycin.Approved
ClemastineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Clemastine.Approved, Investigational
ClindamycinThe risk or severity of adverse effects can be increased when Clindamycin is combined with Epinastine.Approved, Vet Approved
ClobazamThe metabolism of Epinastine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Epinastine can be decreased when combined with Clomipramine.Approved, Investigational, Vet Approved
ClopidogrelThe metabolism of Epinastine can be decreased when combined with Clopidogrel.Approved
CloricromenEpinastine may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneEpinastine may increase the anticoagulant activities of Clorindione.Experimental
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
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Epinastine.Approved, Illicit
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Epinastine is combined with Collagenase clostridium histolyticum.Approved, Investigational
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Epinastine.Approved, Investigational
CrizotinibThe metabolism of Epinastine can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Epinastine can be decreased when combined with Curcumin.Approved, Investigational
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Epinastine.Approved
CyclosporineThe serum concentration of Epinastine can be increased when it is 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, Investigational
DalteparinEpinastine may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidEpinastine may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DapiprazoleDapiprazole may decrease the vasoconstricting activities of Epinastine.Approved
DarexabanEpinastine may increase the anticoagulant activities of Darexaban.Investigational
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
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
DelavirdineEpinastine can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.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 metabolism of Epinastine can be decreased when combined with Desipramine.Approved, Investigational
DesirudinEpinastine may increase the anticoagulant activities of Desirudin.Approved
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
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Epinastine.Approved
DexmethylphenidateThe therapeutic efficacy of Dexmethylphenidate can be decreased when used in combination with Epinastine.Approved, Investigational
DexniguldipineThe serum concentration of Epinastine can be increased when it is combined with Dexniguldipine.Experimental
DextranEpinastine may increase the anticoagulant activities of Dextran.Approved, Investigational, Vet Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Epinastine.Approved, Illicit
DexverapamilThe serum concentration of Epinastine can be increased when it is combined with Dexverapamil.Experimental
DicoumarolEpinastine may increase the anticoagulant activities of Dicoumarol.Approved
DiethylpropionDiethylpropion may decrease the sedative and stimulatory activities of Epinastine.Approved, Illicit
DiflunisalThe risk or severity of adverse effects can be increased when Epinastine is combined with Diflunisal.Approved, Investigational
DihydroergotamineDihydroergotamine may increase the hypertensive and vasoconstricting activities of Epinastine.Approved, Investigational
DiltiazemThe metabolism of Epinastine can be decreased when combined with Diltiazem.Approved, Investigational
DimenhydrinateThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Dimenhydrinate.Approved
DiphenadioneEpinastine may increase the anticoagulant activities of Diphenadione.Experimental
DiphenhydramineThe risk or severity of QTc prolongation can be increased when Diphenhydramine is combined with Epinastine.Approved, Investigational
DipyridamoleEpinastine may increase the anticoagulant activities of Dipyridamole.Approved
DitazoleEpinastine may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DosulepinThe metabolism of Epinastine can be decreased when combined with Dosulepin.Approved
DotarizineThe risk or severity of adverse effects can be increased when Dotarizine is combined with Epinastine.Investigational
DoxazosinThe serum concentration of Epinastine can be increased when it is combined with Doxazosin.Approved
DoxepinDoxepin may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
DoxorubicinThe metabolism of Epinastine can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Epinastine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Epinastine.Approved, Vet Approved
DronedaroneThe metabolism of Epinastine can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may decrease the vasoconstricting activities of Epinastine.Approved, Vet Approved
Drotrecogin alfaEpinastine may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
DuloxetineDuloxetine may increase the tachycardic activities of Epinastine.Approved
Edetic AcidEpinastine may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanEpinastine may increase the anticoagulant activities of Edoxaban.Approved
EliglustatThe metabolism of Epinastine can be decreased when combined with Eliglustat.Approved
EmopamilThe serum concentration of Epinastine can be increased when it is combined with Emopamil.Experimental
