Identification

Name
Asenapine
Accession Number
DB06216
Type
Small Molecule
Groups
Approved
Description

Developed 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
Not Available
External IDs
ORG-5222
Product Ingredients
IngredientUNIICASInChI Key
Asenapine MaleateCU9463U2E285650-56-2GMDCDXMAFMEDAG-CHHFXETESA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SaphrisTablet5 mgSublingualMerck Ltd.2011-12-19Not applicableCanada
SaphrisTablet2.5 mg/1SublingualAllergan2014-12-30Not applicableUs
SaphrisTablet5 mg/1SublingualOrganon2009-08-13Not applicableUs
SaphrisTablet10 mg/1SublingualStat Rx USA2009-08-14Not applicableUs
SaphrisTablet10 mg/1SublingualOrganon2010-06-21Not applicableUs
SaphrisTablet10 mg/1SublingualOrganon2009-08-13Not applicableUs
SaphrisTablet10 mgSublingualMerck Ltd.2011-12-19Not applicableCanada
SaphrisTablet5 mg/1SublingualAllergan2013-09-30Not applicableUs
SaphrisTablet10 mg/1SublingualAllergan2013-09-30Not applicableUs
SaphrisTablet5 mg/1SublingualOrganon2010-06-21Not applicableUs
International/Other Brands
Saphris / Sycrest (Lundbeck )
Categories
UNII
JKZ19V908O
CAS number
65576-45-6
Weight
Average: 401.84
Monoisotopic: 401.103000462
Chemical Formula
C21H20ClNO5
InChI Key
GMDCDXMAFMEDAG-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

Indication

Used for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination.

Structured Indications
Pharmacodynamics

Asenapine 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 action

Asenapine 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.

TargetActionsOrganism
AD(2) dopamine receptor
antagonist
Human
A5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 1A
antagonist
Human
U5-hydroxytryptamine receptor 1B
antagonist
Human
U5-hydroxytryptamine receptor 2B
antagonist
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 5A
antagonist
Human
U5-hydroxytryptamine receptor 6
antagonist
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
UAlpha-2A adrenergic receptor
antagonist
Human
UAlpha-2B adrenergic receptor
antagonist
Human
UAlpha-2C adrenergic receptor
antagonist
Human
UAlpha-1A adrenergic receptor
antagonist
Human
UD(1A) dopamine receptor
antagonist
Human
UD(3) dopamine receptor
antagonist
Human
UD(4) dopamine receptor
antagonist
Human
UHistamine H1 receptor
antagonist
Human
UHistamine H2 receptor
antagonist
Human
UBeta-1 adrenergic receptor
antagonist
Human
UBeta-2 adrenergic receptor
antagonist
Human
Absorption

Cmax, 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 binding

95% 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 elimination

Urine (50%) and feces (50%)

Half life

24 hours (range of 13.4 - 39.2 hours)

