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Identification
NameTrifluoperazine
Accession NumberDB00831  (APRD00173, DB08616)
TypeSmall Molecule
GroupsApproved
Description

A phenothiazine with actions similar to chlorpromazine. It is used as an antipsychotic and an antiemetic. [PubChem]

Structure
Thumb
Synonyms
10-[3-(4-Methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
10-[3-(4-METHYL-piperazin-1-yl)-propyl]-2-trifluoromethyl-10H-phenothiazine
Trifluoperazina
Trifluoperazine
Trifluoperazinum
Trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine
Trifluoroperazine
Trifluperazine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Novo-flurazine Tab 1mgtablet1.18 mgoralNovopharm Limited1971-12-311996-09-10Canada
Novo-flurazine Tab 20mgtablet23.6 mgoralNovopharm Limited1971-12-311996-09-10Canada
Novo-trifluzine - Tab 10mgtablet11.8 mgoralNovopharm Limited1971-12-312013-06-03Canada
Novo-trifluzine - Tab 2mgtablet2.36 mgoralNovopharm Limited1971-12-312013-06-03Canada
Novo-trifluzine - Tab 5mgtablet5.9 mgoralNovopharm Limited1971-12-312013-06-03Canada
PMS Trifluoperazine HCl Syrup 11.8mg/mlsyrup10 mgoralPharmascience Inc1988-12-312012-03-14Canada
PMS Trifluoperazine Tab 10mgtablet10 mgoralPharmascience Inc1988-12-312012-03-14Canada
PMS Trifluoperazine Tab 1mgtablet1 mgoralPharmascience Inc1988-12-311996-09-10Canada
PMS Trifluoperazine Tab 20mgtablet20 mgoralPharmascience Inc1988-12-311996-09-10Canada
PMS Trifluoperazine Tab 2mgtablet2 mgoralPharmascience Inc1988-12-312012-03-14Canada
PMS Trifluoperazine Tab 5mgtablet5 mgoralPharmascience Inc1988-12-312012-03-14Canada
PMS-trifluoperazine HCl Syr 1.18mg/mlsyrup1 mgoralPharmascience Inc1988-12-312012-10-17Canada
Stelazine Tab 10mgtablet10 mgoralSmithkline Beecham Pharma Division Of Smithkline Beecham Inc1993-12-312000-11-30Canada
Stelazine Tab 1mgtablet1 mgoralSmithkline Beecham Pharma Division Of Smithkline Beecham Inc1993-12-312000-11-30Canada
Stelazine Tab 2mgtablet2 mgoralSmithkline Beecham Pharma Division Of Smithkline Beecham Inc1992-12-312000-10-18Canada
Stelazine Tab 5mgtablet5 mgoralSmithkline Beecham Pharma Division Of Smithkline Beecham Inc1993-12-312000-09-28Canada
Terfluzine Concentratesyrup10 mgoralValeant Canada Lp Valeant Canada S.E.C.1974-12-312011-08-03Canada
Terfluzine-1tablet1 mgoralValeant Canada Lp Valeant Canada S.E.C.1974-12-312011-08-03Canada
Terfluzine-10tablet10 mgoralValeant Canada Lp Valeant Canada S.E.C.1973-12-312011-08-03Canada
Terfluzine-2tablet2 mgoralValeant Canada Lp Valeant Canada S.E.C.1978-12-312011-08-03Canada
Terfluzine-5tablet5 mgoralValeant Canada Lp Valeant Canada S.E.C.1968-12-312011-08-03Canada
Trifluoperazinetablet5 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Trifluoperazinetablet20 mgoralAa Pharma Inc1984-12-31Not applicableCanada
Trifluoperazinetablet1 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Trifluoperazinetablet10 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Trifluoperazinetablet2 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Trifluoperazine 10mg Tabletstablet10 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Trifluoperazine 1mg Tabletstablet1 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Trifluoperazine 2mg Tabletstablet2 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Trifluoperazine 5mg Tabletstablet5 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Trifluoperazine Tab 10mgtablet10 mgoralPro Doc Limitee1977-12-312010-07-13Canada
Trifluoperazine Tab 10mgtablet10 mgoralDuchesnay Inc1978-12-312003-07-18Canada
Trifluoperazine Tab 1mgtablet1 mgoralPro Doc Limitee1976-12-312010-07-13Canada
Trifluoperazine Tab 1mgtablet1 mgoralDuchesnay Inc1978-12-312003-07-18Canada
