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Identification
NameAsenapine
Accession NumberDB06216
TypeSmall Molecule
GroupsApproved
DescriptionDeveloped by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Asenapine also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009.
Structure
Thumb
Synonyms
Saphris
External Identifiers
  • ORG-5222
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SaphrisTablet10 mg/1SublingualSTAT Rx USA LLC2009-08-14Not applicableUs
SaphrisTablet5 mg/1SublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs
SaphrisTablet2.5 mg/1SublingualForest Laboratories, Inc.2014-12-30Not applicableUs
SaphrisTablet5 mgSublingualMerck Canada Inc2011-12-19Not applicableCanada
SaphrisTablet10 mg/1SublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs
SaphrisTablet5 mg/1SublingualForest Laboratories, Inc.2013-09-30Not applicableUs
SaphrisTablet10 mgSublingualMerck Canada Inc2011-12-19Not applicableCanada
SaphrisTablet5 mg/1SublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs
SaphrisTablet10 mg/1SublingualForest Laboratories, Inc.2013-09-30Not applicableUs
SaphrisTablet10 mg/1SublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs
SycrestTablet10 mgSublingualN.V. Organon2010-09-01Not applicableEu
SycrestTablet5 mgSublingualN.V. Organon2010-09-01Not applicableEu
SycrestTablet5 mgSublingualN.V. Organon2010-09-01Not applicableEu
SycrestTablet10 mgSublingualN.V. Organon2010-09-01Not applicableEu
SycrestTablet5 mgSublingualN.V. Organon2010-09-01Not applicableEu
SycrestTablet10 mgSublingualN.V. Organon2010-09-01Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Sycrest Lundbeck
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Asenapine Maleate
Thumb
  • InChI Key: GMDCDXMAFMEDAG-CHHFXETESA-N
  • Monoisotopic Mass: 401.103000462
  • Average Mass: 401.84
DBSALT000010
Categories
UNIIJKZ19V908O
CAS number65576-45-6
WeightAverage: 401.84
Monoisotopic: 401.103000462
Chemical FormulaC21H20ClNO5
InChI KeyGMDCDXMAFMEDAG-BTJKTKAUSA-N
InChI
InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
IUPAC Name
(2Z)-but-2-enedioic acid; 17-chloro-4-methyl-13-oxa-4-azatetracyclo[12.4.0.0²,⁶.0⁷,¹²]octadeca-1(14),7,9,11,15,17-hexaene
SMILES
OC(=O)\C=C/C(O)=O.CN1CC2C(C1)C1=C(OC3=CC=CC=C23)C=CC(Cl)=C1
Pharmacology
IndicationUsed for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination.
Structured Indications
PharmacodynamicsAsenapine is a serotonin, dopamine, noradrenaline, and histamine antagonist in which asenapine possess more potent activity with serotonin receptors than dopamine. Sedation in patients is associated with asenapine's antagonist activity at histamine receptors. Its lower incidence of extrapyramidal effects are associated with the upregulation of D1 receptors. This upregulation occurs due to asenapine's dose-dependent effects on glutamate transmission in the brain. It does not have any significant activity with muscarinic, cholinergic receptors therefore symptoms associated with anticholinergic drug activity like dry mouth or constipation are not expected to be observed. Asenapine has a higher affinity for all aforementioned receptors compared to first-generation and second-generation antipsychotics except for 5-HT1A and 5-HT1B receptors.
Mechanism of actionAsenapine is an atypical antipsychotic multireceptor neuroleptic drug which shows strong 5HT2A (serotonin) and D2 (dopamine) receptor antagonism, which has been shown to enhance dopamine (DA) and acetylcholine (Ach) efflux in rat brains. Asenapine may improve cognitive function and negative symptoms in patients with schizophrenia.