EnoxaparinEpinastine may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Epinastine can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe risk or severity of adverse effects can be increased when Eperisone is combined with Epinastine.Approved, Investigational
EpinephrineEpinephrine may decrease the vasoconstricting activities of Epinastine.Approved, Vet Approved
EplivanserinEpinastine may increase the anticoagulant activities of Eplivanserin.Investigational
EpoprostenolEpinastine may increase the anticoagulant activities of Epoprostenol.Approved
EptifibatideEpinastine may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
Ergoloid mesylateErgoloid mesylate may increase the hypertensive and vasoconstricting activities of Epinastine.Approved
ErgonovineErgonovine may increase the hypertensive and vasoconstricting activities of Epinastine.Approved
ErgotamineErgotamine may increase the hypertensive and vasoconstricting activities of Epinastine.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, Investigational, Vet Approved
EscitalopramEscitalopram may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
EthanolEpinastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Epinastine.Approved
Ethyl biscoumacetateEpinastine may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Epinastine.Approved
FamotidineThe risk or severity of QTc prolongation can be increased when Famotidine is combined with Epinastine.Approved
FelodipineThe serum concentration of Epinastine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Epinastine.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 pyrophosphateEpinastine can cause a decrease in the absorption of Ferric pyrophosphate resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Ferulic acidEpinastine may increase the anticoagulant activities of Ferulic acid.Experimental
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Epinastine.Approved
FibrinolysinEpinastine may increase the anticoagulant activities of Fibrinolysin.Investigational
FluconazoleThe metabolism of Epinastine can be decreased when combined with Fluconazole.Approved, Investigational
FluindioneEpinastine may increase the anticoagulant activities of Fluindione.Approved, Investigational
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Epinastine.Approved
FluoxetineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Fluoxetine.Approved, Vet Approved
FlupentixolFlupentixol may decrease the vasoconstricting activities of Epinastine.Approved, Investigational, Withdrawn
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Epinastine.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Epinastine.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Epinastine is combined with Fluvoxamine.Approved, Investigational
FondaparinuxEpinastine 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, Investigational
Fusidic AcidThe serum concentration of Epinastine can be increased when it is combined with Fusidic Acid.Approved, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Epinastine.Approved, Investigational
GabexateEpinastine may increase the anticoagulant activities of Gabexate.Investigational
GallopamilThe serum concentration of Epinastine can be increased when it is combined with Gallopamil.Investigational
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Epinastine.Approved, Investigational
GepefrineGepefrine may decrease the sedative activities of Epinastine.Experimental
GlucosamineGlucosamine may increase the antiplatelet activities of Epinastine.Approved, Investigational
GlyburideThe serum concentration of Epinastine can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Epinastine can be increased when it is combined with Glycerin.Approved, Investigational
GuacetisalThe risk or severity of adverse effects can be increased when Epinastine is combined with Guacetisal.Experimental
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Epinastine.Approved, Investigational
HaloperidolThe metabolism of Epinastine can be decreased when combined with Haloperidol.Approved
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Epinastine is combined with Hemoglobin crosfumaril.Experimental
HeparinEpinastine may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineEpinastine may increase the anticoagulant activities of Higenamine.Investigational
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Epinastine.Approved, Investigational
HydrocodoneEpinastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Epinastine.Approved
HydroxytyrosolEpinastine may increase the antiplatelet activities of Hydroxytyrosol.Investigational
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Epinastine.Approved
IbandronateThe risk or severity of QTc prolongation can be increased when Ibandronate is combined with Epinastine.Approved, Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Epinastine is combined with Ibritumomab tiuxetan.Approved, Investigational
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
IbuprofenThe serum concentration of Epinastine can be increased when it is combined with Ibuprofen.Approved
Icosapent ethylEpinastine may increase the antiplatelet activities of Icosapent ethyl.Approved, Investigational, Nutraceutical
IdelalisibThe metabolism of Epinastine can be decreased when combined with Idelalisib.Approved