Trifluoperazine Tab 2mgtablet2 mgoralPro Doc Limitee1976-12-312010-07-13Canada
Trifluoperazine Tab 2mgtablet2 mgoralDuchesnay Inc1978-12-312003-07-18Canada
Trifluoperazine Tab 5mgtablet5 mgoralDuchesnay Inc1978-12-312003-07-18Canada
Trifluoperazine Tab 5mgtablet5 mgoralPro Doc Limitee1976-12-312010-07-13Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trifluoperazinetablet, film coated2 mg/1oralSTAT Rx USA LLC1981-11-20Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated1 mg/1oralLake Erie Medical DBA Quality Care Products LLC2012-08-22Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated1 mg/1oralMylan Pharmaceuticals Inc.1997-08-29Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated1 mg/1oralMylan Institutional Inc.1998-03-04Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated10 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated5 mg/1oralSandoz Inc1981-11-20Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated2 mg/1oralState of Florida DOH Central Pharmacy2013-01-01Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated2 mg/1oralSandoz Inc1981-11-20Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated10 mg/1oralUpsher Smith Laboratories, Inc.2015-03-09Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated1 mg/1oralSandoz Inc1981-11-20Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated5 mg/1oralREMEDYREPACK INC.2012-09-27Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated5 mg/1oralUpsher Smith Laboratories, Inc.2015-03-09Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated10 mg/1oralMylan Pharmaceuticals Inc.1997-08-29Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated10 mg/1oralMylan Institutional Inc.1998-03-04Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated2 mg/1oralUpsher Smith Laboratories, Inc.2015-03-09Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated5 mg/1oralMylan Pharmaceuticals Inc.1997-08-29Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated5 mg/1oralMylan Institutional Inc.1998-03-04Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated1 mg/1oralUpsher Smith Laboratories, Inc.2015-03-09Not applicableUs
Trifluoperazine Hydrochloridetablet1 mg/1oralREMEDYREPACK INC.2011-12-08Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated2 mg/1oralMylan Pharmaceuticals Inc.1997-08-29Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated2 mg/1oralMylan Institutional Inc.1998-03-04Not applicableUs
Trifluoperazine Hydrochloridetablet, film coated10 mg/1oralSandoz Inc1981-11-20Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EskazineNot Available
EskazinylNot Available
JatroneuralNot Available
ModalinaNot Available
StelazineNot Available
TerfluzineNot Available
TrifluoperazNot Available
TriftazinNot Available
Brand mixtures
NameLabellerIngredients
Stelabid ForteGlaxosmithkline Inc
Stelabid No 1Glaxosmithkline Inc
Stelabid No 2Glaxosmithkline Inc
Salts
Name/CASStructureProperties
Trifluoperazine Hydrochloride
440-17-5
Thumb
  • InChI Key: BXDAOUXDMHXPDI-UHFFFAOYSA-N
  • Monoisotopic Mass: 479.117658566
  • Average Mass: 480.417
DBSALT000569
Categories
UNII214IZI85K3
CAS number117-89-5
WeightAverage: 407.496
Monoisotopic: 407.164303088
Chemical FormulaC21H24F3N3S
InChI KeyInChIKey=ZEWQUBUPAILYHI-UHFFFAOYSA-N
InChI
InChI=1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9-14H2,1H3
IUPAC Name
10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
SMILES
CN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiazines
Sub ClassPhenothiazines
Direct ParentPhenothiazines
Alternative Parents
Substituents
  • Phenothiazine
  • Alkyldiarylamine
  • Diarylthioether
  • N-alkylpiperazine
  • N-methylpiperazine
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation.
PharmacodynamicsTrifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
Mechanism of actionTrifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half life10-20 hours
ClearanceNot Available
ToxicitySymptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9946
Blood Brain Barrier+0.9814
Caco-2 permeable+0.6856
P-glycoprotein substrateSubstrate0.8529
P-glycoprotein inhibitor IInhibitor0.9058
P-glycoprotein inhibitor IIInhibitor0.9089
Renal organic cation transporterInhibitor0.6842
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9109
CYP450 3A4 substrateNon-substrate0.594
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.9144
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.8995
CYP450 3A4 inhibitorNon-inhibitor0.5618
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8247
Ames testNon AMES toxic0.8944
CarcinogenicityNon-carcinogens0.9446
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8411 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9327
hERG inhibition (predictor II)Inhibitor0.8556
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Glaxosmithkline
  • Sandoz inc
  • Wockhardt eu operations (swiss) ag
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Ivax pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral1.18 mg
Tabletoral23.6 mg
Tabletoral11.8 mg
Tabletoral2.36 mg
Tabletoral5.9 mg
Syruporal1 mg
Tabletoral
Syruporal10 mg
Tabletoral1 mg
Tabletoral10 mg
Tabletoral2 mg
Tabletoral20 mg
Tabletoral5 mg
Tabletoral1 mg/1
Tablet, film coatedoral1 mg/1
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral2 mg/1
Tablet, film coatedoral5 mg/1
Prices
Unit descriptionCostUnit
Trifluoperazine HCl 10 mg tablet1.7USD tablet
Trifluoperazine 10 mg tablet1.63USD tablet
Trifluoperazine HCl 5 mg tablet1.09USD tablet
Trifluoperazine 5 mg tablet1.08USD tablet
Trifluoperazine HCl 2 mg tablet0.89USD tablet
Trifluoperazine 2 mg tablet0.86USD tablet
Trifluoperazine HCl 1 mg tablet0.59USD tablet
Trifluoperazine 1 mg tablet0.58USD tablet
Apo-Trifluoperazine 20 mg Tablet0.58USD tablet
Apo-Trifluoperazine 10 mg Tablet0.29USD tablet
Apo-Trifluoperazine 5 mg Tablet0.24USD tablet
Apo-Trifluoperazine 2 mg Tablet0.18USD tablet
Apo-Trifluoperazine 1 mg Tablet0.14USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility12.2 mg/L (at 24 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP5.03HANSCH,C ET AL. (1995)
logS-4.52ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00876 mg/mLALOGPS
logP4.87ALOGPS
logP4.66ChemAxon
logS-4.7ALOGPS
pKa (Strongest Basic)8.39ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area9.72 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity110.98 m3·mol-1ChemAxon
Polarizability41.94 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.1 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-03kc-9740000000-e505b8906d154e2285a4View in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05AB06
AHFS Codes
  • 28:16.08.24
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Trifluoperazine can be increased when it is combined with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Trifluoperazine.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Trifluoperazine.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Trifluoperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
AmisulprideThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Trifluoperazine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Trifluoperazine.
AmphetamineTrifluoperazine may decrease the stimulatory activities of Amphetamine.
AzelastineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Trifluoperazine.
BenzphetamineTrifluoperazine may decrease the stimulatory activities of Benzphetamine.
BortezomibThe metabolism of Trifluoperazine can be decreased when combined with Bortezomib.
Botulinum Toxin Type ATrifluoperazine may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BTrifluoperazine may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
BromocriptineThe therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Bromocriptine.
BuprenorphineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Trifluoperazine.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trifluoperazine.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Trifluoperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
CarbamazepineThe metabolism of Trifluoperazine can be increased when combined with Carbamazepine.
CathinoneTrifluoperazine may decrease the stimulatory activities of Cathinone.
Cimetropium BromideTrifluoperazine may increase the anticholinergic activities of Cimetropium Bromide.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Trifluoperazine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Trifluoperazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Trifluoperazine.
Cyproterone acetateThe serum concentration of Trifluoperazine can be decreased when it is combined with Cyproterone acetate.
DeferasiroxThe serum concentration of Trifluoperazine can be increased when it is combined with Deferasirox.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Trifluoperazine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Trifluoperazine.
DextroamphetamineTrifluoperazine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Trifluoperazine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Trifluoperazine.
DonepezilDonepezil may increase the central neurotoxic activities of Trifluoperazine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Trifluoperazine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Trifluoperazine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Trifluoperazine.