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Asenapine.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
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 Asenapine is combined with 7-Nitroindazole.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 Asenapine is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Aceprometazine.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Asenapine.Investigational, 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
AICA ribonucleotideThe therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Asenapine.Experimental, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Asenapine is combined with Alaproclate.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
AllicinThe therapeutic efficacy of Allicin can be decreased when used in combination with Asenapine.Investigational
AllopregnanoloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Allopregnanolone.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 Asenapine is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Asenapine is combined with Alphaprodine.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
AmiodaroneThe metabolism of Asenapine can be decreased when combined with Amiodarone.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
AnagrelideThe risk or severity of QTc prolongation can be increased when Anagrelide is combined with 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 trioxideThe risk or severity of QTc prolongation can be increased when Arsenic trioxide is combined with Asenapine.Approved, Investigational
ArtemetherThe risk or severity of QTc prolongation can be increased when Asenapine is combined with 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.Investigational, Vet Approved
AzelastineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzithromycinThe metabolism of Asenapine can be decreased when combined with Azithromycin.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 Asenapine is combined with Barbital.Illicit
BedaquilineBedaquiline may increase the QTc-prolonging activities of Asenapine.Approved
Bempedoic acidThe therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Asenapine.Investigational
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 Asenapine is combined with Benzocaine.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
BoceprevirThe metabolism of Asenapine can be decreased when combined with Boceprevir.Approved, Withdrawn
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
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
BromisovalThe risk or severity of adverse effects can be increased when Asenapine is combined with Bromisoval.Experimental
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Asenapine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Asenapine is combined with Bromperidol.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, Investigational, Withdrawn
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Asenapine.Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Bupivacaine.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 Asenapine is combined with Butethal.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
CanertinibThe risk or severity of adverse effects can be increased when Asenapine is combined with Canertinib.Investigational
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
CarbutamideThe therapeutic efficacy of Carbutamide can be decreased when used in combination with Asenapine.Experimental
CarfentanilThe risk or severity of adverse effects can be increased when Asenapine is combined with Carfentanil.Illicit, Investigational, 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 Asenapine is combined with Chloral hydrate.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 Asenapine is combined with Chlormezanone.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Chloroprocaine.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
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with 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 Asenapine is combined with Chlorprothixene.Approved, Investigational, 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 Asenapine is combined with Cinchocaine.Approved, Vet Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Asenapine.Approved, Investigational
CisaprideThe risk or severity of QTc prolongation can be increased when Cisapride is combined with Asenapine.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Asenapine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Asenapine can be decreased when combined with Clarithromycin.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
ClopenthixolThe risk or severity of adverse effects can be increased when Asenapine is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Asenapine.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Asenapine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with 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 Asenapine is combined with Cocaine.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
CrizotinibThe metabolism of Asenapine can be decreased when combined with Crizotinib.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 Asenapine is combined with Dapiprazole.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
DasatinibThe serum concentration of Asenapine can be increased when it is combined with Dasatinib.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
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 Asenapine is combined with Dexmedetomidine.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 Asenapine is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Asenapine is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dezocine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Asenapine.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Asenapine is combined with Diethyl ether.Experimental
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 Asenapine is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dihydromorphine.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
DisopyramideThe risk or severity of QTc prolongation can be increased when Disopyramide is combined with Asenapine.Approved
DixyrazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dixyrazine.Experimental
DofetilideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Asenapine.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Asenapine.Approved
DomperidoneThe risk or severity of QTc prolongation can be increased when Domperidone is combined with Asenapine.Approved, Investigational, Vet Approved
DoramectinThe risk or severity of adverse effects can be increased when Asenapine is combined with Doramectin.Vet Approved
DosulepinThe metabolism of Asenapine can be decreased when combined with Dosulepin.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.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved, Illicit
DronedaroneThe metabolism of Asenapine can be decreased when combined with Dronedarone.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 Asenapine is combined with Drotebanol.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 Asenapine is combined with Dyclonine.Approved
EcgonineThe risk or severity of adverse effects can be increased when Asenapine is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Asenapine is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Asenapine is combined with Efavirenz.Approved, Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Asenapine.Approved, Investigational
EliglustatThe risk or severity of QTc prolongation can be increased when Asenapine is combined with Eliglustat.Approved
EltanoloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Eltanolone.Investigational
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 Asenapine is combined with Enflurane.Approved, Investigational, 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
ErythromycinThe metabolism of Asenapine can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Asenapine.Approved, Investigational
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 Asenapine is combined with Ethchlorvynol.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 Asenapine is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethyl chloride.Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethylmorphine.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.Investigational, 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 Asenapine is combined with Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Asenapine is combined with Etorphine.Illicit, Vet 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 Asenapine is combined with Fencamfamine.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, Investigational
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
FluanisoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Fluanisone.Experimental
FluconazoleFluconazole may increase the QTc-prolonging activities of Asenapine.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Fludiazepam.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 Asenapine is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Asenapine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with 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 Asenapine is combined with Fluspirilene.Approved, Investigational
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, Investigational
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, Investigational
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
GepefrineAsenapine may decrease the stimulatory activities of Gepefrine.Experimental
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.Investigational, 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, Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Asenapine is combined with Glutethimide.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 Asenapine is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Asenapine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Asenapine is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Asenapine is combined with Heroin.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Asenapine is combined with Hexobarbital.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
HydroxyamphetamineAsenapine may decrease the stimulatory activities of Hydroxyamphetamine.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
IbutilideThe risk or severity of QTc prolongation can be increased when Ibutilide is combined with Asenapine.Approved
IdelalisibThe serum concentration of Asenapine can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Iloperidone.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
IndiplonThe risk or severity of adverse effects can be increased when Asenapine is combined with Indiplon.Investigational
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 HumanThe therapeutic efficacy of Insulin Human can be decreased when used in combination with Asenapine.Approved, Investigational
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