TargetKindPharmacological actionActionsOrganismUniProt ID
D(2) dopamine receptorProteinyes
antagonist
HumanP14416 details
5-hydroxytryptamine receptor 2AProteinyes
antagonist
HumanP28223 details
5-hydroxytryptamine receptor 1AProteinunknown
antagonist
HumanP08908 details
5-hydroxytryptamine receptor 1BProteinunknown
antagonist
HumanP28222 details
5-hydroxytryptamine receptor 2BProteinunknown
antagonist
HumanP41595 details
5-hydroxytryptamine receptor 2CProteinunknown
antagonist
HumanP28335 details
5-hydroxytryptamine receptor 5AProteinunknown
antagonist
HumanP47898 details
5-hydroxytryptamine receptor 6Proteinunknown
antagonist
HumanP50406 details
5-hydroxytryptamine receptor 7Proteinunknown
antagonist
HumanP34969 details
Alpha-2A adrenergic receptorProteinunknown
antagonist
HumanP08913 details
Alpha-2B adrenergic receptorProteinunknown
antagonist
HumanP18089 details
Alpha-2C adrenergic receptorProteinunknown
antagonist
HumanP18825 details
Alpha-1A adrenergic receptorProteinunknown
antagonist
HumanP35348 details
D(1A) dopamine receptorProteinunknown
antagonist
HumanP21728 details
D(3) dopamine receptorProteinunknown
antagonist
HumanP35462 details
D(4) dopamine receptorProteinunknown
antagonist
HumanP21917 details
Histamine H1 receptorProteinunknown
antagonist
HumanP35367 details
Histamine H2 receptorProteinunknown
antagonist
HumanP25021 details
Beta-1 adrenergic receptorProteinunknown
antagonist
HumanP08588 details
Beta-2 adrenergic receptorProteinunknown
antagonist
HumanP07550 details
Related Articles
AbsorptionCmax, single 5 mg dose = 4 ng/mL (within 1 hour); Bioavailability, sublingual administration = 35%; Bioavailability, oral administration (swallowed) = <2%; Time to steady state, 5 mg = 3 days; Peak plasma concentration occurs within 0.5 to 1.5 hours. Doubling dose of asenapine results in 1.7-fold increase in maximum concentration and exposure. Drinking water within 2-5 minutes post administration of asenapine results in a decrease in exposure.
Volume of distribution

20-25 L/kg

Protein binding95% protein bound
Metabolism

Asenapine is oxidized via CYP1A2 and undergoes direct glucuronidation via UGT1A4. Oxidation via CYP1A2 is asenapine's primary mode of metabolism.

Route of eliminationUrine (50%) and feces (50%)
Half life24 hours (range of 13.4 - 39.2 hours)
ClearanceNot Available
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
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Asenapine is combined with 1,1,1,2 Tetrafluoroethane.Investigational
2,5-Dimethoxy-4-ethylamphetamineAsenapine may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.Experimental, Illicit
3,4-MethylenedioxyamphetamineAsenapine may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.Experimental, Illicit
3,4-MethylenedioxymethamphetamineAsenapine may decrease the stimulatory activities of 3,4-Methylenedioxymethamphetamine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamineAsenapine may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Asenapine.Experimental
AbirateroneThe serum concentration of Asenapine can be increased when it is combined with Abiraterone.Approved
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Asenapine.Approved, Investigational
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Asenapine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Asenapine.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Asenapine.Withdrawn
adipiplonThe risk or severity of adverse effects can be increased when Asenapine is combined with adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Asenapine is combined with Agomelatine.Approved, Investigational
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Asenapine.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Asenapine.Approved, Illicit
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Asenapine.Approved, Investigational
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Asenapine.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Asenapine.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Asenapine.Approved, Illicit, Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Asenapine.Approved
AmiodaroneAmiodarone may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Amisulpride.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Asenapine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Asenapine.Approved, Illicit
AmoxapineAmoxapine may increase the QTc-prolonging activities of Asenapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Asenapine is combined with Amperozide.Experimental
AmphetamineAsenapine may decrease the stimulatory activities of Amphetamine.Approved, Illicit
AnagrelideAnagrelide may increase the QTc-prolonging activities of Asenapine.Approved
ApomorphineApomorphine may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
AprepitantThe serum concentration of Asenapine can be increased when it is combined with Aprepitant.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
ArtemetherAsenapine may increase the QTc-prolonging activities of Artemether.Approved
ArticaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Articaine.Approved
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Asenapine.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Asenapine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Azaperone.Vet Approved
AzelastineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Asenapine is combined with Azelastine.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Asenapine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Asenapine is combined with Baclofen.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Asenapine.Investigational
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Asenapine.Illicit
BedaquilineBedaquiline may increase the QTc-prolonging activities of Asenapine.Approved
BenperidolThe risk or severity of adverse effects can be increased when Asenapine is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Asenapine.Approved
BenzphetamineAsenapine may decrease the stimulatory activities of Benzphetamine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Asenapine is combined with Benzyl alcohol.Approved
BexaroteneThe serum concentration of Asenapine can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Asenapine can be decreased when combined with Boceprevir.Approved
BortezomibBortezomib may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
BosentanThe serum concentration of Asenapine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Asenapine.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Asenapine is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Asenapine.Approved, Illicit
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Asenapine.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Asenapine is combined with Brotizolam.Approved, Withdrawn
