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Identification
NameAsenapine
Accession NumberDB06216
TypeSmall Molecule
GroupsApproved
DescriptionDeveloped by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Asenapine also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009.
Structure
Thumb
Synonyms
Saphris
External Identifiers
  • ORG-5222
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Saphristablet10 mg/1sublingualSTAT Rx USA LLC2009-08-14Not applicableUs
Saphristablet5 mg/1sublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs
Saphristablet2.5 mg/1sublingualForest Laboratories, Inc.2014-12-30Not applicableUs
Saphristablet5 mgsublingualMerck Canada Inc2011-12-19Not applicableCanada
Saphristablet10 mg/1sublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs
Saphristablet5 mg/1sublingualForest Laboratories, Inc.2013-09-30Not applicableUs
Saphristablet10 mgsublingualMerck Canada Inc2011-12-19Not applicableCanada
Saphristablet5 mg/1sublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs
Saphristablet10 mg/1sublingualForest Laboratories, Inc.2013-09-30Not applicableUs
Saphristablet10 mg/1sublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs
SycrestSublingual tablet10 mgSublingual useN.V. Organon2010-09-01Not applicableEu
SycrestSublingual tablet5 mgSublingual useN.V. Organon2010-09-01Not applicableEu
SycrestSublingual tablet5 mgSublingual useN.V. Organon2010-09-01Not applicableEu
SycrestSublingual tablet10 mgSublingual useN.V. Organon2010-09-01Not applicableEu
SycrestSublingual tablet5 mgSublingual useN.V. Organon2010-09-01Not applicableEu
SycrestSublingual tablet10 mgSublingual useN.V. Organon2010-09-01Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Sycrest Lundbeck
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Asenapine Maleate
Thumb
  • InChI Key: GMDCDXMAFMEDAG-CHHFXETESA-N
  • Monoisotopic Mass: 401.103000462
  • Average Mass: 401.84
DBSALT000010
Categories
UNIIJKZ19V908O
CAS number65576-45-6
WeightAverage: 401.84
Monoisotopic: 401.103000462
Chemical FormulaC21H20ClNO5
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxepines
Sub ClassDibenzoxepines
Direct ParentDibenzoxepines
Alternative Parents
Substituents
  • Dibenzoxepine
  • Diaryl ether
  • Aralkylamine
  • Chlorobenzene
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • N-alkylpyrrolidine
  • Unsaturated fatty acid
  • Dicarboxylic acid or derivatives
  • Aryl halide
  • Aryl chloride
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationUsed for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination.
PharmacodynamicsAsenapine is a serotonin, dopamine, noradrenaline, and histamine antagonist in which asenapine possess more potent activity with serotonin receptors than dopamine. Sedation in patients is associated with asenapine's antagonist activity at histamine receptors. Its lower incidence of extrapyramidal effects are associated with the upregulation of D1 receptors. This upregulation occurs due to asenapine's dose-dependent effects on glutamate transmission in the brain. It does not have any significant activity with muscarinic, cholinergic receptors therefore symptoms associated with anticholinergic drug activity like dry mouth or constipation are not expected to be observed. Asenapine has a higher affinity for all aforementioned receptors compared to first-generation and second-generation antipsychotics except for 5-HT1A and 5-HT1B receptors.
Mechanism of actionAsenapine is an atypical antipsychotic multireceptor neuroleptic drug which shows strong 5HT2A (serotonin) and D2 (dopamine) receptor antagonism, which has been shown to enhance dopamine (DA) and acetylcholine (Ach) efflux in rat brains. Asenapine may improve cognitive function and negative symptoms in patients with schizophrenia.
Related Articles
AbsorptionCmax, single 5 mg dose = 4 ng/mL (within 1 hour); Bioavailability, sublingual administration = 35%; Bioavailability, oral administration (swallowed) = <2%; Time to steady state, 5 mg = 3 days; Peak plasma concentration occurs within 0.5 to 1.5 hours. Doubling dose of asenapine results in 1.7-fold increase in maximum concentration and exposure. Drinking water within 2-5 minutes post administration of asenapine results in a decrease in exposure.
