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Identification
NameTapentadol
Accession NumberDB06204
TypeSmall Molecule
GroupsApproved
DescriptionOpioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008.
Structure
Thumb
Synonyms
BN-200
CG-5503
Nucynta
Tapentadol
External Identifiers
  • R331333
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NucyntaTablet, film coated100 mg/1OralStat Rx USA2009-06-01Not applicableUs
NucyntaTablet, film coated100 mg/1OralJanssen Pharmaceuticals, Inc.2009-06-01Not applicableUs
NucyntaTablet50 mg/1OralLake Erie Medical DBA Quality Care Products LLC2010-09-29Not applicableUs
NucyntaTablet, film coated100 mg/1OralPhysicians Total Care, Inc.2010-03-19Not applicableUs
NucyntaSolution20 mg/mLOralJanssen Pharmaceuticals, Inc.2012-10-15Not applicableUs
NucyntaTablet, film coated50 mg/1OralStat Rx USA2009-06-01Not applicableUs
NucyntaTablet, film coated100 mg/1OralLake Erie Medical DBA Quality Care Products LLC2009-06-01Not applicableUs
NucyntaTablet, film coated50 mg/1Oralbryant ranch prepack2009-06-01Not applicableUs
NucyntaTablet, film coated75 mg/1OralLake Erie Medical DBA Quality Care Products LLC2011-07-13Not applicableUs
NucyntaTablet, film coated50 mg/1OralJanssen Pharmaceuticals, Inc.2009-06-01Not applicableUs
NucyntaTablet, film coated75 mg/1OralSTAT Rx USA LLC2009-06-01Not applicableUs
NucyntaTablet, film coated50 mg/1OralPhysicians Total Care, Inc.2010-03-19Not applicableUs
NucyntaTablet, film coated100 mg/1Oralbryant ranch prepack2009-06-01Not applicableUs
NucyntaTablet, film coated75 mg/1OralJanssen Pharmaceuticals, Inc.2009-06-01Not applicableUs
NucyntaTablet, film coated50 mg/1OralRebel Distributors Corp2009-06-01Not applicableUs
NucyntaTablet, film coated75 mg/1OralPhysicians Total Care, Inc.2010-03-19Not applicableUs
Nucynta CRTablet, extended release50 mgOralJanssen Inc2011-02-172014-08-19Canada
Nucynta CRTablet, extended release250 mgOralJanssen Inc2011-02-172015-03-25Canada
Nucynta CRTablet, extended release100 mgOralJanssen Inc2011-02-172014-08-19Canada
Nucynta CRTablet, extended release150 mgOralJanssen Inc2011-02-172014-09-30Canada
Nucynta CRTablet, extended release200 mgOralJanssen Inc2011-02-172014-12-04Canada
Nucynta ERTablet, film coated, extended release50 mg/1OralLake Erie Medical DBA Quality Care Products LLC2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release200 mg/1OralJanssen Pharmaceuticals, Inc.2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release250 mg/1OralJanssen Pharmaceuticals, Inc.2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release50 mg/1OralJanssen Pharmaceuticals, Inc.2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release100 mg/1OralJanssen Pharmaceuticals, Inc.2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release100 mg/1OralLake Erie Medical DBA Quality Care Products LLC2011-08-25Not applicableUs
Nucynta ERTablet, film coated, extended release150 mg/1OralJanssen Pharmaceuticals, Inc.2011-08-25Not applicableUs
Nucynta Extended-releaseTablet, extended release100 mgOralJanssen Inc2014-04-16Not applicableCanada
Nucynta Extended-releaseTablet, extended release150 mgOralJanssen Inc2014-04-16Not applicableCanada
Nucynta Extended-releaseTablet, extended release200 mgOralJanssen Inc2014-04-16Not applicableCanada
Nucynta Extended-releaseTablet, extended release50 mgOralJanssen Inc2014-04-16Not applicableCanada
Nucynta Extended-releaseTablet, extended release250 mgOralJanssen Inc2014-04-16Not applicableCanada
Nucynta IrTablet, multilayer, extended release50 mgOralJanssen Inc2012-03-20Not applicableCanada
Nucynta IrTablet, multilayer, extended release75 mgOralJanssen Inc2012-03-20Not applicableCanada
Nucynta IrTablet, multilayer, extended release100 mgOralJanssen Inc2012-03-20Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PalexiaGrünenthal Ltd
TAPAL MSN Labs
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tapentadol Hydrochloride
Thumb
  • InChI Key: ZELFLGGRLLOERW-YECZQDJWSA-N
  • Monoisotopic Mass: 257.154642102
  • Average Mass: 257.799
DBSALT000169
Categories
UNIIH8A007M585
CAS number175591-23-8
WeightAverage: 221.3385
Monoisotopic: 221.177964363
Chemical FormulaC14H23NO
InChI KeyKWTWDQCKEHXFFR-SMDDNHRTSA-N
InChI
InChI=1S/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1
IUPAC Name
3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
SMILES
CC[[email protected]]([C@@H](C)CN(C)C)C1=CC(O)=CC=C1
Pharmacology
IndicationThe immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy.
Structured Indications
PharmacodynamicsTapentadol is a centrally-acting synthetic analgesic. It is 18 times less potent than morphine in terms of binding to human mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake. Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval.
Mechanism of actionTapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.
