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Identification
NameThioridazine
Accession NumberDB00679  (APRD00596)
TypeSmall Molecule
GroupsApproved
Description

A phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. It has little antiemetic activity. Thioridazine has a higher incidence of antimuscarinic effects, but a lower incidence of extrapyramidal symptoms, than chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p618)

Structure
Thumb
Synonyms
SynonymLanguageCode
10-[2-(1-Methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazineNot AvailableNot Available
2-Methylmercapto-10-(2-(N-methyl-2-piperidyl)ethyl)phenothiazineNot AvailableNot Available
3-Methylmercapto-N-(2'-(N-methyl-2-piperidyl)ethyl)phenothiazineNot AvailableNot Available
MallorolNot AvailableNot Available
MallorylNot AvailableNot Available
MelerilNot AvailableNot Available
MellarilNot AvailableNot Available
Mellaril-SNot AvailableNot Available
MelleretsNot AvailableNot Available
MelleretteNot AvailableNot Available
MellerilNot AvailableNot Available
OrsanilNot AvailableNot Available
SonapaxNot AvailableNot Available
ThioridazinNot AvailableNot Available
ThioridazinumNot AvailableNot Available
TioridazinaNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thioridazine Hydrochloridetablet, film coated10 mgoralMylan Pharmaceuticals Inc.1983-03-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated25 mgoralMylan Pharmaceuticals Inc.1983-03-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated50 mgoralMylan Pharmaceuticals Inc.1983-03-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated100 mgoralMylan Pharmaceuticals Inc.1983-11-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet25 mgoralREMEDYREPACK INC.2011-04-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet50 mgoralREMEDYREPACK INC.2011-04-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated10 mgoralMylan Institutional Inc.2012-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated25 mgoralMylan Institutional Inc.2012-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated50 mgoralMylan Institutional Inc.2012-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated100 mgoralMylan Institutional Inc.2012-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated10 mgoralMutual Pharmaceutical1988-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated25 mgoralMutual Pharmaceutical1988-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated50 mgoralMutual Pharmaceutical1988-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Thioridazine Hydrochloridetablet, film coated100 mgoralMutual Pharmaceutical1988-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
AldazineNot Available
MallorolNot Available
MelerilNot Available
MellarilNot Available
MelleretteNot Available
MellerettenNot Available
MellerilNot Available
NovoridazineNot Available
RidazinNot Available
RidazineNot Available
SonapaxNot Available
ThiorilNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Thioridazine Hydrochloride
130-61-0
Thumb
  • InChI Key: NZFNXWQNBYZDAQ-UHFFFAOYNA-N
  • Monoisotopic Mass: 406.130417961
  • Average Mass: 407.035
DBSALT000503
Categories
CAS number50-52-2
WeightAverage: 370.575
Monoisotopic: 370.153740222
Chemical FormulaC21H26N2S2
InChI KeyKLBQZWRITKRQQV-UHFFFAOYSA-N
InChI
InChI=1S/C21H26N2S2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
IUPAC Name
10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine
SMILES
CSC1=CC2=C(SC3=CC=CC=C3N2CCC2CCCCN2C)C=C1
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
  • Alkylarylthioether
  • Benzenoid
  • Piperidine
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Sulfenyl compound
  • Thioether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of schizophrenia and generalized anxiety disorder.
PharmacodynamicsThioridazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Thioridazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
Mechanism of actionThioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect, 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.
Absorption60%
Volume of distributionNot Available
Protein binding95%
Metabolism