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Asenapine.Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Asenapine.Approved, Investigational
BuprenorphineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Asenapine.Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Asenapine.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Asenapine.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Asenapine is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Asenapine is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Asenapine.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Asenapine.Approved, Illicit, Vet Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Asenapine.Approved
CaffeineThe metabolism of Asenapine can be decreased when combined with Caffeine.Approved
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Asenapine.Approved
CarbamazepineThe metabolism of Asenapine can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Asenapine.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Asenapine is combined with Carisoprodol.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Asenapine.Experimental
CefditorenThe serum concentration of Cefditoren can be decreased when it is combined with Asenapine.Approved
CefpodoximeAsenapine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Vet Approved
CefuroximeAsenapine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CeritinibThe serum concentration of Asenapine can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Asenapine.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Asenapine.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Asenapine.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Asenapine.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Chlorphenamine.Approved
ChlorphentermineAsenapine may decrease the stimulatory activities of Chlorphentermine.Illicit, Withdrawn
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Asenapine.Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Asenapine.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Chlorzoxazone.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Asenapine.Experimental
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Asenapine.Approved, Vet Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
CisaprideCisapride may increase the QTc-prolonging activities of Asenapine.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the QTc-prolonging activities of Asenapine.Approved
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Asenapine.Approved
ClemastineThe metabolism of Asenapine can be decreased when combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Asenapine is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Asenapine is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Asenapine is combined with clomethiazole.Investigational
ClomipramineClomipramine may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Asenapine.Approved, Illicit
ClotrimazoleThe metabolism of Asenapine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the QTc-prolonging activities of Asenapine.Approved
CobicistatThe metabolism of Asenapine can be decreased when combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Asenapine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Asenapine.Approved, Illicit
ConivaptanThe serum concentration of Asenapine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibCrizotinib may increase the QTc-prolonging activities of Asenapine.Approved
CyclizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Asenapine.Approved
CyclosporineThe metabolism of Asenapine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyproheptadine.Approved
Cyproterone acetateThe serum concentration of Asenapine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
CysteamineThe therapeutic efficacy of Cysteamine can be decreased when used in combination with Asenapine.Approved, Investigational
DabrafenibThe serum concentration of Asenapine can be decreased when it is combined with Dabrafenib.Approved
DantroleneThe risk or severity of adverse effects can be increased when Asenapine is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Asenapine.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dapoxetine.Investigational
DarunavirThe metabolism of Asenapine can be decreased when combined with Darunavir.Approved
DasatinibAsenapine 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 Asenapine can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Asenapine.Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Asenapine.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Asenapine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when Asenapine is combined with deramciclane.Investigational
DesfluraneDesflurane may increase the QTc-prolonging activities of Asenapine.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Asenapine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Asenapine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Detomidine.Vet Approved
DexamethasoneThe serum concentration of Asenapine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Asenapine.Approved, Vet Approved
DexmethylphenidateAsenapine can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved
DextroamphetamineAsenapine may decrease the stimulatory activities of Dextroamphetamine.Approved, Illicit
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Asenapine.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Asenapine.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Asenapine.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Asenapine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Asenapine.Approved, Illicit, Vet Approved
DiethylpropionAsenapine may decrease the stimulatory activities of Diethylpropion.Approved, Illicit
DifenoxinThe risk or severity of adverse effects can be increased when Asenapine is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Asenapine.Approved, Illicit
DihydroergotamineThe metabolism of Asenapine can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Asenapine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Asenapine.Experimental, Illicit
DiltiazemThe metabolism of Asenapine can be decreased when combined with Diltiazem.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Asenapine is combined with Dimenhydrinate.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Asenapine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Asenapine.Approved, Illicit
DisopyramideDisopyramide may increase the QTc-prolonging activities of Asenapine.Approved
DofetilideDofetilide may increase the QTc-prolonging activities of Asenapine.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Asenapine.Approved