IdraparinuxEpinastine may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilEpinastine may increase the antiplatelet activities of Ifenprodil.Approved, Investigational, Withdrawn
IfetrobanEpinastine may increase the antiplatelet activities of Ifetroban.Investigational
IloperidoneIloperidone may decrease the vasoconstricting activities of Epinastine.Approved
IloprostEpinastine may increase the anticoagulant activities of Iloprost.Approved, Investigational
ImatinibThe metabolism of Epinastine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Epinastine can be decreased when 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
IndoraminIndoramin may decrease the vasoconstricting activities of Epinastine.Withdrawn
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Epinastine.Approved
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
IsavuconazoleThe serum concentration of Epinastine can be increased when it is combined with Isavuconazole.Approved, Investigational
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, Investigational
IsradipineThe serum concentration of Epinastine can be increased when it is combined with Isradipine.Approved, Investigational
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
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
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Epinastine.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
LetaxabanEpinastine may increase the anticoagulant activities of Letaxaban.Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Epinastine.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the tachycardic activities of Epinastine.Approved, Investigational
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, Investigational
LinsidomineEpinastine may increase the antiplatelet activities of Linsidomine.Experimental
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Epinastine.Approved, Investigational
LomerizineThe serum concentration of Epinastine can be increased when it is combined with Lomerizine.Experimental
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 risk or severity of QTc prolongation can be increased when Epinastine is combined with Loratadine.Approved, Investigational
LorcaserinThe metabolism of Epinastine can be decreased when combined with Lorcaserin.Approved
LorpiprazoleThe serum concentration of Epinastine can be increased when it is combined with Lorpiprazole.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
Magnesium carbonateThe risk or severity of adverse effects can be increased when Magnesium carbonate is combined with Epinastine.Approved, Investigational
Magnesium citrateThe risk or severity of adverse effects can be increased when Magnesium citrate is combined with Epinastine.Approved
Magnesium sulfateThe therapeutic efficacy of Epinastine can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
Magnesium TrisilicateThe risk or severity of adverse effects can be increased when Magnesium Trisilicate is combined with Epinastine.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Epinastine.Approved
MelagatranEpinastine may increase the anticoagulant activities of Melagatran.Experimental
MephedroneMephedrone may decrease the sedative activities of Epinastine.Investigational
MephentermineMephentermine may decrease the sedative activities of Epinastine.Approved
MepyramineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Mepyramine.Approved, Vet Approved
MesalazineThe therapeutic efficacy of Mesalazine can be decreased when used in combination with Epinastine.Approved
MethadoneThe metabolism of Epinastine can be decreased when 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, Investigational
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Epinastine.Experimental
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Epinastine.Approved
MethylergometrineMethylergometrine may increase the hypertensive and vasoconstricting activities of Epinastine.Approved
MethylphenidateThe therapeutic efficacy of Methylphenidate can be decreased when used in combination with Epinastine.Approved, Investigational
MetoclopramideThe risk or severity of QTc prolongation can be increased when Metoclopramide is combined with Epinastine.Approved, Investigational
MibefradilThe metabolism of Epinastine can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Epinastine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidomafetamineMidomafetamine may decrease the sedative activities of Epinastine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Epinastine can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Epinastine can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the tachycardic activities of Epinastine.Approved, Investigational
MilrinoneMilrinone may increase the antiplatelet activities of Epinastine.Approved
MirabegronThe metabolism of Epinastine can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Epinastine can be decreased when it is combined with Mitotane.Approved
MMDAMMDA may decrease the sedative activities of Epinastine.Experimental, Illicit
MoxifloxacinThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Moxifloxacin.Approved, Investigational
NadroparinEpinastine may increase the anticoagulant activities of Nadroparin.Approved, Investigational