TargetKindPharmacological actionActionsOrganismUniProt ID
Mu-type opioid receptorProteinyes
agonist
HumanP35372 details
Sodium-dependent noradrenaline transporterProteinyes
inhibitor
HumanP23975 details
Kappa-type opioid receptorProteinunknownNot AvailableHumanP41145 details
Delta-type opioid receptorProteinunknownNot AvailableHumanP41143 details
5-hydroxytryptamine receptor 3AProteinunknownNot AvailableHumanP46098 details
Sodium-dependent serotonin transporterProteinunknown
inhibitor
HumanP31645 details
Related Articles
AbsorptionBioavailability, immediate release (IR), 86 mg: 32%; Bioavailability, extended release (ER), 86 mg: 32%; Cmax, IR: 64.2 ng/mL; Cmax, ER: 22.5 ng/mL; T max, IR: 1.5 hours; T max, ER: 5.0 hours; Tapentadol accumulates following multiple repeat doses.
Volume of distribution

Following IV administration, volume of distribution is 540 ± 98 L.

Protein binding~20%
Metabolism

97% of the dose is metabolized mostly via conjugation with glucuronic acid to produce glucuronides. Tapentadol is also metabolized into N-desmethyl tapentadol (13%) by CYP2C9 and CYP 2C19. CYP2D6 is involved in the formation of the metabolite, hydroxy tapentadol (2%). All metabolites are inactive.

SubstrateEnzymesProduct
Tapentadol
Not Available
N-desmethyl tapentadolDetails
Route of eliminationTapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.
Half lifeElimination half-life, IV: 4 hours.
Clearance

Total clearance = 1530 ± 177 ml/min.

ToxicityOral, rabbit: LD50 = 3200 mg/kg; Oral, mouse: LD50 = 300 mg/kg; Oral, rat: LD50: 980 mg/kg; The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneTapentadol may increase the central nervous system depressant (CNS depressant) activities of 1,1,1,2 Tetrafluoroethane.Investigational
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Tapentadol.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may increase the analgesic activities of Tapentadol.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may increase the analgesic activities of Tapentadol.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Tapentadol.Experimental, Illicit
7-NitroindazoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of 7-Nitroindazole.Experimental
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe risk or severity of adverse effects can be increased when Tapentadol is combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.Experimental
AbirateroneThe serum concentration of Tapentadol can be increased when it is combined with Abiraterone.Approved
AcepromazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Acepromazine.Approved, Vet Approved
AceprometazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Aceprometazine.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Acetazolamide.Approved, Vet Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Acetophenazine.Approved
AclidiniumThe risk or severity of adverse effects can be increased when Aclidinium is combined with Tapentadol.Approved
adipiplonTapentadol may increase the central nervous system depressant (CNS depressant) activities of adipiplon.Investigational
AgomelatineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Agomelatine.Approved, Investigational
AlfaxaloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Alfaxalone.Vet Approved
AlfentanilTapentadol may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.Approved, Illicit
AlimemazineAlimemazine may increase the hypotensive activities of Tapentadol.Approved, Vet Approved
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Tapentadol.Approved, Investigational
AlphacetylmethadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Alphacetylmethadol.Experimental, Illicit
AlprazolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Alprazolam.Approved, Illicit, Investigational
AlvimopanThe risk or severity of adverse effects can be increased when Tapentadol is combined with Alvimopan.Approved
AmilorideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Amiloride.Approved
AmiodaroneThe metabolism of Tapentadol can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amisulpride.Approved, Investigational
AmitriptylineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amitriptyline.Approved
Ammonium chlorideAmmonium chloride may increase the excretion rate of Tapentadol which could result in a lower serum level and potentially a reduction in efficacy.Approved, Vet Approved
AmobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.Approved, Illicit
AmoxapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amoxapine.Approved
AmperozideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amperozide.Experimental
AmphetamineAmphetamine may increase the analgesic activities of Tapentadol.Approved, Illicit
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Tapentadol.Approved
AprepitantThe metabolism of Tapentadol can be increased when combined with Aprepitant.Approved, Investigational
AripiprazoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of Aripiprazole.Approved, Investigational
ArmodafinilThe metabolism of Tapentadol can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Tapentadol can be decreased when combined with Artemether.Approved
ArticaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Articaine.Approved
AsenapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.Approved
AtomoxetineThe metabolism of Tapentadol can be decreased when combined with Atomoxetine.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Tapentadol.Approved
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Tapentadol.Approved, Vet Approved
AzaperoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Azaperone.Vet Approved
AzelastineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzosemideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Azosemide.Investigational
BaclofenTapentadol may increase the central nervous system depressant (CNS depressant) activities of Baclofen.Approved
BarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Barbital.Illicit
BenactyzineThe risk or severity of adverse effects can be increased when Benactyzine is combined with Tapentadol.Withdrawn
BendroflumethiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Bendroflumethiazide.Approved
BenmoxinThe risk or severity of adverse effects can be increased when Tapentadol is combined with Benmoxin.Withdrawn
BenperidolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Benperidol.Investigational
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Tapentadol.Approved
BenzocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Benzocaine.Approved
BenzphetamineBenzphetamine may increase the analgesic activities of Tapentadol.Approved, Illicit
Benzyl alcoholTapentadol may increase the central nervous system depressant (CNS depressant) activities of Benzyl alcohol.Approved
BetaxololThe metabolism of Tapentadol can be decreased when combined with Betaxolol.Approved
BifeprunoxThe risk or severity of adverse effects can be increased when Tapentadol is combined with Bifeprunox.Investigational
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Tapentadol.Approved
BL-1020BL-1020 may increase the hypotensive activities of Tapentadol.Investigational
BortezomibThe metabolism of Tapentadol can be decreased when combined with Bortezomib.Approved, Investigational
BrexpiprazoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of Brexpiprazole.Approved
BrimonidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Brimonidine.Approved
BromazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Bromazepam.Approved, Illicit
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Tapentadol.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Bromperidol.Investigational
BrompheniramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Brompheniramine.Approved
BrotizolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Brotizolam.Approved, Withdrawn
BumetanideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Bumetanide.Approved
BupivacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Bupivacaine.Approved, Investigational
BuprenorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Tapentadol can be decreased when combined with Bupropion.Approved
BuspironeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Buspirone.Approved, Investigational
ButabarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.Approved, Illicit
ButacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butacaine.Vet Approved
ButalbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butalbital.Approved, Illicit
ButambenTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butamben.Approved
ButethalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butethal.Approved, Illicit
ButorphanolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.Approved, Illicit, Vet Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tapentadol.Approved
Canrenoic acidThe risk or severity of adverse effects can be increased when Tapentadol is combined with Canrenoic acid.Approved, Withdrawn
CanrenoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Canrenone.Investigational
CapecitabineThe metabolism of Tapentadol can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Carbamazepine.Approved, Investigational
CarbinoxamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Carbinoxamine.Approved
CarfentanilTapentadol may increase the central nervous system depressant (CNS depressant) activities of Carfentanil.Illicit, Vet Approved
CariprazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Cariprazine.Approved
CarisoprodolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Carisoprodol.Approved
CaroxazoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Caroxazone.Withdrawn
CelecoxibThe metabolism of Tapentadol can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Tapentadol can be increased when it is combined with Ceritinib.Approved
CetirizineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cetirizine.Approved
Chloral hydrateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chloral hydrate.Approved, Illicit, Vet Approved
ChloramphenicolThe metabolism of Tapentadol can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlordiazepoxide.Approved, Illicit
ChlormezanoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlormezanone.Approved, Withdrawn
ChloroprocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chloroprocaine.Approved
ChloroquineThe metabolism of Tapentadol can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorothiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Chlorothiazide.Approved, Vet Approved
ChlorphenamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlorphenamine.Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Tapentadol.Withdrawn
ChlorphentermineChlorphentermine may increase the analgesic activities of Tapentadol.Illicit, Withdrawn
ChlorpromazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlorpromazine.Approved, Vet Approved
ChlorprothixeneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlorprothixene.Approved, Withdrawn
ChlorthalidoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Chlorthalidone.Approved
ChlorzoxazoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.Approved
CholecalciferolThe metabolism of Tapentadol can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CicletanineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Cicletanine.Investigational
CimetidineThe metabolism of Tapentadol can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Tapentadol can be decreased when combined with Cinacalcet.Approved
CinchocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cinchocaine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Tapentadol.Approved
ClemastineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clemastine.Approved
ClidiniumTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clidinium.Approved
ClobazamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clobazam.Approved, Illicit
clomethiazoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of clomethiazole.Investigational
ClomipramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clomipramine.Approved, Vet Approved
ClonazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clonazepam.Approved, Illicit
ClonidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clonidine.Approved
ClorazepateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.Approved, Illicit
ClotrimazoleThe metabolism of Tapentadol can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clozapine.Approved
CobicistatThe serum concentration of Tapentadol can be increased when it is combined with Cobicistat.Approved
CocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cocaine.Approved, Illicit
CodeineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Codeine.Approved, Illicit
ConivaptanThe risk or severity of adverse effects can be increased when Tapentadol is combined with Conivaptan.Approved, Investigational
CyamemazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Cyamemazine.Approved
CyclizineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyclizine.Approved
CyclobenzaprineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyclobenzaprine.Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Tapentadol.Approved
CyclosporineThe metabolism of Tapentadol can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Cyclothiazide.Approved
CyproheptadineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Cyproheptadine.Approved
DabrafenibThe serum concentration of Tapentadol can be decreased when it is combined with Dabrafenib.Approved
DantroleneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dantrolene.Approved
DapiprazoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Tapentadol.Investigational
DarifenacinThe metabolism of Tapentadol can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Tapentadol can be increased when it is combined with Darunavir.Approved
DelavirdineThe metabolism of Tapentadol can be decreased when combined with Delavirdine.Approved
deramciclaneTapentadol may increase the central nervous system depressant (CNS depressant) activities of deramciclane.Investigational
DesfluraneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Desflurane.Approved
DesipramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Desipramine.Approved
DesloratadineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.Approved, Investigational
DesmopressinThe risk or severity of adverse effects can be increased when Tapentadol is combined with Desmopressin.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Desvenlafaxine.Approved
DetomidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Detomidine.Vet Approved
DexbrompheniramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dexbrompheniramine.Approved
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Tapentadol.Withdrawn
DexmedetomidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dexmedetomidine.Approved, Vet Approved
DextroamphetamineDextroamphetamine may increase the analgesic activities of Tapentadol.Approved, Illicit
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Tapentadol.Approved
DextromoramideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dezocine.Approved
DiazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Illicit, Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Tapentadol.Approved
DiethylpropionDiethylpropion may increase the analgesic activities of Tapentadol.Approved, Illicit
DifenoxinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Difenoxin.Approved, Illicit
DihydrocodeineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dihydrocodeine.Approved, Illicit
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Tapentadol.Approved
DihydroetorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dihydromorphine.Experimental, Illicit
DimenhydrinateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.Approved
DiphenhydramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Diphenhydramine.Approved
DiphenoxylateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Diphenoxylate.Approved, Illicit
DolasetronDolasetron may decrease the analgesic activities of Tapentadol.Approved
DoramectinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Doramectin.Vet Approved
DoxepinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Doxepin.Approved
DoxylamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Doxylamine.Approved, Vet Approved
DPDPETapentadol may increase the central nervous system depressant (CNS depressant) activities of DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved, Illicit
DronedaroneThe metabolism of Tapentadol can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved, Vet Approved
DrospirenoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Drospirenone.Approved
DrotebanolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Tapentadol.Approved
DyclonineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Dyclonine.Approved
EcgonineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERTapentadol may increase the central nervous system depressant (CNS depressant) activities of ECGONINE METHYL ESTER.Experimental
EcopipamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ecopipam.Investigational
EfavirenzTapentadol may increase the central nervous system depressant (CNS depressant) activities of Efavirenz.Approved, Investigational
EfonidipineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Efonidipine.Approved
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Tapentadol.Approved, Investigational
EliglustatThe metabolism of Tapentadol can be decreased when combined with Eliglustat.Approved
EluxadolineTapentadol may increase the constipating activities of Eluxadoline.Approved
EnfluraneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Enflurane.Approved, Vet Approved
EntacaponeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Entacapone.Approved, Investigational
EplerenoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Eplerenone.Approved
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Tapentadol.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Tapentadol.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Tapentadol.Approved
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Tapentadol.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Tapentadol can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Tapentadol can be decreased when combined with Esomeprazole.Approved, Investigational
EstazolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Illicit
EszopicloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Eszopiclone.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Tapentadol is combined with Etacrynic acid.Approved
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved
EthchlorvynolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethchlorvynol.Approved, Illicit, Withdrawn
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Tapentadol.Approved
EthosuximideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethosuximide.Approved
EthotoinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethotoin.Approved
EthoxzolamideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Ethoxzolamide.Withdrawn
Ethyl carbamateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethyl carbamate.Withdrawn
Ethyl loflazepateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethyl loflazepate.Approved, Illicit
EthylmorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ethylmorphine.Approved, Illicit
EtidocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Etidocaine.Approved
EtifoxineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Etifoxine.Withdrawn
EtizolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Etizolam.Approved
EtomidateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Etomidate.Approved
EtoperidoneTapentadol may increase the serotonergic activities of Etoperidone.Approved
EtorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Etorphine.Illicit, Vet Approved
EtravirineThe metabolism of Tapentadol can be decreased when combined with Etravirine.Approved
EzogabineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ezogabine.Approved
FelbamateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Felbamate.Approved
FencamfamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fencamfamine.Approved, Illicit, Withdrawn
FentanylTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Tapentadol.Approved
FexofenadineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fexofenadine.Approved
FlibanserinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flibanserin.Approved
FloxuridineThe metabolism of Tapentadol can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Tapentadol can be decreased when combined with Fluconazole.Approved
FludiazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.Approved, Illicit
FlunarizineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.Approved
FlunitrazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Illicit
FluorouracilThe metabolism of Tapentadol can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Tapentadol can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.Approved, Withdrawn
FluphenazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fluphenazine.Approved
FlurazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flurazepam.Approved, Illicit
FluspirileneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fluspirilene.Approved
Fluticasone PropionateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fluticasone Propionate.Approved
FluvastatinThe metabolism of Tapentadol can be decreased when combined with Fluvastatin.Approved
FluvoxamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fluvoxamine.Approved, Investigational
FosphenytoinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fosphenytoin.Approved
FospropofolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.Approved, Illicit
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Tapentadol.Approved, Investigational
FurazolidoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Furazolidone.Approved, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Furosemide.Approved, Vet Approved
GabapentinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin.Approved, Investigational
gabapentin enacarbilTapentadol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.Approved
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tapentadol.Approved
Gamma Hydroxybutyric AcidTapentadol may increase the central nervous system depressant (CNS depressant) activities of Gamma Hydroxybutyric Acid.Approved, Illicit
GemfibrozilThe metabolism of Tapentadol can be decreased when combined with Gemfibrozil.Approved
GepironeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Gepirone.Investigational
GlutethimideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Glutethimide.Approved, Illicit
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrronium is combined with Tapentadol.Approved, Investigational, Vet Approved
GranisetronGranisetron may decrease the analgesic activities of Tapentadol.Approved, Investigational
GuanfacineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.Approved, Investigational
HalazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Illicit, Withdrawn
HaloperidolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Haloperidol.Approved
HalothaneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Halothane.Approved, Vet Approved
HeroinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Hexamethonium is combined with Tapentadol.Experimental
HexobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Hexobarbital.Approved
HomatropineThe risk or severity of adverse effects can be increased when Homatropine is combined with Tapentadol.Approved
HydracarbazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Hydracarbazine.Approved
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Hydrochlorothiazide.Approved, Vet Approved
HydrocodoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydroflumethiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Hydroflumethiazide.Approved
HydromorphoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Hydromorphone.Approved, Illicit
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may increase the analgesic activities of Tapentadol.Approved
HydroxyzineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Hydroxyzine.Approved
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Tapentadol.Approved
IloperidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.Approved
ImipramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Imipramine.Approved
IndalpineTapentadol may increase the serotonergic activities of Indalpine.Investigational, Withdrawn
IndapamideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Indapamide.Approved
IndinavirThe metabolism of Tapentadol can be decreased when combined with Indinavir.Approved
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Tapentadol.Approved
IproclozideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Iproclozide.Withdrawn
IproniazidThe risk or severity of adverse effects can be increased when Tapentadol is combined with Iproniazid.Withdrawn
IrbesartanThe metabolism of Tapentadol can be decreased when combined with Irbesartan.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Tapentadol is combined with Isocarboxazid.Approved
IsofluraneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Isoflurane.Approved, Vet Approved