EluxadolineTrifluoperazine may increase the activities of Eluxadoline.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Trifluoperazine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Trifluoperazine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Trifluoperazine.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Trifluoperazine.
EthanolTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Trifluoperazine.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Trifluoperazine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Trifluoperazine.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Trifluoperazine.
GalantamineGalantamine may increase the central neurotoxic activities of Trifluoperazine.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Glucagon recombinant.
HydrocodoneTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Trifluoperazine.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Trifluoperazine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Trifluoperazine.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Trifluoperazine.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Trifluoperazine.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Trifluoperazine.
LisdexamfetamineTrifluoperazine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Trifluoperazine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Trifluoperazine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Trifluoperazine.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Trifluoperazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Trifluoperazine.
MequitazineTrifluoperazine may increase the arrhythmogenic activities of Mequitazine.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Trifluoperazine.
MethamphetamineTrifluoperazine may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Trifluoperazine.
MetyrosineTrifluoperazine may increase the sedative activities of Metyrosine.
MexiletineThe metabolism of Trifluoperazine can be decreased when combined with Mexiletine.
MianserinMianserin may increase the anticholinergic activities of Trifluoperazine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Trifluoperazine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
MirabegronThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Mirabegron.
MirtazapineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Trifluoperazine.
MorphineTrifluoperazine may increase the hypotensive activities of Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Trifluoperazine.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Trifluoperazine.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Trifluoperazine.
OrphenadrineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Trifluoperazine can be increased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Trifluoperazine.
PhendimetrazineTrifluoperazine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Trifluoperazine.
PhentermineTrifluoperazine may decrease the stimulatory activities of Phentermine.
PorfimerTrifluoperazine may increase the photosensitizing activities of Porfimer.
Potassium ChlorideTrifluoperazine may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Trifluoperazine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Trifluoperazine.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Trifluoperazine.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Trifluoperazine.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Trifluoperazine.
PyrimethamineThe serum concentration of Trifluoperazine can be increased when it is combined with Pyrimethamine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Trifluoperazine.
RamosetronTrifluoperazine may increase the activities of Ramosetron.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Trifluoperazine.
RivastigmineRivastigmine may increase the central neurotoxic activities of Trifluoperazine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Trifluoperazine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Trifluoperazine.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Trifluoperazine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Trifluoperazine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Trifluoperazine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
SulpirideThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Trifluoperazine.
SuvorexantTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Trifluoperazine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Trifluoperazine.
TeriflunomideThe serum concentration of Trifluoperazine can be decreased when it is combined with Teriflunomide.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Trifluoperazine.
ThalidomideTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThiopentalThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Thiopental.
TiotropiumTrifluoperazine may increase the anticholinergic activities of Tiotropium.
TopiramateThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Trifluoperazine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Trifluoperazine.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Trifluoperazine.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Trifluoperazine.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Trifluoperazine.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Trifluoperazine.
VemurafenibThe serum concentration of Trifluoperazine can be increased when it is combined with Vemurafenib.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Trifluoperazine.
VerteporfinTrifluoperazine may increase the photosensitizing activities of Verteporfin.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Trifluoperazine.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Trifluoperazine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Trifluoperazine.
ZolpidemTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706 ]
  3. Lahti RA, Evans DL, Stratman NC, Figur LM: Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur J Pharmacol. 1993 Jun 4;236(3):483-6. [PubMed:8102973 ]
  4. Schmidt MH, Lee T: Investigation of striatal dopamine D2 receptor acquisition following prenatal neuroleptic exposure. Psychiatry Res. 1991 Mar;36(3):319-28. [PubMed:1676523 ]
  5. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. [PubMed:15695070 ]
  6. Seeman P, Lee T, Chau-Wong M, Wong K: Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976 Jun 24;261(5562):717-9. [PubMed:945467 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Clathrin light chain binding
Specific Function:
Interacts with clathrin light chain A and stimulates clathrin self-assembly and clathrin-mediated endocytosis.