DomperidoneDomperidone may increase the QTc-prolonging activities of Asenapine.Approved, Investigational, Vet Approved
DoramectinThe risk or severity of adverse effects can be increased when Asenapine is combined with Doramectin.Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Asenapine.Approved
DoxycyclineThe metabolism of Asenapine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Asenapine is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Illicit
DronedaroneDronedarone may increase the QTc-prolonging activities of Asenapine.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Asenapine.Experimental, Illicit
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Asenapine.Approved
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Asenapine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Asenapine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Asenapine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Asenapine.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Asenapine is combined with Ecopipam.Investigational
EfavirenzThe serum concentration of Asenapine can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Asenapine.Approved, Investigational
EliglustatAsenapine may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Asenapine.Approved
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Asenapine.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Asenapine is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Asenapine can be decreased when it is combined with Enzalutamide.Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Asenapine.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Asenapine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Asenapine.Approved
EribulinEribulin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Asenapine.Approved, Investigational
ErythromycinErythromycin may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
EscitalopramEscitalopram may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Asenapine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Asenapine.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Asenapine.Approved
EthanolAsenapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Asenapine.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Asenapine.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Asenapine.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Asenapine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Asenapine is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Asenapine is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Asenapine.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Asenapine.Illicit, Vet Approved
EtravirineThe serum concentration of Asenapine can be decreased when it is combined with Etravirine.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Asenapine.Approved, Investigational
EzogabineEzogabine may increase the QTc-prolonging activities of Asenapine.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Asenapine.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Asenapine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Asenapine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Asenapine.Approved, Illicit, Investigational, Vet Approved
Ferric CarboxymaltoseAsenapine can cause a decrease in the absorption of Ferric Carboxymaltose resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ferric CitrateAsenapine can cause a decrease in the absorption of Ferric Citrate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ferric pyrophosphateAsenapine 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 Asenapine.Approved
FexofenadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Fexofenadine.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Asenapine.Approved, Withdrawn
FlibanserinThe risk or severity of adverse effects can be increased when Asenapine is combined with Flibanserin.Approved
FluconazoleFluconazole may increase the QTc-prolonging activities of Asenapine.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Asenapine.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Asenapine.Approved, Illicit
FluoxetineFluoxetine may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
FlupentixolFlupentixol may increase the QTc-prolonging activities of Asenapine.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Asenapine.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Asenapine.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Asenapine.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Asenapine is combined with Fluticasone Propionate.Approved
FluvoxamineThe serum concentration of Asenapine can be increased when it is combined with Fluvoxamine.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
FosamprenavirThe serum concentration of Fosamprenavir can be decreased when it is combined with Asenapine.Approved
FosaprepitantThe serum concentration of Asenapine can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Asenapine.Approved
FosphenytoinThe metabolism of Asenapine can be increased when combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Asenapine is combined with Fospropofol.Approved, Illicit
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Asenapine.Approved, Investigational
Fusidic AcidThe serum concentration of Asenapine can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Asenapine.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Asenapine is combined with gabapentin enacarbil.Approved
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Asenapine.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Asenapine.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Asenapine.Approved, Illicit
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Asenapine.Approved, Investigational
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
GepironeThe risk or severity of adverse effects can be increased when Asenapine is combined with Gepirone.Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Asenapine.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Asenapine.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Asenapine.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Asenapine.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Asenapine.Approved
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Asenapine.Approved, Illicit
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Asenapine.Approved
GoserelinGoserelin may increase the QTc-prolonging activities of Asenapine.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
GuanfacineThe risk or severity of adverse effects can be increased when Asenapine is combined with Guanfacine.Approved, Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Asenapine.Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Asenapine.Approved, Illicit, Withdrawn