IsoniazidThe metabolism of Tapentadol can be decreased when combined with Isoniazid.Approved
IsosorbideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Isosorbide.Approved
KetamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ketamine.Approved, Vet Approved
KetazolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ketazolam.Approved
KetobemidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ketobemidone.Approved
KetoconazoleThe metabolism of Tapentadol can be decreased when combined with Ketoconazole.Approved, Investigational
KW-3902The risk or severity of adverse effects can be increased when Tapentadol is combined with KW-3902.Investigational
LamotrigineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lamotrigine.Approved, Investigational
LeflunomideThe metabolism of Tapentadol can be decreased when combined with Leflunomide.Approved, Investigational
LevetiracetamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levetiracetam.Approved, Investigational
LevobupivacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levobupivacaine.Approved
LevocabastineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocabastine.Approved
LevocetirizineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.Approved
LevodopaTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levodopa.Approved
Levomethadyl AcetateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Tapentadol is combined with Levomilnacipran.Approved
LevorphanolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Levorphanol.Approved
LidocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lidocaine.Approved, Vet Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Tapentadol.Approved, Investigational
LisdexamfetamineLisdexamfetamine may increase the analgesic activities of Tapentadol.Approved, Investigational
LithiumTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lithium.Approved
LofentanilTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lofentanil.Illicit
LopinavirThe metabolism of Tapentadol can be decreased when combined with Lopinavir.Approved
LoratadineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Loratadine.Approved
LorazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lorazepam.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Tapentadol.Approved
LosartanThe metabolism of Tapentadol can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Tapentadol can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Loxapine.Approved
Lu AA21004Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Lu AA21004.Investigational
LuliconazoleThe serum concentration of Tapentadol can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Tapentadol can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Tapentadol can be decreased when combined with Lumefantrine.Approved
LurasidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.Approved
Magnesium SulfateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Magnesium Sulfate.Approved, Vet Approved
MannitolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Mannitol.Approved, Investigational
MaprotilineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Maprotiline.Approved
MebanazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Mebanazine.Withdrawn
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Tapentadol.Approved
MeclizineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Meclizine.Approved
MedetomidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Medetomidine.Vet Approved
MelatoninTapentadol may increase the central nervous system depressant (CNS depressant) activities of Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Melperone.Approved
MephedroneMephedrone may increase the analgesic activities of Tapentadol.Investigational
MephentermineMephentermine may increase the analgesic activities of Tapentadol.Approved
MepivacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Mepivacaine.Approved, Vet Approved
MeprobamateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.Approved, Illicit
MersalylThe risk or severity of adverse effects can be increased when Tapentadol is combined with Mersalyl.Approved
MesoridazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Mesoridazine.Approved
MetaxaloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.Approved
MethadoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methadone.Approved
Methadyl AcetateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methadyl Acetate.Approved, Illicit
MethamphetamineMethamphetamine may increase the analgesic activities of Tapentadol.Approved, Illicit
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Tapentadol.Approved
MethapyrileneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methapyrilene.Withdrawn
MethaqualoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methaqualone.Illicit, Withdrawn
MethazolamideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Methazolamide.Approved
MethocarbamolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.Approved, Vet Approved
MethohexitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methohexital.Approved
MethotrimeprazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methoxyflurane.Approved, Vet Approved
MethsuximideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methsuximide.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Methyclothiazide.Approved
Methylene blueThe risk or severity of adverse effects can be increased when Tapentadol is combined with Methylene blue.Investigational
MethylphenobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methylphenobarbital.Approved
MetixeneThe risk or severity of adverse effects can be increased when Metixene is combined with Tapentadol.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Metoclopramide.Approved, Investigational
MetolazoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Metolazone.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Tapentadol.Approved, Investigational
MetyrosineTapentadol may increase the sedative activities of Metyrosine.Approved
MidazolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Tapentadol can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Tapentadol.Approved
MinaprineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Minaprine.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved, Investigational
MirabegronThe metabolism of Tapentadol can be decreased when combined with Mirabegron.Approved
MirtazapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MMDAMMDA may increase the analgesic activities of Tapentadol.Experimental, Illicit
MoclobemideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Moclobemide.Approved
ModafinilThe metabolism of Tapentadol can be decreased when combined with Modafinil.Approved, Investigational
MolindoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Molindone.Approved
MoricizineMoricizine may increase the hypotensive activities of Tapentadol.Approved, Withdrawn
MorphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Morphine.Approved, Investigational
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when N-butylscopolammonium bromide is combined with Tapentadol.Vet Approved
NabiloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nabilone.Approved, Investigational
NalbuphineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nalbuphine.Approved
NaltrexoneThe therapeutic efficacy of Tapentadol can be decreased when used in combination with Naltrexone.Approved, Investigational, Vet Approved
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Tapentadol.Approved, Investigational
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Tapentadol.Approved, Withdrawn
NelfinavirThe metabolism of Tapentadol can be decreased when combined with Nelfinavir.Approved
NevirapineThe metabolism of Tapentadol can be decreased when combined with Nevirapine.Approved
NialamideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Nialamide.Withdrawn
NicardipineThe metabolism of Tapentadol can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Tapentadol can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
Nitrous oxideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nitrous oxide.Approved, Vet Approved
NormethadoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Normethadone.Approved, Illicit
NortriptylineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nortriptyline.Approved
NVA237The risk or severity of adverse effects can be increased when NVA237 is combined with Tapentadol.Investigational