Volume of distribution

20-25 L/kg

Protein binding95% protein bound
Metabolism

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

Route of eliminationUrine (50%) and feces (50%)
Half life24 hours (range of 13.4 - 39.2 hours)
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9849
Blood Brain Barrier+0.8842
Caco-2 permeable+0.5605
P-glycoprotein substrateSubstrate0.7617
P-glycoprotein inhibitor INon-inhibitor0.9375
P-glycoprotein inhibitor IINon-inhibitor0.8901
Renal organic cation transporterNon-inhibitor0.7054
CYP450 2C9 substrateNon-substrate0.7964
CYP450 2D6 substrateNon-substrate0.7864
CYP450 3A4 substrateSubstrate0.5065
CYP450 1A2 substrateNon-inhibitor0.5212
CYP450 2C9 inhibitorNon-inhibitor0.7185
CYP450 2D6 inhibitorNon-inhibitor0.6781
CYP450 2C19 inhibitorNon-inhibitor0.5762
CYP450 3A4 inhibitorNon-inhibitor0.8625
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6005
Ames testNon AMES toxic0.5417
CarcinogenicityNon-carcinogens0.8694
BiodegradationNot ready biodegradable0.9894
Rat acute toxicity2.7083 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8125
hERG inhibition (predictor II)Non-inhibitor0.6697
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletsublingual10 mg/1
Tabletsublingual10 mg
Tabletsublingual2.5 mg/1
Tabletsublingual5 mg/1
Tabletsublingual5 mg
Sublingual tabletSublingual use10 mg
Sublingual tabletSublingual use5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5763476 Yes2000-12-092020-12-09Us
US7741358 Yes2006-10-062026-10-06Us
US8022228 Yes2006-10-062026-10-06Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP3.72ChemAxon
pKa (Strongest Basic)7.29ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity81.65 m3·mol-1ChemAxon
Polarizability30.9 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4145434
General References
  1. Huang M, Li Z, Dai J, Shahid M, Wong EH, Meltzer HY: Asenapine increases dopamine, norepinephrine, and acetylcholine efflux in the rat medial prefrontal cortex and hippocampus. Neuropsychopharmacology. 2008 Nov;33(12):2934-45. doi: 10.1038/npp.2008.20. Epub 2008 Apr 16. [PubMed:18418367 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
  3. Franberg O, Wiker C, Marcus MM, Konradsson A, Jardemark K, Schilstrom B, Shahid M, Wong EH, Svensson TH: Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. Epub 2007 Oct 17. [PubMed:17940749 ]
  4. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
External Links
ATC CodesN05AH05
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (448 KB)
MSDSDownload (91.9 KB)
Interactions
Drug Interactions
Drug
3,4-MethylenedioxyamphetamineAsenapine may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.
3,4-MethylenedioxymethamphetamineAsenapine may decrease the stimulatory activities of 3,4-Methylenedioxymethamphetamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Asenapine.
AbirateroneThe serum concentration of Asenapine can be increased when it is combined with Abiraterone.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Asenapine.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Asenapine.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Asenapine.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Asenapine.
adipiplonThe risk or severity of adverse effects can be increased when Asenapine is combined with adipiplon.
AgomelatineThe risk or severity of adverse effects can be increased when Asenapine is combined with Agomelatine.
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Asenapine.
AlfaxaloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Alfaxalone.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Asenapine.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Asenapine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Asenapine.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Asenapine.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Asenapine.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Asenapine.
AmantadineAmantadine may increase the QTc-prolonging activities of Asenapine.
AmiodaroneAmiodarone may increase the QTc-prolonging activities of Asenapine.
AmisulprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Asenapine.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Asenapine.
AmoxapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Asenapine is combined with Amperozide.
AmphetamineAsenapine may decrease the stimulatory activities of Amphetamine.
AnagrelideAnagrelide may increase the QTc-prolonging activities of Asenapine.
ApomorphineApomorphine may increase the QTc-prolonging activities of Asenapine.
AprepitantThe serum concentration of Asenapine can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Asenapine.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Asenapine.
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Asenapine.
ArtemetherAsenapine may increase the QTc-prolonging activities of Artemether.
ArticaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Articaine.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Asenapine.
AtazanavirThe metabolism of Asenapine can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Asenapine can be decreased when combined with Atomoxetine.
AzaperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Azaperone.
AzelastineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Asenapine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Asenapine.