NafamostatEpinastine may increase the anticoagulant activities of Nafamostat.Approved, 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
NetupitantThe serum concentration of Epinastine can be increased when it is combined with Netupitant.Approved, Investigational
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, Investigational
NicergolineNicergoline may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
NiguldipineThe serum concentration of Epinastine can be increased when it is combined with Niguldipine.Experimental
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Epinastine.Approved, Investigational
NimodipineThe serum concentration of Epinastine can be increased when it is combined with Nimodipine.Approved, Investigational
NisoldipineThe serum concentration of Epinastine can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Epinastine can be increased when it is combined with Nitrendipine.Approved, Investigational
NitroaspirinThe risk or severity of adverse effects can be increased when Epinastine is combined with Nitroaspirin.Investigational
NortriptylineNortriptyline may decrease the vasoconstricting activities of Epinastine.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Epinastine is combined with Obinutuzumab.Approved, Investigational
OlanzapineOlanzapine may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
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, Nutraceutical
OmeprazoleThe serum concentration of Epinastine can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Ondansetron.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
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Epinastine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Epinastine.Approved, Investigational, Vet Approved
OzagrelEpinastine may increase the anticoagulant activities of Ozagrel.Investigational
PalbociclibThe serum concentration of Epinastine can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidonePaliperidone may decrease the vasoconstricting activities of Epinastine.Approved
PanobinostatThe serum concentration of Epinastine can be increased when it is combined with Panobinostat.Approved, Investigational
ParnaparinEpinastine may increase the anticoagulant activities of Parnaparin.Approved, Investigational
ParomomycinThe risk or severity of adverse effects can be increased when Paromomycin is combined with Epinastine.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when Epinastine is combined with Paroxetine.Approved, Investigational
PazopanibEpinastine can cause a decrease in the absorption of Pazopanib resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Peginterferon alfa-2bThe serum concentration of Epinastine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Penfluridol is combined with Epinastine.Experimental
Pentaerythritol TetranitrateEpinastine may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
PentobarbitalThe metabolism of Epinastine can be increased when combined with Pentobarbital.Approved, Investigational, 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
PhenindioneEpinastine may increase the anticoagulant activities of Phenindione.Approved, Investigational
PheniramineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Pheniramine.Approved
PhenobarbitalThe metabolism of Epinastine can be increased when combined with Phenobarbital.Approved, Investigational
PhenoxybenzaminePhenoxybenzamine may decrease the vasoconstricting activities of Epinastine.Approved
PhenprocoumonEpinastine may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenterminePhentermine may decrease the sedative activities of Epinastine.Approved, Illicit
PhentolaminePhentolamine may decrease the vasoconstricting activities of Epinastine.Approved
Phenyl aminosalicylateThe risk or severity of adverse effects can be increased when Epinastine is combined with Phenyl aminosalicylate.Approved
PhenytoinThe metabolism of Epinastine can be increased when combined with Phenytoin.Approved, Vet Approved
PicotamideEpinastine may increase the anticoagulant activities of Picotamide.Experimental
PitolisantThe serum concentration of Pitolisant can be increased when it is combined with Epinastine.Approved, Investigational
PizotifenPizotifen may decrease the vasoconstricting activities of Epinastine.Approved
PosaconazoleThe serum concentration of Posaconazole can be decreased when it is combined with Epinastine.Approved, Investigational, Vet Approved
Potassium CitrateEpinastine may increase the anticoagulant activities of Potassium Citrate.Approved, Investigational, Vet Approved
PramipexoleEpinastine may increase the sedative activities of Pramipexole.Approved, Investigational
PrasugrelEpinastine may increase the anticoagulant activities of Prasugrel.Approved
PrazosinPrazosin may decrease the vasoconstricting activities of Epinastine.Approved
PregabalinThe therapeutic efficacy of Epinastine can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrimidoneThe metabolism of Epinastine can be increased when combined with Primidone.Approved, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Epinastine.Approved, Vet Approved
PromazineThe metabolism of Epinastine can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Epinastine.Approved, Investigational
PropafenoneThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Propafenone.Approved