OctamoxinThe risk or severity of adverse effects can be increased when Tapentadol is combined with Octamoxin.Withdrawn
OlanzapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Olanzapine.Approved, Investigational
OlopatadineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Olopatadine.Approved
OmeprazoleThe metabolism of Tapentadol can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ondansetron.Approved
OpiumTapentadol may increase the central nervous system depressant (CNS depressant) activities of Opium.Approved, Illicit
OrphenadrineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantTapentadol may increase the central nervous system depressant (CNS depressant) activities of Osanetant.Investigational
OxazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.Approved
OxetacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxetacaine.Investigational
OxprenololTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxprenolol.Approved
OxybuprocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxybuprocaine.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Tapentadol.Approved, Investigational
OxycodoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Tapentadol.Approved
PaliperidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.Approved
PalonosetronPalonosetron may decrease the analgesic activities of Tapentadol.Approved, Investigational
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Tapentadol.Approved
PanobinostatThe serum concentration of Tapentadol can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Tapentadol can be decreased when combined with Pantoprazole.Approved
ParaldehydeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
PargylineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Pargyline.Approved
ParoxetineThe metabolism of Tapentadol can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Tapentadol can be decreased when it is combined with Peginterferon alfa-2b.Approved
PegvisomantThe therapeutic efficacy of Pegvisomant can be decreased when used in combination with Tapentadol.Approved
PentazocineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pentazocine.Approved, Vet Approved
PentobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Tapentadol.Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved
PerazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Perazine.Investigational
PerospironeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Perospirone.Approved
PerphenazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Perphenazine.Approved
PethidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pethidine.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Phenelzine.Approved
PheniprazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Pheniprazine.Withdrawn
PhenobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.Approved
PhenoxyethanolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Phenoxyethanol.Approved
PhenoxypropazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Phenoxypropazine.Withdrawn
PhenterminePhentermine may increase the analgesic activities of Tapentadol.Approved, Illicit
PhenytoinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Phenytoin.Approved, Vet Approved
PimozideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
PipamperoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pipamperone.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Tapentadol.Approved
PipotiazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pipotiazine.Approved
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Tapentadol.Approved
PiretanideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Piretanide.Experimental
PiritramideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Piritramide.Investigational
PirlindoleThe risk or severity of adverse effects can be increased when Tapentadol is combined with Pirlindole.Approved
PivhydrazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Pivhydrazine.Withdrawn
PizotifenTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pizotifen.Approved
PolythiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Polythiazide.Approved
PomalidomideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pomalidomide.Approved
PotassiumThe risk or severity of adverse effects can be increased when Tapentadol is combined with Potassium.Approved
Potassium CitrateThe risk or severity of adverse effects can be increased when Tapentadol is combined with Potassium Citrate.Approved, Vet Approved
PramipexoleTapentadol may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pramocaine.Approved
PrazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Prazepam.Approved, Illicit
PregabalinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pregabalin.Approved, Illicit, Investigational
PregnanoloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pregnanolone.Investigational
PrilocaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Prilocaine.Approved
PrimidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Primidone.Approved, Vet Approved
ProcaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Procaine.Approved, Investigational, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Tapentadol.Approved
ProchlorperazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Prochlorperazine.Approved, Vet Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Tapentadol.Approved
PromazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Promazine.Approved, Vet Approved
PromethazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Promethazine.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Tapentadol.Approved
ProparacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Proparacaine.Approved, Vet Approved
PropericiazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Propericiazine.Approved
PropiopromazinePropiopromazine may increase the hypotensive activities of Tapentadol.Vet Approved
PropiverineThe risk or severity of adverse effects can be increased when Propiverine is combined with Tapentadol.Investigational
PropofolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Propofol.Approved, Investigational, Vet Approved
PropoxycaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Propoxycaine.Approved
ProthipendylThe risk or severity of adverse effects can be increased when Tapentadol is combined with Prothipendyl.Investigational
ProtriptylineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Protriptyline.Approved
PSD502Tapentadol may increase the central nervous system depressant (CNS depressant) activities of PSD502.Investigational
PseudoephedrinePseudoephedrine may increase the analgesic activities of Tapentadol.Approved
PyrimethamineThe metabolism of Tapentadol can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Quazepam.Approved, Illicit
QuetiapineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Quetiapine.Approved
QuinethazoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Quinethazone.Approved
QuinidineThe metabolism of Tapentadol can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Tapentadol can be decreased when combined with Quinine.Approved
RacloprideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Raclopride.Investigational
RamelteonTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ramelteon.Approved, Investigational
RamosetronTapentadol may increase the constipating activities of Ramosetron.Approved
RanolazineThe metabolism of Tapentadol can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Rasagiline.Approved
RemifentanilTapentadol may increase the central nervous system depressant (CNS depressant) activities of Remifentanil.Approved
RemoxiprideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.Approved, Withdrawn
ReserpineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Reserpine.Approved
RifampicinThe metabolism of Tapentadol can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Tapentadol can be increased when combined with Rifapentine.Approved
RisperidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Risperidone.Approved, Investigational
RitanserinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ritanserin.Investigational
RitobegronRitobegron may increase the analgesic activities of Tapentadol.Investigational
RitonavirThe metabolism of Tapentadol can be decreased when combined with Ritonavir.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Tapentadol.Approved
RolapitantThe metabolism of Tapentadol can be decreased when combined with Rolapitant.Approved
RolofyllineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Rolofylline.Investigational
RomifidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Romifidine.Vet Approved
RopiniroleTapentadol may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ropivacaine.Approved
RotigotineTapentadol may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tapentadol.Approved
S-EthylisothioureaTapentadol may increase the central nervous system depressant (CNS depressant) activities of S-Ethylisothiourea.Experimental
SafrazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Safrazine.Withdrawn
Sage 547Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Sage 547.Investigational
ScopolamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Scopolamine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Scopolamine butylbromide is combined with Tapentadol.Approved
SecobarbitalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleTapentadol may increase the central nervous system depressant (CNS depressant) activities of Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Tapentadol.Approved
SevofluraneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Tapentadol can be decreased when combined with Sildenafil.Approved, Investigational
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Tapentadol.Approved
SolifenacinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Tapentadol.Approved
SorafenibThe metabolism of Tapentadol can be decreased when combined with Sorafenib.Approved, Investigational
SpironolactoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Spironolactone.Approved
StiripentolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Stiripentol.Approved
SuccinylcholineSuccinylcholine may increase the bradycardic activities of Tapentadol.Approved
SufentanilTapentadol may increase the central nervous system depressant (CNS depressant) activities of Sufentanil.Approved, Investigational
SulfadiazineThe metabolism of Tapentadol can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Tapentadol can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Tapentadol can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Sulpiride.Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Tapentadol.Approved, Investigational
SuvorexantTapentadol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tandospirone.Investigational
TasimelteonTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Tapentadol.Approved
TemazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Temazepam.Approved
TerbinafineThe metabolism of Tapentadol can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TetrabenazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.Approved
TetracaineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tetracaine.Approved, Vet Approved
TetrodotoxinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tetrodotoxin.Investigational
ThalidomideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheobromineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Theobromine.Approved
ThiamylalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thiamylal.Approved, Vet Approved
ThiethylperazineThiethylperazine may increase the hypotensive activities of Tapentadol.Withdrawn
ThiopentalTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thiopental.Approved, Vet Approved
ThioproperazineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Thioproperazine.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Tapentadol.Approved
ThiothixeneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thiothixene.Approved
TiagabineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tiagabine.Approved
TiaprideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tiapride.Investigational
TicagrelorThe metabolism of Tapentadol can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Tapentadol can be decreased when combined with Ticlopidine.Approved
TicrynafenThe risk or severity of adverse effects can be increased when Tapentadol is combined with Ticrynafen.Withdrawn
TiletamineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tiletamine.Vet Approved
TiotropiumThe risk or severity of adverse effects can be increased when Tiotropium is combined with Tapentadol.Approved
TipranavirThe metabolism of Tapentadol can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tizanidine.Approved
TolbutamideThe metabolism of Tapentadol can be decreased when combined with Tolbutamide.Approved
TolcaponeTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.Approved, Withdrawn
ToloxatoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Toloxatone.Approved
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Tapentadol.Approved, Investigational
TolvaptanThe risk or severity of adverse effects can be increased when Tapentadol is combined with Tolvaptan.Approved
TopiramateTapentadol may increase the central nervous system depressant (CNS depressant) activities of Topiramate.Approved
TorasemideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Torasemide.Approved
TramadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tramadol.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tapentadol is combined with Tranylcypromine.Approved
TrazodoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Trazodone.Approved, Investigational
TriamtereneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Triamterene.Approved
TriazolamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Triazolam.Approved
TrichlormethiazideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Trichlormethiazide.Approved, Vet Approved
TrifluoperazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.Approved
TriflupromazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Triflupromazine.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Tapentadol.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Tapentadol.Approved
TrimethoprimThe metabolism of Tapentadol can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Trimipramine.Approved
TriprolidineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Triprolidine.Approved
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Tapentadol.Approved
TropisetronTropisetron may decrease the analgesic activities of Tapentadol.Investigational
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Tapentadol.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Tapentadol.Approved
Uc1010Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Uc1010.Investigational
UlaritideThe risk or severity of adverse effects can be increased when Tapentadol is combined with Ularitide.Investigational
UmeclidiniumThe risk or severity of adverse effects can be increased when Umeclidinium is combined with Tapentadol.Approved
Valproic AcidTapentadol may increase the central nervous system depressant (CNS depressant) activities of Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Tapentadol can be decreased when combined with Valsartan.Approved, Investigational
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Tapentadol.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Tapentadol.Approved
VigabatrinTapentadol may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Tapentadol is combined with Vilazodone.Approved
VoriconazoleThe metabolism of Tapentadol can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Vortioxetine.Approved
XylazineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Xylazine.Vet Approved
ZafirlukastThe metabolism of Tapentadol can be decreased when combined with Zafirlukast.Approved, Investigational
ZaleplonTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.Approved, Illicit, Investigational
ZiconotideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ziconotide.Approved
ZimelidineTapentadol may increase the serotonergic activities of Zimelidine.Withdrawn
ZiprasidoneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Ziprasidone.Approved
ZolazepamTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zolazepam.Vet Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Tapentadol.Approved, Investigational
ZolpidemTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zonisamide.Approved, Investigational
ZopicloneTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.Approved
ZotepineTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zotepine.Approved
ZuclopenthixolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.Approved, Investigational
Food Interactions
  • Food increases the AUC and Cmax of tapentadol. Despite this, tapentadol can be given without regards to food.