BaclofenThe risk or severity of adverse effects can be increased when Asenapine is combined with Baclofen.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Asenapine.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Asenapine.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Asenapine.
BenzphetamineAsenapine may decrease the stimulatory activities of Benzphetamine.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Asenapine is combined with Benzyl alcohol.
BexaroteneThe serum concentration of Asenapine can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Asenapine can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Asenapine can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Asenapine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Asenapine.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Asenapine is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
BrimonidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Asenapine.
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Asenapine.
BrompheniramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Brompheniramine.
BrotizolamThe risk or severity of adverse effects can be increased when Asenapine is combined with Brotizolam.
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Asenapine.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Asenapine.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Asenapine.
BuserelinBuserelin may increase the QTc-prolonging activities of Asenapine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Asenapine.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Asenapine.
ButacaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Butacaine.
ButalbitalThe risk or severity of adverse effects can be increased when Asenapine is combined with Butalbital.
ButambenThe risk or severity of adverse effects can be increased when Asenapine is combined with Butamben.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Asenapine.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Asenapine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Asenapine.
CaffeineThe metabolism of Asenapine can be decreased when combined with Caffeine.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Asenapine.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Asenapine.
CarbinoxamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Carbinoxamine.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Asenapine.
CarisoprodolThe risk or severity of adverse effects can be increased when Asenapine is combined with Carisoprodol.
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Asenapine.
CefditorenThe serum concentration of Cefditoren can be decreased when it is combined with Asenapine.
CefpodoximeAsenapine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
CefuroximeAsenapine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
CeritinibCeritinib may increase the QTc-prolonging activities of Asenapine.
CetirizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cetirizine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Asenapine.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Asenapine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Asenapine.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Asenapine.
ChloroquineChloroquine may increase the QTc-prolonging activities of Asenapine.
ChlorphenamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Chlorphenamine.
ChlorphentermineAsenapine may decrease the stimulatory activities of Chlorphentermine.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Asenapine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Chlorpromazine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Asenapine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Asenapine.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Chlorzoxazone.
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Asenapine.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Asenapine.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Asenapine.
CisaprideCisapride may increase the QTc-prolonging activities of Asenapine.
CitalopramCitalopram may increase the QTc-prolonging activities of Asenapine.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Asenapine.
ClemastineThe metabolism of Asenapine can be decreased when combined with Clemastine.
ClemastineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Asenapine is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Asenapine is combined with Clobazam.
clomethiazoleThe risk or severity of adverse effects can be increased when Asenapine is combined with clomethiazole.
ClomipramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Asenapine.
ClotrimazoleThe metabolism of Asenapine can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Asenapine.
ClozapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Clozapine.
CobicistatThe metabolism of Asenapine can be decreased when combined with Cobicistat.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Asenapine.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Asenapine.
ConivaptanThe serum concentration of Asenapine can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Asenapine.
CyclizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Asenapine.
CyclosporineThe metabolism of Asenapine can be decreased when combined with Cyclosporine.
CyproheptadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Cyproheptadine.
Cyproterone acetateThe serum concentration of Asenapine can be decreased when it is combined with Cyproterone acetate.
CysteamineThe therapeutic efficacy of Cysteamine can be decreased when used in combination with Asenapine.
DabrafenibThe serum concentration of Dabrafenib can be decreased when it is combined with Asenapine.
DantroleneThe risk or severity of adverse effects can be increased when Asenapine is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Asenapine.
DapoxetineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dapoxetine.
DarunavirThe metabolism of Asenapine can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Asenapine can be increased when it is combined with Dasatinib.
DasatinibAsenapine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
DeferasiroxThe serum concentration of Asenapine can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Asenapine.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Asenapine.
DelavirdineThe metabolism of Asenapine can be decreased when combined with Delavirdine.
deramciclaneThe risk or severity of adverse effects can be increased when Asenapine is combined with deramciclane.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Asenapine.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Asenapine.
DesloratadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Desloratadine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Asenapine.
DetomidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Detomidine.
DexamethasoneThe serum concentration of Asenapine can be decreased when it is combined with Dexamethasone.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Dexbrompheniramine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Asenapine.
DexmethylphenidateAsenapine can cause an increase in the absorption of Dexmethylphenidate resulting in an increased serum concentration and potentially a worsening of adverse effects.