HaloperidolHaloperidol may increase the QTc-prolonging activities of Asenapine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Asenapine.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Asenapine.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Asenapine.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Asenapine.Approved
HydrocodoneAsenapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Asenapine.Approved, Illicit
Hydroxyamphetamine hydrobromideAsenapine may decrease the stimulatory activities of Hydroxyamphetamine hydrobromide.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
IbutilideIbutilide may increase the QTc-prolonging activities of Asenapine.Approved
IdelalisibThe serum concentration of Asenapine can be increased when it is combined with Idelalisib.Approved
IloperidoneIloperidone may increase the QTc-prolonging activities of Asenapine.Approved
ImatinibThe metabolism of Asenapine can be decreased when combined with Imatinib.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Asenapine.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Asenapine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Asenapine is combined with Indalpine.Investigational, Withdrawn
IndapamideIndapamide may increase the QTc-prolonging activities of Asenapine.Approved
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Asenapine.Approved
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Asenapine.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Asenapine.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Asenapine.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Asenapine.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Asenapine.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Asenapine.Approved
IronAsenapine can cause a decrease in the absorption of Iron resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Iron DextranAsenapine 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 saccharateAsenapine 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 Asenapine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Asenapine.Approved
IsofluraneIsoflurane may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Asenapine.Approved
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Asenapine.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Asenapine.Approved
IvacaftorThe serum concentration of Asenapine can be increased when it is combined with Ivacaftor.Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Asenapine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Asenapine.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Ketobemidone.Approved
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Asenapine.Approved, Investigational
KetoconazoleThe metabolism of Asenapine can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Asenapine is combined with Lamotrigine.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Asenapine.Approved
LenvatinibLenvatinib may increase the QTc-prolonging activities of Asenapine.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Asenapine is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Asenapine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocetirizine.Approved
LevodopaThe therapeutic efficacy of Levodopa can be decreased when used in combination with Asenapine.Approved
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Asenapine.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Asenapine.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Asenapine.Approved
LidocaineThe metabolism of Asenapine can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Asenapine.Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Asenapine.Approved, Investigational
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Asenapine.Approved
LisdexamfetamineAsenapine may decrease the stimulatory activities of Lisdexamfetamine.Approved, Investigational
LithiumLithium may increase the neurotoxic activities of Asenapine.Approved
LofentanilThe risk or severity of adverse effects can be increased when Asenapine is combined with Lofentanil.Illicit
LopinavirLopinavir may increase the QTc-prolonging activities of Asenapine.Approved
LoratadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Asenapine.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Asenapine.Approved
LovastatinThe metabolism of Asenapine can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Asenapine.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Lu AA21004 is combined with Asenapine.Investigational
LuliconazoleThe serum concentration of Asenapine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Asenapine can be increased when combined with Lumacaftor.Approved
LumefantrineAsenapine may increase the QTc-prolonging activities of Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Vet Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Asenapine.Approved
MeclizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Medetomidine.Vet Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Asenapine.Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Asenapine.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Melperone.Approved
MephedroneAsenapine may decrease the stimulatory activities of Mephedrone.Investigational
MephentermineAsenapine may decrease the stimulatory activities of Mephentermine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Asenapine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Asenapine.Approved, Illicit
MequitazineAsenapine may increase the arrhythmogenic activities of Mequitazine.Approved
MesalazineThe therapeutic efficacy of Mesalazine can be decreased when used in combination with Asenapine.Approved
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Asenapine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Metaxalone.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Asenapine.Approved
MethadoneMethadone may increase the QTc-prolonging activities of Asenapine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Asenapine.Approved, Illicit
MethamphetamineAsenapine may decrease the stimulatory activities of Methamphetamine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Asenapine.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Asenapine.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Asenapine is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Asenapine.Approved
MethotrimeprazineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Asenapine.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Asenapine is combined with Methsuximide.Approved
MethylphenidateThe risk or severity of adverse effects can be increased when Asenapine is combined with Methylphenidate.Approved, Investigational