References
Synthesis Reference

Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, “PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF.” U.S. Patent US20120232306, issued September 13, 2012.

US20120232306
General References
  1. Tzschentke TM, Christoph T, Kogel B, Schiene K, Hennies HH, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J: (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007 Oct;323(1):265-76. Epub 2007 Jul 26. [PubMed:17656655 ]
  2. Gohler K, Brett M, Smit JW, Rengelshausen J, Terlinden R: Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Int J Clin Pharmacol Ther. 2013 Apr;51(4):338-48. doi: 10.5414/CP201722. [PubMed:23357834 ]
  3. Xu XS, Smit JW, Lin R, Stuyckens K, Terlinden R, Nandy P: Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010 Oct;49(10):671-82. doi: 10.2165/11535390-000000000-00000. [PubMed:20818833 ]
External Links
ATC CodesN02AX06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (666 KB)
MSDSDownload (481 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9937
Blood Brain Barrier+0.9232
Caco-2 permeable+0.7912
P-glycoprotein substrateSubstrate0.559
P-glycoprotein inhibitor INon-inhibitor0.9304
P-glycoprotein inhibitor IINon-inhibitor0.9408
Renal organic cation transporterNon-inhibitor0.6918
CYP450 2C9 substrateNon-substrate0.8085
CYP450 2D6 substrateNon-substrate0.5219
CYP450 3A4 substrateSubstrate0.5509
CYP450 1A2 substrateInhibitor0.6665
CYP450 2C9 inhibitorNon-inhibitor0.8856
CYP450 2D6 inhibitorNon-inhibitor0.5538
CYP450 2C19 inhibitorNon-inhibitor0.921
CYP450 3A4 inhibitorNon-inhibitor0.8389
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8875
Ames testNon AMES toxic0.6862
CarcinogenicityNon-carcinogens0.5177
BiodegradationNot ready biodegradable0.9421
Rat acute toxicity2.6035 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7187
hERG inhibition (predictor II)Inhibitor0.6155
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
SolutionOral20 mg/mL
TabletOral50 mg/1
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral50 mg/1
Tablet, film coatedOral75 mg/1
Tablet, film coated, extended releaseOral100 mg/1
Tablet, film coated, extended releaseOral150 mg/1
Tablet, film coated, extended releaseOral200 mg/1
Tablet, film coated, extended releaseOral250 mg/1
Tablet, film coated, extended releaseOral50 mg/1
Tablet, extended releaseOral100 mg
Tablet, extended releaseOral150 mg
Tablet, extended releaseOral200 mg
Tablet, extended releaseOral250 mg
Tablet, extended releaseOral50 mg
Tablet, multilayer, extended releaseOral100 mg
Tablet, multilayer, extended releaseOral50 mg
Tablet, multilayer, extended releaseOral75 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6071970 No1997-06-062017-06-06Us
US7994364 No2005-06-272025-06-27Us
US8075872 No2003-11-202023-11-20Us
US8114383 No2004-10-102024-10-10Us
US8309060 No2003-11-202023-11-20Us
US8420056 No2003-11-202023-11-20Us
US8536130 No2008-09-222028-09-22Us
USRE39593 No2002-08-052022-08-05Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.87 FDA label
pKa9.34 - 10.45 FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.78 mg/mLALOGPS
logP3.47ALOGPS
logP2.96ChemAxon
logS-2.5ALOGPS
pKa (Strongest Acidic)10.28ChemAxon
pKa (Strongest Basic)9.6ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity69.56 m3·mol-1ChemAxon
Polarizability26.58 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpropylamines. These are compounds containing a phenylpropylamine moiety, which consists of a phenyl group substituted at the third carbon by an propan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylpropylamines
Direct ParentPhenylpropylamines
Alternative Parents
Substituents
  • Phenylpropylamine
  • Phenylpropane
  • Aralkylamine
  • Phenol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Voltage-gated calcium channel activity
Specific Function:
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44778.855 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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Tzschentke TM, Christoph T, Kogel B, Schiene K, Hennies HH, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J: (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007 Oct;323(1):265-76. Epub 2007 Jul 26. [PubMed:17656655 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. 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. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurot...
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40368.235 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated potassium channel 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. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Raffa RB, Buschmann H, Christoph T, Eichenbaum G, Englberger W, Flores CM, Hertrampf T, Kogel B, Schiene K, Strassburger W, Terlinden R, Tzschentke TM: Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012 Jul;13(10):1437-49. doi: 10.1517/14656566.2012.696097. Epub 2012 Jun 15. [PubMed:22698264 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [PubMed:19356073 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Glucuronosyltransferase activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites. Is also active with androsterone, hyodeoxycholic acid and tetrachlorocatechol...
Gene Name:
UGT2B7
Uniprot ID:
P16662
Molecular Weight:
60694.12 Da
References
  1. Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [PubMed:19356073 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [PubMed:19356073 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [PubMed:19356073 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Kneip C, Terlinden R, Beier H, Chen G: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. [PubMed:19356073 ]
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Drug created on March 19, 2008 10:17 / Updated on December 04, 2016 02:45