DextroamphetamineAsenapine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Asenapine.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Asenapine.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Asenapine.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Asenapine.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Asenapine.
DifenoxinThe risk or severity of adverse effects can be increased when Asenapine is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Asenapine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Asenapine.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Asenapine.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Asenapine.
DiltiazemThe metabolism of Asenapine can be decreased when combined with Diltiazem.
DimenhydrinateThe risk or severity of adverse effects can be increased when Asenapine is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Asenapine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Asenapine.
DisopyramideDisopyramide may increase the QTc-prolonging activities of Asenapine.
DofetilideDofetilide may increase the QTc-prolonging activities of Asenapine.
DolasetronDolasetron may increase the QTc-prolonging activities of Asenapine.
DomperidoneDomperidone may increase the QTc-prolonging activities of Asenapine.
DoramectinThe risk or severity of adverse effects can be increased when Asenapine is combined with Doramectin.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Asenapine.
DoxycyclineThe metabolism of Asenapine can be decreased when combined with Doxycycline.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
DoxylamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when Asenapine is combined with DPDPE.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
DronedaroneDronedarone may increase the QTc-prolonging activities of Asenapine.
DroperidolDroperidol may increase the QTc-prolonging activities of Asenapine.
DroperidolThe risk or severity of adverse effects can be increased when Asenapine is combined with Droperidol.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Asenapine.
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Asenapine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Asenapine.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Asenapine.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Asenapine.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Asenapine.
EfavirenzThe serum concentration of Asenapine can be decreased when it is combined with Efavirenz.
EfavirenzThe risk or severity of adverse effects can be increased when Asenapine is combined with Efavirenz.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Asenapine.
EliglustatAsenapine may increase the QTc-prolonging activities of Eliglustat.
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Asenapine.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Asenapine.
EntacaponeThe risk or severity of adverse effects can be increased when Asenapine is combined with Entacapone.
EnzalutamideThe serum concentration of Asenapine can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Asenapine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Asenapine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Asenapine.
EribulinEribulin may increase the QTc-prolonging activities of Asenapine.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Asenapine.
ErythromycinErythromycin may increase the QTc-prolonging activities of Asenapine.
EscitalopramEscitalopram may increase the QTc-prolonging activities of Asenapine.
Eslicarbazepine acetateThe serum concentration of Asenapine can be decreased when it is combined with Eslicarbazepine acetate.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Asenapine.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Asenapine.
EthanolAsenapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Asenapine.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Asenapine.
EthosuximideThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Asenapine is combined with Ethotoin.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Asenapine.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Asenapine.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Asenapine.
EtidocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Etidocaine.
EtifoxineThe risk or severity of adverse effects can be increased when Asenapine is combined with Etifoxine.
EtizolamThe risk or severity of adverse effects can be increased when Asenapine is combined with Etizolam.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Asenapine.
EtoperidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Asenapine.
EtravirineThe serum concentration of Asenapine can be decreased when it is combined with Etravirine.
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Asenapine.
EzogabineThe risk or severity of adverse effects can be increased when Asenapine is combined with Ezogabine.
FamotidineFamotidine may increase the QTc-prolonging activities of Asenapine.
FelbamateThe risk or severity of adverse effects can be increased when Asenapine is combined with Felbamate.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Asenapine.
FenfluramineThe risk or severity of adverse effects can be increased when Asenapine is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Asenapine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Asenapine.
FexofenadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Fexofenadine.
FingolimodFingolimod may increase the QTc-prolonging activities of Asenapine.
FlecainideFlecainide may increase the QTc-prolonging activities of Asenapine.
FlibanserinThe risk or severity of adverse effects can be increased when Asenapine is combined with Flibanserin.
FluconazoleThe metabolism of Asenapine can be decreased when combined with Fluconazole.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Asenapine.
FlunarizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Asenapine.
FluoxetineFluoxetine may increase the QTc-prolonging activities of Asenapine.
FlupentixolFlupentixol may increase the QTc-prolonging activities of Asenapine.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Asenapine.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Asenapine.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Asenapine.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Asenapine is combined with Fluticasone Propionate.
FluvoxamineThe serum concentration of Asenapine can be increased when it is combined with Fluvoxamine.
FluvoxamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Asenapine.