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Asenapine.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Asenapine.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Asenapine.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Asenapine.Approved
MetyrosineAsenapine may increase the sedative activities of Metyrosine.Approved
MexiletineThe metabolism of Asenapine can be decreased when combined with Mexiletine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Asenapine.Approved, Illicit
MifepristoneMifepristone may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Asenapine.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Asenapine.Approved
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Asenapine.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Investigational
MirabegronMirabegron may increase the QTc-prolonging activities of Asenapine.Approved
MirtazapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Asenapine.Approved, Investigational
MitotaneThe serum concentration of Asenapine can be decreased when it is combined with Mitotane.Approved
MMDAAsenapine may decrease the stimulatory activities of MMDA.Experimental, Illicit
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Asenapine.Approved
ModafinilThe serum concentration of Asenapine can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Asenapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Asenapine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Asenapine.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Investigational
NafcillinThe serum concentration of Asenapine can be decreased when it is combined with Nafcillin.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Asenapine.Approved
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Asenapine.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Asenapine.Approved, Investigational
NefazodoneThe metabolism of Asenapine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Asenapine.Approved
NetupitantThe serum concentration of Asenapine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Asenapine can be increased when combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Asenapine.Approved
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Asenapine.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Asenapine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Asenapine is combined with Nitrous oxide.Approved, Vet Approved
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Asenapine.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Normethadone.Approved, Illicit
NortriptylineNortriptyline may increase the QTc-prolonging activities of Asenapine.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Asenapine.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
OlaparibThe metabolism of Asenapine can be decreased when combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Asenapine.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Olopatadine.Approved
OndansetronOndansetron may increase the QTc-prolonging activities of Asenapine.Approved
OpiumThe risk or severity of adverse effects can be increased when Asenapine is combined with Opium.Approved, Illicit
OrphenadrineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Asenapine.Investigational
OsimertinibThe serum concentration of Asenapine can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Asenapine.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Asenapine.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Asenapine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Asenapine.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Asenapine.Approved, Investigational, Vet Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
PalbociclibThe serum concentration of Asenapine can be increased when it is combined with Palbociclib.Approved
PaliperidonePaliperidone may increase the QTc-prolonging activities of Asenapine.Approved
PanobinostatPanobinostat may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
ParaldehydeAsenapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineParoxetine may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Asenapine.Approved
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Asenapine.Approved
Peginterferon alfa-2bThe serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.Approved
PentamidinePentamidine may increase the QTc-prolonging activities of Asenapine.Approved
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Asenapine.Approved, Vet Approved
PentobarbitalThe metabolism of Asenapine can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
PerazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Perazine.Investigational
PerflutrenPerflutren may increase the QTc-prolonging activities of Asenapine.Approved
PerospironeThe risk or severity of adverse effects can be increased when Asenapine is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Asenapine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Asenapine.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Asenapine.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Asenapine.Approved, Withdrawn
PhenobarbitalThe metabolism of Asenapine can be increased when combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenoxyethanol.Approved
PhentermineAsenapine may decrease the stimulatory activities of Phentermine.Approved, Illicit
PhenytoinThe metabolism of Asenapine can be increased when combined with Phenytoin.Approved, Vet Approved
PimozidePimozide may increase the QTc-prolonging activities of Asenapine.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Asenapine.Approved, Investigational
PipamperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Pipotiazine.Approved
PiribedilThe therapeutic efficacy of Piribedil can be decreased when used in combination with Asenapine.Investigational
PiritramideThe risk or severity of adverse effects can be increased when Asenapine is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Asenapine is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Asenapine is combined with Pomalidomide.Approved
PosaconazoleThe serum concentration of Posaconazole can be decreased when it is combined with Asenapine.Approved, Investigational, Vet Approved
PramipexoleAsenapine may increase the sedative activities of Pramipexole.Approved, Investigational
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Asenapine.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Asenapine.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Asenapine.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Asenapine.Approved
PrimaquinePrimaquine may increase the QTc-prolonging activities of Asenapine.Approved