Gene Name:
CALY
Uniprot ID:
Q9NYX4
Molecular Weight:
23433.49 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Seeman P, Lee T, Chau-Wong M, Wong K: Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976 Jun 24;261(5562):717-9. [PubMed:945467 ]
  3. Madrid PB, Polgar WE, Toll L, Tanga MJ: Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3014-7. Epub 2007 Mar 24. [PubMed:17407813 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Fujinaga M, Hoffman BB, Baden JM: Receptor subtype and intracellular signal transduction pathway associated with situs inversus induced by alpha 1 adrenergic stimulation in rat embryos. Dev Biol. 1994 Apr;162(2):558-67. [PubMed:8150214 ]
  4. Huerta-Bahena J, Villalobos-Molina R, Garcia-Sainz JA: Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects. Mol Pharmacol. 1983 Jan;23(1):67-70. [PubMed:6135146 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Titin binding
Specific Function:
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Torres-Piedra M, Figueroa M, Hernandez-Abreu O, Ibarra-Barajas M, Navarrete-Vazquez G, Estrada-Soto S: Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. Bioorg Med Chem. 2011 Jan 1;19(1):542-6. doi: 10.1016/j.bmc.2010.10.063. Epub 2010 Nov 4. [PubMed:21129983 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Troponin t binding
Specific Function:
Troponin is the central regulatory protein of striated muscle contraction. Tn consists of three components: Tn-I which is the inhibitor of actomyosin ATPase, Tn-T which contains the binding site for tropomyosin and Tn-C. The binding of calcium to Tn-C abolishes the inhibitory action of Tn on actin filaments.
Gene Name:
TNNC1
Uniprot ID:
P63316
Molecular Weight:
18402.36 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Kleerekoper Q, Liu W, Choi D, Putkey JA: Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C. J Biol Chem. 1998 Apr 3;273(14):8153-60. [PubMed:9525919 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Rage receptor binding
Specific Function:
Not Available
Gene Name:
S100A4
Uniprot ID:
P26447
Molecular Weight:
11728.41 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
  2. Malashkevich VN, Dulyaninova NG, Ramagopal UA, Liriano MA, Varney KM, Knight D, Brenowitz M, Weber DJ, Almo SC, Bresnick AR: Phenothiazines inhibit S100A4 function by inducing protein oligomerization. Proc Natl Acad Sci U S A. 2010 May 11;107(19):8605-10. doi: 10.1073/pnas.0913660107. Epub 2010 Apr 26. [PubMed:20421509 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
conversion inhibitor
General Function:
Xanthine oxidase activity
Specific Function:
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro).
Gene Name:
XDH
Uniprot ID:
P47989
Molecular Weight:
146422.99 Da
References
  1. Hirata Y, Ishii K, Taguchi T, Suita S, Takeshige K: Conversion of xanthine dehydrogenase to xanthine oxidase during ischemia of the rat small intestine and the effect of trifluoperazine on the conversion. J Pediatr Surg. 1993 Apr;28(4):597-600. [PubMed:8483075 ]
  2. Greene EL, Paller MS: Calcium and free radicals in hypoxia/reoxygenation injury of renal epithelial cells. Am J Physiol. 1994 Jan;266(1 Pt 2):F13-20. [PubMed:8304479 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Protein homodimerization activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1 (By similarity).
Gene Name:
UGT1A4
Uniprot ID:
P22310
Molecular Weight:
60024.535 Da
References
  1. Kerdpin O, Mackenzie PI, Bowalgaha K, Finel M, Miners JO: Influence of N-terminal domain histidine and proline residues on the substrate selectivities of human UDP-glucuronosyltransferase 1A1, 1A6, 1A9, 2B7, and 2B10. Drug Metab Dispos. 2009 Sep;37(9):1948-55. doi: 10.1124/dmd.109.028225. Epub 2009 Jun 1. [PubMed:19487247 ]
  2. Fujiwara R, Nakajima M, Yamanaka H, Katoh M, Yokoi T: Interactions between human UGT1A1, UGT1A4, and UGT1A6 affect their enzymatic activities. Drug Metab Dispos. 2007 Oct;35(10):1781-7. Epub 2007 Jul 9. [PubMed:17620344 ]
  3. Uchaipichat V, Mackenzie PI, Elliot DJ, Miners JO: Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) "probes" for human udp-glucuronosyltransferases. Drug Metab Dispos. 2006 Mar;34(3):449-56. Epub 2005 Dec 28. [PubMed:16381668 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12