FosamprenavirThe serum concentration of Fosamprenavir can be decreased when it is combined with Asenapine.
FosamprenavirThe metabolism of Asenapine can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Asenapine can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Asenapine.
FosphenytoinThe risk or severity of adverse effects can be increased when Asenapine is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Asenapine is combined with Fospropofol.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Asenapine.
Fusidic AcidThe serum concentration of Asenapine can be increased when it is combined with Fusidic Acid.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Asenapine.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Asenapine is combined with gabapentin enacarbil.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Asenapine.
GalantamineGalantamine may increase the QTc-prolonging activities of Asenapine.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Asenapine.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Asenapine.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Asenapine.
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Asenapine.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Asenapine.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Asenapine.
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Asenapine.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Asenapine.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Asenapine.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Asenapine.
GoserelinGoserelin may increase the QTc-prolonging activities of Asenapine.
GranisetronGranisetron may increase the QTc-prolonging activities of Asenapine.
GuanfacineThe risk or severity of adverse effects can be increased when Asenapine is combined with Guanfacine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Asenapine.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Asenapine.
HaloperidolThe risk or severity of adverse effects can be increased when Asenapine is combined with Haloperidol.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Asenapine.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Asenapine.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Asenapine.
HistrelinHistrelin may increase the QTc-prolonging activities of Asenapine.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Asenapine.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Asenapine.
Hydroxyamphetamine hydrobromideAsenapine may decrease the stimulatory activities of Hydroxyamphetamine hydrobromide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
HydroxyzineThe risk or severity of adverse effects can be increased when Asenapine is combined with Hydroxyzine.
IbandronateIbandronate may increase the QTc-prolonging activities of Asenapine.
IbutilideIbutilide may increase the QTc-prolonging activities of Asenapine.
IdelalisibThe serum concentration of Asenapine can be increased when it is combined with Idelalisib.
IloperidoneIloperidone may increase the QTc-prolonging activities of Asenapine.
ImatinibThe metabolism of Asenapine can be decreased when combined with Imatinib.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Asenapine.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Asenapine.
IndalpineThe risk or severity of adverse effects can be increased when Asenapine is combined with Indalpine.
IndapamideIndapamide may increase the QTc-prolonging activities of Asenapine.
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Asenapine.
IndinavirThe metabolism of Asenapine can be decreased when combined with Indinavir.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Asenapine.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Asenapine.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Asenapine.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Asenapine.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Asenapine.
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Asenapine.
IsavuconazoniumThe metabolism of Asenapine can be decreased when combined with Isavuconazonium.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Asenapine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Asenapine.
IsradipineThe metabolism of Asenapine can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Asenapine.
ItraconazoleThe metabolism of Asenapine can be decreased when combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Asenapine.
IvacaftorThe serum concentration of Asenapine can be increased when it is combined with Ivacaftor.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Asenapine.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Asenapine.
KetobemidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Ketobemidone.
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Asenapine.
KetoconazoleThe metabolism of Asenapine can be decreased when combined with Ketoconazole.
LamotrigineThe risk or severity of adverse effects can be increased when Asenapine is combined with Lamotrigine.
LapatinibLapatinib may increase the QTc-prolonging activities of Asenapine.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Asenapine.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Asenapine.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Asenapine.
LevetiracetamThe risk or severity of adverse effects can be increased when Asenapine is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Asenapine.
LevocabastineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Asenapine is combined with Levodopa.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Asenapine.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Asenapine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Asenapine is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Asenapine.
LidocaineThe metabolism of Asenapine can be decreased when combined with Lidocaine.
LidocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Lidocaine.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Asenapine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Asenapine.
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Asenapine.
LisdexamfetamineAsenapine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Asenapine.
LithiumThe risk or severity of adverse effects can be increased when Asenapine is combined with Lithium.
LofentanilThe risk or severity of adverse effects can be increased when Asenapine is combined with Lofentanil.
LopinavirLopinavir may increase the QTc-prolonging activities of Asenapine.
LoratadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Asenapine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Asenapine.
LovastatinThe metabolism of Asenapine can be decreased when combined with Lovastatin.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Asenapine.
Lu AA21004The risk or severity of adverse effects can be increased when Asenapine is combined with Lu AA21004.
LuliconazoleThe serum concentration of Asenapine can be increased when it is combined with Luliconazole.