Iofetamine I-123Asenapine may decrease the stimulatory activities of Iofetamine I-123.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 Asenapine is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Asenapine.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 Asenapine is combined with Levobupivacaine.Approved, Investigational
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 Asenapine is combined with Levomethadyl Acetate.Approved, Investigational
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
LobeglitazoneThe metabolism of Asenapine can be decreased when combined with Lobeglitazone.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Asenapine is combined with Lofentanil.Illicit
LopinavirThe metabolism of Asenapine can be decreased when combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Asenapine is combined with Loprazolam.Experimental
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
LormetazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Lormetazepam.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
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
LumefantrineThe risk or severity of QTc prolongation can be increased when Asenapine is combined with 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
MebicarThe risk or severity of adverse effects can be increased when Asenapine is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Medazepam.Experimental
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 Asenapine is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Melperone.Approved, Investigational
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 Asenapine is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Asenapine.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Asenapine is combined with Meptazinol.Experimental
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 Asenapine is combined with Mesoridazine.Approved, Investigational
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
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Asenapine.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Asenapine is combined with Methadyl Acetate.Approved, Illicit
MethamphetamineAsenapine may decrease the stimulatory activities of Methamphetamine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Asenapine is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Methaqualone.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 Asenapine is combined with Methoxyflurane.Approved, Investigational, Vet Approved
MethoxyphenamineAsenapine may decrease the stimulatory activities of Methoxyphenamine.Experimental
MethsuximideThe risk or severity of adverse effects can be increased when Asenapine is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Asenapine is combined with Methylecgonine.Experimental
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 Asenapine is combined with Methylphenobarbital.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
MidomafetamineAsenapine may decrease the stimulatory activities of Midomafetamine.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Asenapine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Asenapine can be increased when it is combined with Mifepristone.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
MoexiprilMoexipril may increase the QTc-prolonging activities of Asenapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Molindone.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
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
NorfluraneThe risk or severity of adverse effects can be increased when Asenapine is combined with Norflurane.Investigational
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
OndansetronThe risk or severity of adverse effects can be increased when Asenapine is combined with Ondansetron.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 Asenapine is combined with Osanetant.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
OxethazaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Oxethazaine.Approved, Investigational
OxprenololThe risk or severity of adverse effects can be increased when Asenapine is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Oxybuprocaine.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
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with 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, Investigational
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
PenfluridolThe risk or severity of adverse effects can be increased when Asenapine is combined with Penfluridol.Experimental
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
PhenazocineThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenazocine.Experimental
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, Investigational, Withdrawn
PhenibutThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Asenapine can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenoperidine.Experimental
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
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with 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, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Pipotiazine.Approved, Investigational
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 Asenapine is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Asenapine.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Prilocaine.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
ProcainamideThe risk or severity of QTc prolongation can be increased when Procainamide is combined with Asenapine.Approved
ProcaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Procaine.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
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Asenapine.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Asenapine.Approved
PropafenonePropafenone may increase the QTc-prolonging activities of Asenapine.Approved
PropanididThe risk or severity of adverse effects can be increased when Asenapine is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Proparacaine.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
ProxibarbalThe risk or severity of adverse effects can be increased when Asenapine is combined with Proxibarbal.Experimental
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
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Asenapine.Approved
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Asenapine.Approved
QuinidineThe risk or severity of QTc prolongation can be increased when Quinidine is combined with Asenapine.Approved
QuinineThe risk or severity of QTc prolongation can be increased when Quinine is combined with Asenapine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Quinisocaine.Experimental
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 Asenapine is combined with Remoxipride.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, Investigational
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
RitonavirRitonavir may increase the QTc-prolonging activities of Asenapine.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 Asenapine is combined with Ropivacaine.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
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
SepranoloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Asenapine is combined with Sertindole.Approved, Investigational, 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
SotagliflozinThe therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Asenapine.Investigational
SotalolThe risk or severity of QTc prolongation can be increased when Sotalol is combined with Asenapine.Approved
St. John's WortThe serum concentration of Asenapine can be decreased when it is combined with St. John&#39;s Wort.Investigational, 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
SulfisoxazoleThe metabolism of Asenapine can be decreased when combined with Sulfisoxazole.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, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Sultopride.Experimental
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, Withdrawn
TelavancinTelavancin may increase the QTc-prolonging activities of Asenapine.Approved
TelithromycinThe metabolism of Asenapine can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Asenapine.Approved
Tenofovir disoproxilThe metabolism of Asenapine can be decreased when combined with Tenofovir disoproxil.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
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Asenapine is combined with Tetrodotoxin.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 Asenapine is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Asenapine is combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Asenapine.Approved, Withdrawn
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.Approved, 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
TilidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tilidine.Experimental
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
ToremifeneThe risk or severity of QTc prolongation can be increased when Toremifene is combined with 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 Asenapine is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tranylcypromine.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
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Asenapine is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Asenapine is combined with Trichloroethylene.Experimental
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Asenapine.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Asenapine is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Triflupromazine.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.Investigational, Withdrawn
Valproic AcidThe risk or severity of adverse effects can be increased when Asenapine is combined with Valproic Acid.Approved, Investigational
VandetanibThe risk or severity of QTc prolongation can be increased when Vandetanib is combined with 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
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Asenapine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Veralipride.Experimental
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
Vinyl etherThe risk or severity of adverse effects can be increased when Asenapine is combined with Vinyl ether.Experimental
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
XenonThe risk or severity of adverse effects can be increased when Asenapine is combined with Xenon.Experimental
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
ZiprasidoneThe metabolism of Asenapine can be decreased when combined with Ziprasidone.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, Investigational
ZucapsaicinThe metabolism of Asenapine can be decreased when combined with Zucapsaicin.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Asenapine.Approved, Investigational
Food Interactions
  • Avoid water and food for at least 10 minutes post administration of asenapine