PrimidoneThe metabolism of Asenapine can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideProcainamide may increase the QTc-prolonging activities of Asenapine.Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Asenapine.Approved, Investigational, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Asenapine.Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Asenapine.Approved, Vet Approved
PromazinePromazine may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Asenapine.Approved
PropafenonePropafenone may increase the QTc-prolonging activities of Asenapine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Asenapine.Approved, Vet Approved
PropofolPropofol may increase the QTc-prolonging activities of Asenapine.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Propoxycaine.Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Asenapine.Approved
PSD502The risk or severity of adverse effects can be increased when Asenapine is combined with PSD502.Investigational
PseudoephedrineAsenapine may decrease the stimulatory activities of Pseudoephedrine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Asenapine.Approved, Illicit
QuetiapineQuetiapine may increase the QTc-prolonging activities of Asenapine.Approved
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Asenapine.Approved
QuinidineQuinidine may increase the QTc-prolonging activities of Asenapine.Approved
QuinineQuinine may increase the QTc-prolonging activities of Asenapine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Asenapine is combined with Ramelteon.Approved, Investigational
RanolazineRanolazine may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Asenapine.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Asenapine.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Asenapine.Approved, Withdrawn
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Asenapine.Approved, Investigational
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Asenapine.Approved
RifabutinThe metabolism of Asenapine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Asenapine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Asenapine can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Asenapine.Approved
RisedronateThe serum concentration of Risedronate can be increased when it is combined with Asenapine.Approved, Investigational
RisperidoneRisperidone may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Asenapine is combined with Ritanserin.Investigational
RitobegronAsenapine may decrease the stimulatory activities of Ritobegron.Investigational
RitonavirThe metabolism of Asenapine can be decreased when combined with Ritonavir.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Asenapine.Approved
RomifidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Romifidine.Vet Approved
RopiniroleAsenapine may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Asenapine.Approved
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Asenapine.Approved, Investigational
RotigotineAsenapine may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Asenapine.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Asenapine.Experimental
Sage 547The risk or severity of adverse effects can be increased when Asenapine is combined with Sage 547.Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Asenapine.Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Asenapine.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Asenapine.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Asenapine.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Asenapine.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Asenapine.Approved, Withdrawn
SertralineSertraline may increase the QTc-prolonging activities of Asenapine.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
SildenafilThe metabolism of Asenapine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Asenapine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Asenapine can be increased when it is combined with Simeprevir.Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Asenapine.Approved, Investigational
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
SolifenacinSolifenacin may increase the QTc-prolonging activities of Asenapine.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
SotalolSotalol may increase the QTc-prolonging activities of Asenapine.Approved
St. John's WortThe serum concentration of Asenapine can be decreased when it is combined with St. John&#39;s Wort.Nutraceutical
StiripentolThe serum concentration of Asenapine can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Asenapine.Approved, Investigational
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Asenapine.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Asenapine.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Asenapine is combined with Sulpiride.Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Asenapine.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
SuvorexantAsenapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TamoxifenTamoxifen may increase the QTc-prolonging activities of Asenapine.Approved
TandospironeThe risk or severity of adverse effects can be increased when Asenapine is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Asenapine is combined with Tasimelteon.Approved
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Asenapine.Approved
TelaprevirThe metabolism of Asenapine can be decreased when combined with Telaprevir.Approved
TelavancinTelavancin may increase the QTc-prolonging activities of Asenapine.Approved
TelithromycinTelithromycin may increase the QTc-prolonging activities of Asenapine.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Asenapine.Approved
TenofovirThe metabolism of Asenapine can be decreased when combined with Tenofovir.Approved, Investigational
TerbutalineTerbutaline may increase the QTc-prolonging activities of Asenapine.Approved
TeriflunomideThe serum concentration of Asenapine can be decreased when it is combined with Teriflunomide.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Asenapine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Asenapine.Investigational
ThalidomideAsenapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Asenapine can be decreased when combined with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Asenapine.Approved, Vet Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Asenapine.Investigational
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Asenapine.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Asenapine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Asenapine.Approved
TiagabineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Tiapride.Investigational
TiclopidineThe metabolism of Asenapine can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tiletamine.Vet Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Asenapine.Approved
TocilizumabThe serum concentration of Asenapine can be decreased when it is combined with Tocilizumab.Approved