LumefantrineAsenapine may increase the QTc-prolonging activities of Lumefantrine.
LurasidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Asenapine is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Asenapine.
MeclizineThe risk or severity of adverse effects can be increased when Asenapine is combined with Meclizine.
MedetomidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Medetomidine.
MefloquineMefloquine may increase the QTc-prolonging activities of Asenapine.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Asenapine.
MelperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Melperone.
MephentermineAsenapine may decrease the stimulatory activities of Mephentermine.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Asenapine.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Asenapine.
MequitazineAsenapine may increase the arrhythmogenic activities of Mequitazine.
MesalazineThe therapeutic efficacy of Mesalazine can be decreased when used in combination with Asenapine.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Asenapine.
MetaxaloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Metaxalone.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Asenapine.
MethadoneMethadone may increase the QTc-prolonging activities of Asenapine.
MethadoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Methadone.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Asenapine.
MethamphetamineAsenapine may decrease the stimulatory activities of Methamphetamine.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Asenapine.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Asenapine.
MethocarbamolThe risk or severity of adverse effects can be increased when Asenapine is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Asenapine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Asenapine.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Asenapine.
MethsuximideThe risk or severity of adverse effects can be increased when Asenapine is combined with Methsuximide.
MethylphenidateThe risk or severity of adverse effects can be increased when Asenapine is combined with Methylphenidate.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Asenapine.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Asenapine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Asenapine.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Asenapine.
MetyrosineAsenapine may increase the sedative activities of Metyrosine.
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Asenapine.
MexiletineThe metabolism of Asenapine can be decreased when combined with Mexiletine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Asenapine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Asenapine.
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Asenapine.
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Asenapine.
MilnacipranThe risk or severity of adverse effects can be increased when Asenapine is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
MirabegronMirabegron may increase the QTc-prolonging activities of Asenapine.
MirtazapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Asenapine.
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Asenapine.
MitotaneThe serum concentration of Asenapine can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Asenapine.
ModafinilThe serum concentration of Asenapine can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Asenapine.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Asenapine.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Asenapine.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Asenapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
NabiloneThe risk or severity of adverse effects can be increased when Asenapine is combined with Nabilone.
NafcillinThe serum concentration of Asenapine can be decreased when it is combined with Nafcillin.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Asenapine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Asenapine.
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Asenapine.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Asenapine.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Asenapine.
NelfinavirThe metabolism of Asenapine can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Asenapine can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Asenapine can be decreased when combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Asenapine.
NilotinibNilotinib may increase the QTc-prolonging activities of Asenapine.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Asenapine.
Nitrous oxideThe risk or severity of adverse effects can be increased when Asenapine is combined with Nitrous oxide.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Asenapine.
NormethadoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Normethadone.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Asenapine.
OctreotideOctreotide may increase the QTc-prolonging activities of Asenapine.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Asenapine.
OlanzapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Olanzapine.
OlaparibThe metabolism of Asenapine can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Asenapine.
OlopatadineThe risk or severity of adverse effects can be increased when Asenapine is combined with Olopatadine.
OndansetronOndansetron may increase the QTc-prolonging activities of Asenapine.
OndansetronThe risk or severity of adverse effects can be increased when Asenapine is combined with Ondansetron.
OpiumThe risk or severity of adverse effects can be increased when Asenapine is combined with Opium.
OrphenadrineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Asenapine.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Asenapine.
OsimertinibThe serum concentration of Asenapine can be increased when it is combined with Osimertinib.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Asenapine.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Asenapine.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Asenapine.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Asenapine.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Asenapine.
OxytocinOxytocin may increase the QTc-prolonging activities of Asenapine.
PalbociclibThe serum concentration of Asenapine can be increased when it is combined with Palbociclib.
PaliperidonePaliperidone may increase the QTc-prolonging activities of Asenapine.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Asenapine.
ParaldehydeAsenapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with Asenapine.
ParoxetineThe risk or severity of adverse effects can be increased when Asenapine is combined with Paroxetine.
PasireotidePasireotide may increase the QTc-prolonging activities of Asenapine.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Asenapine.
PazopanibPazopanib may increase the QTc-prolonging activities of Asenapine.
Peginterferon alfa-2bThe serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.