References

Synthesis Reference
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
KEGG Drug
D02995
PubChem Compound
11954293
PubChem Substance
175427062
ChemSpider
10128588
ChEBI
71253
ChEMBL
CHEMBL3544974
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Asenapine
ATC Codes
N05AH05 — Asenapine
AHFS Codes
  • 28:16.08.04 — Atypical Antipsychotics
FDA label
Download (448 KB)
MSDS
Download (91.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBipolar Disorder (BD) / Schizophrenic Disorders1
1CompletedTreatmentBipolar I Disorder / Schizophrenic Disorders1
2CompletedOtherPsychosis1
2RecruitingTreatmentDepression, Bipolar1
3CompletedTreatmentBipolar 1 Disorder2
3CompletedTreatmentBipolar Disorder (BD)7
3CompletedTreatmentBipolar Disorder, Pediatric1
3CompletedTreatmentBipolar I Disorder1
3CompletedTreatmentPsychosis1
3CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders2
3CompletedTreatmentSchizophrenia, Disorganized / Schizophrenia, paranoid type / Schizophrenia, Undifferentiated2
3CompletedTreatmentSchizophrenic Disorders14
3RecruitingTreatmentSchizophrenic Disorders1
3SuspendedTreatmentStuttering1
3Unknown StatusTreatmentPsychosis Nos/Other1
4CompletedTreatmentAcute Agitation1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentMajor Depressive Disorder Without Psychotic Features1
4CompletedTreatmentPosttraumatic Stress Disorders1
4CompletedTreatmentPsychotic Disorder NOS1
4CompletedTreatmentSchizophrenic Disorders1
4Unknown StatusTreatmentDisorders / Schizophrenia and Disorders With Psychotic Features1
Not AvailableEnrolling by InvitationNot AvailableBipolar Disorder (BD)1
Not AvailableRecruitingNot AvailableBipolar Disorder (BD)1
Not AvailableRecruitingNot AvailableSchizophrenic Disorders1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletSublingual10 mg/1
TabletSublingual10 mg
TabletSublingual2.5 mg/1
TabletSublingual5 mg
TabletSublingual5 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5763476Yes2000-12-092020-12-09Us
US7741358Yes2006-10-062026-10-06Us
US8022228Yes2006-10-062026-10-06Us

Properties

State
Solid
Experimental Properties
Not 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 RuleNoChemAxon
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)

Spectra

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzoxepines
Sub Class
Dibenzoxepines
Direct Parent
Dibenzoxepines
Alternative Parents
Diarylethers / Aralkylamines / Unsaturated fatty acids / Aryl chlorides / N-alkylpyrrolidines / Benzenoids / Dicarboxylic acids and derivatives / Trialkylamines / Oxacyclic compounds / Azacyclic compounds
show 6 more
Substituents
Dibenzoxepine / Diaryl ether / Aralkylamine / Aryl chloride / Aryl halide / Dicarboxylic acid or derivatives / Unsaturated fatty acid / N-alkylpyrrolidine / Benzenoid / Fatty acid
show 21 more
Molecular Framework
Not Available
External Descriptors
Not 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
Uniprot Name
D(2) dopamine receptor
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-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
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...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
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 subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
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...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
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-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
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 ...
Gene Name
HTR5A
Uniprot ID
P47898
Uniprot Name
5-hydroxytryptamine receptor 5A
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 ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
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 ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
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
Uniprot Name
Alpha-2C adrenergic receptor
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) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
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
Uniprot Name
D(1A) dopamine receptor
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
Uniprot Name
D(3) dopamine receptor
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 ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
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 catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
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 diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
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 e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
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 ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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...
Gene Name
UGT1A4
Uniprot ID
P22310
Uniprot Name
UDP-glucuronosyltransferase 1-4
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on March 19, 2008 10:17 / Updated on November 22, 2017 12:36