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Asenapine.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Asenapine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Asenapine is combined with Tolcapone.Approved, Withdrawn
TolterodineTolterodine may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Asenapine is combined with Topiramate.Approved
ToremifeneToremifene may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Asenapine.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Asenapine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Asenapine.Approved
TrazodoneTrazodone may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Asenapine.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Asenapine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Asenapine.Approved, Vet Approved
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Asenapine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Triprolidine.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Asenapine.Approved, Vet Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Asenapine.Withdrawn
Uc1010The risk or severity of adverse effects can be increased when Asenapine is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Asenapine.Approved, Investigational
VandetanibVandetanib may increase the QTc-prolonging activities of Asenapine.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Asenapine.Approved
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Asenapine.Approved, Investigational
VemurafenibThe serum concentration of Asenapine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Asenapine.Approved
VerapamilThe metabolism of Asenapine can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Asenapine is combined with Vigabatrin.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Asenapine.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Asenapine.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Asenapine.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Asenapine.Approved, Investigational
VoriconazoleThe metabolism of Asenapine can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Asenapine is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Asenapine.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Asenapine is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Zimelidine.Withdrawn
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Asenapine.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Zolazepam.Vet Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Asenapine.Approved, Investigational
ZolpidemAsenapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Asenapine is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Asenapine.Approved
ZotepineThe risk or severity of adverse effects can be increased when Asenapine is combined with Zotepine.Approved
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
Food Interactions
  • Avoid water and food for at least 10 minutes post administration of asenapine
References
Synthesis Reference

DrugSyn.org

US4145434
General References
  1. Huang M, Li Z, Dai J, Shahid M, Wong EH, Meltzer HY: Asenapine increases dopamine, norepinephrine, and acetylcholine efflux in the rat medial prefrontal cortex and hippocampus. Neuropsychopharmacology. 2008 Nov;33(12):2934-45. doi: 10.1038/npp.2008.20. Epub 2008 Apr 16. [PubMed:18418367 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
  3. Franberg O, Wiker C, Marcus MM, Konradsson A, Jardemark K, Schilstrom B, Shahid M, Wong EH, Svensson TH: Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. Epub 2007 Oct 17. [PubMed:17940749 ]
  4. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
External Links
ATC CodesN05AH05
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (448 KB)
MSDSDownload (91.9 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9849
Blood Brain Barrier+0.8842
Caco-2 permeable+0.5605
P-glycoprotein substrateSubstrate0.7617
P-glycoprotein inhibitor INon-inhibitor0.9375
P-glycoprotein inhibitor IINon-inhibitor0.8901
Renal organic cation transporterNon-inhibitor0.7054
CYP450 2C9 substrateNon-substrate0.7964
CYP450 2D6 substrateNon-substrate0.7864
CYP450 3A4 substrateSubstrate0.5065
CYP450 1A2 substrateNon-inhibitor0.5212
CYP450 2C9 inhibitorNon-inhibitor0.7185
CYP450 2D6 inhibitorNon-inhibitor0.6781
CYP450 2C19 inhibitorNon-inhibitor0.5762
CYP450 3A4 inhibitorNon-inhibitor0.8625
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6005
Ames testNon AMES toxic0.5417
CarcinogenicityNon-carcinogens0.8694
BiodegradationNot ready biodegradable0.9894
Rat acute toxicity2.7083 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8125
hERG inhibition (predictor II)Non-inhibitor0.6697
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletSublingual10 mg/1
TabletSublingual10 mg
TabletSublingual2.5 mg/1
TabletSublingual5 mg/1
TabletSublingual5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5763476 Yes2000-12-092020-12-09Us
US7741358 Yes2006-10-062026-10-06Us
US8022228 Yes2006-10-062026-10-06Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP3.72ChemAxon
pKa (Strongest Basic)7.29ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity81.65 m3·mol-1ChemAxon
Polarizability30.9 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxepines
Sub ClassDibenzoxepines
Direct ParentDibenzoxepines
Alternative Parents
Substituents
  • Dibenzoxepine
  • Diaryl ether
  • Aralkylamine
  • Chlorobenzene
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • N-alkylpyrrolidine
  • Unsaturated fatty acid
  • Dicarboxylic acid or derivatives
  • Aryl halide
  • Aryl chloride
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Sep;666(1-3):43-52. doi: 10.1016/j.ejphar.2011.05.050. Epub 2011 Jun 1. [PubMed:21658377 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 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 modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
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.
Gene Name:
HTR5A
Uniprot ID:
P47898
Molecular Weight:
40254.69 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
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. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine 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 clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Sep;666(1-3):43-52. doi: 10.1016/j.ejphar.2011.05.050. Epub 2011 Jun 1. [PubMed:21658377 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity).
Gene Name:
UGT1A4
Uniprot ID:
P22310
Molecular Weight:
60024.535 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
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. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
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Drug created on March 19, 2008 10:17 / Updated on December 02, 2016 03:58