PentamidinePentamidine may increase the QTc-prolonging activities of Asenapine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Asenapine.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Asenapine.
PerampanelThe risk or severity of adverse effects can be increased when Asenapine is combined with Perampanel.
PerflutrenPerflutren may increase the QTc-prolonging activities of Asenapine.
PerospironeThe risk or severity of adverse effects can be increased when Asenapine is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Asenapine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Asenapine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Asenapine.
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Asenapine.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Asenapine.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenoxyethanol.
PhentermineAsenapine may decrease the stimulatory activities of Phentermine.
PhenytoinThe risk or severity of adverse effects can be increased when Asenapine is combined with Phenytoin.
PimozidePimozide may increase the QTc-prolonging activities of Asenapine.
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Asenapine.
PipamperoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Pipamperone.
PipotiazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Asenapine is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Asenapine is combined with Pomalidomide.
PosaconazoleThe serum concentration of Posaconazole can be decreased when it is combined with Asenapine.
PosaconazoleThe metabolism of Asenapine can be decreased when combined with Posaconazole.
PramipexoleAsenapine may increase the sedative activities of Pramipexole.
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Asenapine.
PramocaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Pramocaine.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Asenapine.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Asenapine.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Asenapine.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Asenapine.
PrimidoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Primidone.
ProcainamideProcainamide may increase the QTc-prolonging activities of Asenapine.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Asenapine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Asenapine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Asenapine.
PromazinePromazine may increase the QTc-prolonging activities of Asenapine.
PromazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Promazine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Asenapine.
PropafenonePropafenone may increase the QTc-prolonging activities of Asenapine.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Asenapine.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Asenapine.
PropoxycaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Propoxycaine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Asenapine.
PSD502The risk or severity of adverse effects can be increased when Asenapine is combined with PSD502.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Asenapine.
QuetiapineQuetiapine may increase the QTc-prolonging activities of Asenapine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Asenapine.
QuinidineQuinidine may increase the QTc-prolonging activities of Asenapine.
QuinineQuinine may increase the QTc-prolonging activities of Asenapine.
RamelteonThe risk or severity of adverse effects can be increased when Asenapine is combined with Ramelteon.
RanolazineThe metabolism of Asenapine can be decreased when combined with Ranolazine.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Asenapine.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Asenapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Asenapine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Asenapine.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Asenapine.
RifabutinThe metabolism of Asenapine can be increased when combined with Rifabutin.
RifampicinThe metabolism of Asenapine can be increased when combined with Rifampicin.
RifapentineThe metabolism of Asenapine can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Asenapine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Asenapine.
RisedronateThe serum concentration of Risedronate can be increased when it is combined with Asenapine.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Asenapine.
RitonavirThe metabolism of Asenapine can be decreased when combined with Ritonavir.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Asenapine.
RomifidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Romifidine.
RopiniroleAsenapine may increase the sedative activities of Ropinirole.
RopiniroleThe metabolism of Asenapine can be decreased when combined with Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Asenapine.
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Asenapine.
RotigotineAsenapine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Asenapine.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Asenapine.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Asenapine.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Asenapine.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Asenapine.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Asenapine.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Asenapine.
ScopolamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Scopolamine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Asenapine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Asenapine.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Asenapine.
SertralineThe risk or severity of adverse effects can be increased when Asenapine is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Asenapine.
SildenafilThe metabolism of Asenapine can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Asenapine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Asenapine can be increased when it is combined with Simeprevir.
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Asenapine.
Sodium oxybateThe risk or severity of adverse effects can be increased when Asenapine is combined with Sodium oxybate.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Asenapine.
SorafenibSorafenib may increase the QTc-prolonging activities of Asenapine.
SotalolSotalol may increase the QTc-prolonging activities of Asenapine.
St. John's WortThe serum concentration of Asenapine can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe risk or severity of adverse effects can be increased when Asenapine is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Asenapine.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Asenapine.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Asenapine.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Asenapine.
SulpirideThe risk or severity of adverse effects can be increased when Asenapine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Asenapine.
SunitinibSunitinib may increase the QTc-prolonging activities of Asenapine.
SuvorexantThe risk or severity of adverse effects can be increased when Asenapine is combined with Suvorexant.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Asenapine.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Asenapine.