PropericiazinePropericiazine may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
PropiomazinePropiomazine may decrease the vasoconstricting activities of Epinastine.Approved
PropiverinePropiverine may decrease the vasoconstricting activities of Epinastine.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
PseudoephedrinePseudoephedrine may decrease the sedative and stimulatory activities of Epinastine.Approved
PyrantelThe risk or severity of adverse effects can be increased when Pyrantel is combined with Epinastine.Approved, Vet Approved
QuazepamThe serum concentration of Epinastine can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Quetiapine.Approved
QuinidineThe metabolism of Epinastine can be decreased when combined with Quinidine.Approved, Investigational
QuinineThe metabolism of Epinastine can be decreased when combined with Quinine.Approved
RacepinephrineRacepinephrine may decrease the vasoconstricting activities of Epinastine.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
RelcovaptanEpinastine may increase the antiplatelet activities of Relcovaptan.Investigational
ResveratrolEpinastine may increase the antiplatelet activities of Resveratrol.Approved, Experimental, Investigational
ReteplaseEpinastine may increase the anticoagulant activities of Reteplase.Approved, Investigational
ReviparinEpinastine may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelEpinastine may increase the antiplatelet activities of Ridogrel.Approved
RifabutinThe metabolism of Epinastine can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Epinastine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Epinastine can be increased when combined with Rifapentine.Approved, Investigational
RisedronateEpinastine can cause an increase in the absorption of Risedronate resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved, Investigational
RisperidoneRisperidone may decrease the vasoconstricting activities of 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
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Epinastine.Approved
RolapitantThe metabolism of Epinastine can be decreased when combined with Rolapitant.Approved, Investigational
RucaparibThe metabolism of Epinastine can be decreased when combined with Rucaparib.Approved, Investigational
SalbutamolThe risk or severity of QTc prolongation can be increased when Salbutamol is combined with Epinastine.Approved, Vet Approved
SalmeterolThe risk or severity of QTc prolongation can be increased when Salmeterol is combined with Epinastine.Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Epinastine.Approved, Investigational
SarilumabThe therapeutic efficacy of Epinastine can be decreased when used in combination with Sarilumab.Approved, Investigational
SarpogrelateEpinastine may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseEpinastine may increase the anticoagulant activities of Saruplase.Experimental
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Epinastine.Approved, Investigational
SelexipagEpinastine may increase the anticoagulant activities of Selexipag.Approved
SertralineThe metabolism of Epinastine can be decreased when 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
SilodosinSilodosin may decrease the vasoconstricting activities of Epinastine.Approved
SiltuximabThe serum concentration of Epinastine can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Epinastine can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Epinastine can be decreased when combined with Sorafenib.Approved, Investigational
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.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Epinastine can be increased when it is combined with Stiripentol.Approved
StreptokinaseEpinastine may increase the anticoagulant activities of Streptokinase.Approved, Investigational
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 risk or severity of adverse effects can be increased when Sumatriptan is combined with Epinastine.Approved, Investigational
TamsulosinTamsulosin may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
TelaprevirThe metabolism of Epinastine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Epinastine can be decreased when combined with Telithromycin.Approved
TenecteplaseEpinastine may increase the anticoagulant activities of Tenecteplase.Approved
TerazosinTerazosin may decrease the vasoconstricting activities of Epinastine.Approved
TerodilineThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Terodiline.Experimental
TesmilifeneEpinastine may increase the antiplatelet activities of Tesmilifene.Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Tetracycline is combined with Epinastine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Epinastine.Investigational
TetrandrineThe serum concentration of Epinastine can be increased when it is combined with Tetrandrine.Experimental
ThioproperazineThioproperazine may decrease the vasoconstricting activities of Epinastine.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Epinastine.Approved, Withdrawn
ThiotepaThe metabolism of Epinastine can be decreased when combined with Thiotepa.Approved, Investigational
TicagrelorEpinastine may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineThe metabolism of Epinastine can be decreased when combined with Ticlopidine.Approved