TasimelteonThe risk or severity of adverse effects can be increased when Asenapine is combined with Tasimelteon.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Asenapine.
TelaprevirThe metabolism of Asenapine can be decreased when combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Asenapine.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Asenapine.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Asenapine.
TenofovirThe metabolism of Asenapine can be decreased when combined with Tenofovir.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Asenapine.
TeriflunomideThe serum concentration of Asenapine can be decreased when it is combined with Teriflunomide.
TetrabenazineTetrabenazine may increase the QTc-prolonging activities of Asenapine.
TetracaineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tetracaine.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Asenapine.
ThalidomideAsenapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Asenapine.
TheophyllineThe metabolism of Asenapine can be decreased when combined with Theophylline.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Asenapine.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Asenapine.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Asenapine.
ThioridazineThioridazine may increase the QTc-prolonging activities of Asenapine.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Asenapine.
TiagabineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tiagabine.
TiclopidineThe metabolism of Asenapine can be decreased when combined with Ticlopidine.
TiletamineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tiletamine.
TizanidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tizanidine.
TocilizumabThe serum concentration of Asenapine can be decreased when it is combined with Tocilizumab.
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Asenapine.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Asenapine.
TolcaponeThe risk or severity of adverse effects can be increased when Asenapine is combined with Tolcapone.
TolterodineTolterodine may increase the QTc-prolonging activities of Asenapine.
TopiramateThe risk or severity of adverse effects can be increased when Asenapine is combined with Topiramate.
ToremifeneToremifene may increase the QTc-prolonging activities of Asenapine.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Asenapine.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Asenapine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Asenapine.
TrazodoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Trazodone.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Asenapine.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Asenapine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Asenapine.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Asenapine.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Asenapine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Asenapine.
TriprolidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Triprolidine.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Asenapine.
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Asenapine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Asenapine.
VandetanibVandetanib may increase the QTc-prolonging activities of Asenapine.
VardenafilVardenafil may increase the QTc-prolonging activities of Asenapine.
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Asenapine.
VemurafenibAsenapine may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Asenapine.
VerapamilThe metabolism of Asenapine can be decreased when combined with Verapamil.
VigabatrinThe risk or severity of adverse effects can be increased when Asenapine is combined with Vigabatrin.
VilanterolVilanterol may increase the QTc-prolonging activities of Asenapine.
VilazodoneThe risk or severity of adverse effects can be increased when Asenapine is combined with Vilazodone.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Asenapine.
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Asenapine.
VoriconazoleThe metabolism of Asenapine can be decreased when combined with Voriconazole.
VorinostatVorinostat may increase the QTc-prolonging activities of Asenapine.
VortioxetineThe risk or severity of adverse effects can be increased when Asenapine is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Asenapine is combined with Xylazine.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Asenapine.
ZiconotideThe risk or severity of adverse effects can be increased when Asenapine is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Asenapine is combined with Zimelidine.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Asenapine.
ZolazepamThe risk or severity of adverse effects can be increased when Asenapine is combined with Zolazepam.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Asenapine.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Asenapine.
ZonisamideThe risk or severity of adverse effects can be increased when Asenapine is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Asenapine.
ZotepineThe risk or severity of adverse effects can be increased when Asenapine is combined with Zotepine.
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Asenapine.
Food Interactions
  • Avoid water and food for at least 10 minutes post administration of asenapine

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Sep;666(1-3):43-52. doi: 10.1016/j.ejphar.2011.05.050. Epub 2011 Jun 1. [PubMed:21658377 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
Molecular Weight:
54297.41 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins.
Gene Name:
HTR5A
Uniprot ID:
P47898
Molecular Weight:
40254.69 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Sep;666(1-3):43-52. doi: 10.1016/j.ejphar.2011.05.050. Epub 2011 Jun 1. [PubMed:21658377 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) si...
Gene Name:
HRH2
Uniprot ID:
P25021
Molecular Weight:
40097.65 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. [PubMed:18308814 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. doi: 10.2147/NDT.S16077. Epub 2011 May 26. [PubMed:21655346 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity).
Gene Name:
UGT1A4
Uniprot ID:
P22310
Molecular Weight:
60024.535 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. [PubMed:23356509 ]
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Drug created on March 19, 2008 10:17 / Updated on September 24, 2016 03:31