TinzaparinEpinastine may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolEpinastine may increase the anticoagulant activities of Tioclomarol.Experimental
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
TolazolineTolazoline may decrease the vasoconstricting activities of Epinastine.Approved, Vet Approved
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Epinastine.Approved
TositumomabThe risk or severity of adverse effects can be increased when Epinastine is combined with Tositumomab.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Epinastine.Approved, Investigational
TranylcypromineThe metabolism of Epinastine can be decreased when combined with Tranylcypromine.Approved, Investigational
TrapidilEpinastine may increase the antiplatelet activities of Trapidil.Approved
TrazodoneTrazodone may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
TreprostinilEpinastine may increase the anticoagulant activities of Treprostinil.Approved, Investigational
TrifluoperazineTrifluoperazine may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
TriflusalEpinastine may increase the anticoagulant activities of Triflusal.Approved, Investigational
TrimazosinTrimazosin may decrease the vasoconstricting activities of Epinastine.Experimental
TrimethadioneThe risk or severity of adverse effects can be increased when Trimethadione is combined with Epinastine.Approved
TrimipramineTrimipramine may decrease the vasoconstricting activities of Epinastine.Approved
TroxerutinEpinastine may increase the anticoagulant activities of Troxerutin.Investigational
UrapidilUrapidil may decrease the vasoconstricting activities of Epinastine.Investigational
UrokinaseEpinastine may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
Valproic AcidThe risk or severity of QTc prolongation can be increased when Epinastine is combined with Valproic Acid.Approved, Investigational
VancomycinThe risk or severity of adverse effects can be increased when Vancomycin is combined with Epinastine.Approved
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Epinastine.Approved, Investigational
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Epinastine.Approved
VemurafenibThe serum concentration of Epinastine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Epinastine can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Epinastine can be increased when it is combined with Verapamil.Approved
VinpocetineThe risk or severity of adverse effects can be increased when Vinpocetine is combined with Epinastine.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
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Epinastine.Approved
ZiprasidoneThe metabolism of Epinastine can be decreased when combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Epinastine.Approved, Investigational
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Epinastine.Approved, Investigational
ZuclopenthixolZuclopenthixol may decrease the vasoconstricting activities of Epinastine.Approved, Investigational
Food Interactions
Not 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
Human Metabolome Database
HMDB0014889
KEGG Drug
D01713
PubChem Compound
3241
PubChem Substance
46509056
ChemSpider
3128
BindingDB
50131441
ChEBI
51032
ChEMBL
CHEMBL1106
Therapeutic Targets Database
DAP001074
PharmGKB
PA164764489
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Epinastine
ATC Codes
R06AX24 — EpinastineS01GX10 — Epinastine
FDA label
Download (113 KB)
MSDS
Download (57 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers3
2CompletedTreatmentAllergic Rhinitis (AR)1
3CompletedNot AvailableConjunctivitis, Seasonal Allergic1
3CompletedTreatmentRhinitis, Allergic, Perennial1
4CompletedTreatmentConjunctivitis, Seasonal Allergic2
4CompletedTreatmentHypersensitivity / Ocular Allergy1
4WithdrawnTreatmentConjunctivitis, Seasonal Allergic1
Not AvailableCompletedNot AvailableConjunctivitis, Seasonal Allergic1
Not AvailableCompletedNot AvailableRhinitis, Allergic, Perennial2
Not AvailableCompletedNot AvailableUrticarias1

Pharmacoeconomics

Manufacturers
  • Allergan inc
Packagers
  • Allergan Inc.
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)
US7429602No2000-11-292020-11-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)205-208 °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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzazepines
Sub Class
Dibenzazepines
Direct Parent
Dibenzazepines
Alternative Parents
Azepines / Benzenoids / Imidazolines / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Dibenzazepine / Azepine / Benzenoid / 2-imidazoline / Guanidine / Azacycle / Organic 1,3-dipolar compound / Propargyl-type 1,3-dipolar organic compound / Carboximidamide / Organic nitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
guanidines, benzazepine (CHEBI:51032)

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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
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 diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
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 ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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
Substrate
Inhibitor
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on August 02, 2018 07:46