Hepatic

Route of eliminationNot Available
Half life21-25 hours
ClearanceNot Available
ToxicityLD50=956-1034 mg/kg (Orally in rats); Agitation, blurred vision, coma, confusion, constipation, difficulty breathing, dilated or constricted pupils, diminished flow of urine, dry mouth, dry skin, excessively high or low body temperature, extremely low blood pressure, fluid in the lungs, heart abnormalities, inability to urinate, intestinal blockage, nasal congestion, restlessness, sedation, seizures, shock
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+0.9068
Blood Brain Barrier+0.9901
Caco-2 permeable+0.7912
P-glycoprotein substrateSubstrate0.7863
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IIInhibitor0.9115
Renal organic cation transporterInhibitor0.7943
CYP450 2C9 substrateNon-substrate0.7981
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.5068
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 substrateNon-inhibitor0.908
CYP450 2D6 substrateInhibitor0.8932
CYP450 2C19 substrateNon-inhibitor0.7697
CYP450 3A4 substrateNon-inhibitor0.8308
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5826
Ames testNon AMES toxic0.8703
CarcinogenicityNon-carcinogens0.9528
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5395 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.906
hERG inhibition (predictor II)Inhibitor0.8384
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
  • Actavis mid atlantic llc
  • Alpharma us pharmaceuticals division
  • Hi tech pharmacal co inc
  • Pharmaceutical assoc inc div beach products
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Wockhardt eu operations (swiss) ag
  • Roxane laboratories inc
  • Ivax pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral25 mg
Tabletoral50 mg
Tablet, film coatedoral10 mg
Tablet, film coatedoral100 mg
Tablet, film coatedoral25 mg
Tablet, film coatedoral50 mg
Prices
Unit descriptionCostUnit
Thioridazine hcl powder11.16USD g
Thioridazine HCl 200 mg tablet1.14USD tablet
Thioridazine HCl 150 mg tablet1.01USD tablet
Thioridazine HCl 100 mg tablet0.69USD tablet
Thioridazine 100 mg tablet0.67USD tablet
Thioridazine HCl 50 mg tablet0.61USD tablet
Thioridazine 50 mg tablet0.58USD tablet
Thioridazine HCl 25 mg tablet0.49USD tablet
Thioridazine 25 mg tablet0.47USD tablet
Thioridazine HCl 15 mg tablet0.45USD tablet
Thioridazine HCl 10 mg tablet0.35USD tablet
Thioridazine 10 mg tablet0.33USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point73 °CPhysProp
boiling point230 °C at 2.00E-02 mm HgPhysProp
water solubility0.0336 mg/LNot Available
logP5.90HANSCH,C ET AL. (1995)
pKa9.5EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.000855 mg/mLALOGPS
logP5.93ALOGPS
logP5.47ChemAxon
logS-5.6ALOGPS
pKa (Strongest Basic)8.93ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity113.52 m3·mol-1ChemAxon
Polarizability43.26 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.15 KB)
SpectraMS
References
Synthesis ReferenceNot Available
General ReferenceNot Available
External Links
ATC CodesN05AC02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (44.7 KB)
Interactions
Drug Interactions
Drug
AbirateroneCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
AclidiniumMay enhance the anticholinergic effect of Anticholinergic Agents.
AlmotriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Aluminum hydroxideMay decrease the absorption of Antipsychotic Agents (Phenothiazines).
AmiodaroneCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
AmisulprideAntipsychotic Agents may enhance the adverse/toxic effect of Amisulpride.
AmitriptylineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
AmoxapineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
AmphetamineMay diminish the stimulatory effect of Amphetamines.
AripiprazoleCYP2D6 Inhibitors (Strong) may increase the serum concentration of ARIPiprazole.
ArtemetherCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
AtomoxetineCYP2D6 Inhibitors (Strong) may increase the serum concentration of AtoMOXetine.
BenzphetamineMay diminish the stimulatory effect of Amphetamines.
BuprenorphineCNS Depressants may enhance the CNS depressant effect of Buprenorphine.
BupropionCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
BuspironeSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
CabergolineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Calcium carbonateMay decrease the absorption of Antipsychotic Agents (Phenothiazines).
CathinoneAntipsychotic Agents may diminish the stimulatory effect of Amphetamines.
CelecoxibCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
ChloroquineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
ChlorphenamineChlorpheniramine may enhance the arrhythmogenic effect of Thioridazine. Thioridazine may increase the serum concentration of Chlorpheniramine.
ChlorpromazineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
CimetidineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
CinacalcetCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
CitalopramSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ClobazamCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
ClomipramineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ClozapineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
CocaineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
CodeineCYP2D6 Inhibitors (Strong) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine.
CyclobenzaprineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
DapoxetineMay enhance the arrhythmogenic effect of Thioridazine. Dapoxetine may increase the serum concentration of Thioridazine.
DarifenacinCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
DarunavirMay increase the serum concentration of CYP2D6 Substrates.
DelavirdineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
DesipramineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
DesvenlafaxineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
DextroamphetamineMay diminish the stimulatory effect of Amphetamines.
DextromethorphanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
DihydroergotamineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
DonepezilAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
DoxylamineMay enhance the CNS depressant effect of CNS Depressants.
DronabinolMay enhance the CNS depressant effect of CNS Depressants.
DronedaroneCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
DuloxetineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
EletriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
EliglustatCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
Ergoloid mesylateSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ErgonovineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ErgotamineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
EscitalopramSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
FentanylSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
FesoterodineCYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s) of Fesoterodine.
FluoxetineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
FluvoxamineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
FrovatriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
GalantamineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
HaloperidolCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
HydrocodoneCNS Depressants may enhance the CNS depressant effect of Hydrocodone.
ImipramineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
IsocarboxazidSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
IsoniazidCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
ItoprideAnticholinergic Agents may diminish the therapeutic effect of Itopride.
LevomilnacipranSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
LinezolidSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
LisdexamfetamineMay diminish the stimulatory effect of Amphetamines.
LithiumLithium may enhance the neurotoxic effect of Antipsychotic Agents. Lithium may decrease the serum concentration of Antipsychotic Agents. Specifically noted with chlorpromazine.
LopinavirCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
LorcaserinSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
LumefantrineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
Magnesium oxideMay decrease the absorption of Antipsychotic Agents (Phenothiazines).
Magnesium SulfateMay enhance the CNS depressant effect of CNS Depressants.
MaprotilineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
MequitazineCYP2D6 Inhibitors (Strong) may increase the serum concentration of Mequitazine.
MethadoneSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
MethamphetamineMay diminish the stimulatory effect of Amphetamines.
MethotrimeprazineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
MethylergometrineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
MethylphenidateMay enhance the adverse/toxic effect of Methylphenidate. Methylphenidate may enhance the adverse/toxic effect of Antipsychotic Agents.
MetoclopramideMay enhance the adverse/toxic effect of Antipsychotic Agents.
MetoprololCYP2D6 Inhibitors may increase the serum concentration of Metoprolol.
MetyrosineCNS Depressants may enhance the sedative effect of Metyrosine.
MifepristoneMay enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents.
MilnacipranSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
MirabegronCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
MoclobemideMay increase the serum concentration of Thioridazine.
NabiloneMay enhance the CNS depressant effect of CNS Depressants.
NaratriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
NebivololCYP2D6 Inhibitors (Strong) may increase the serum concentration of Nebivolol.
NefazodoneSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
NilotinibCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
NortriptylineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
OrphenadrineCNS Depressants may enhance the CNS depressant effect of Orphenadrine.
PanobinostatCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
ParoxetineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
Peginterferon alfa-2bMay decrease the serum concentration of CYP2D6 Substrates. Peginterferon Alfa-2b may increase the serum concentration of CYP2D6 Substrates.
PerampanelMay enhance the CNS depressant effect of CNS Depressants.
PethidineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
PhendimetrazineMay diminish the stimulatory effect of Amphetamines.
PhenelzineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
PhentermineMay diminish the stimulatory effect of Amphetamines.
PimozideCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
PorfimerPhotosensitizing Agents may enhance the photosensitizing effect of Porfimer.
Potassium ChlorideAnticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride.
PramlintideMay enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract.
ProcarbazineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
PromazineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
PromethazineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ProtriptylineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
QuinidineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
QuinineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
RasagilineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
RitonavirCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
RivastigmineAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
RizatriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
RufinamideMay enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
SecretinAnticholinergic Agents may diminish the therapeutic effect of Secretin.
SelegilineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
SertralineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
SulpirideAntipsychotic Agents may enhance the adverse/toxic effect of Sulpiride.
SumatriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
SuvorexantCNS Depressants may enhance the CNS depressant effect of Suvorexant.
TamoxifenCYP2D6 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Tamoxifen. Specifically, strong CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites.
TamsulosinCYP2D6 Inhibitors (Strong) may increase the serum concentration of Tamsulosin.
TapentadolMay enhance the CNS depressant effect of CNS Depressants.
Tedizolid PhosphateSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
TetrabenazineTetrabenazine may enhance the adverse/toxic effect of Antipsychotic Agents.
ThalidomideCNS Depressants may enhance the CNS depressant effect of Thalidomide.
ThiopentalAntipsychotic Agents (Phenothiazines) may enhance the adverse/toxic effect of Thiopental.
TiclopidineCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
TiotropiumAnticholinergic Agents may enhance the anticholinergic effect of Tiotropium.
TipranavirCYP2D6 Inhibitors may increase the serum concentration of Thioridazine.
TopiramateAnticholinergic Agents may enhance the adverse/toxic effect of Topiramate.
TramadolSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
TranylcypromineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
TrimipramineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
VenlafaxineSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
VerteporfinPhotosensitizing Agents may enhance the photosensitizing effect of Verteporfin.
VilazodoneSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ZolmitriptanSerotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
ZolpidemCNS Depressants may enhance the CNS depressant effect of Zolpidem.
Food InteractionsNot Available

Targets

1. D(2) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

References:

  1. Seeman P: Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage. Acta Psychiatr Scand Suppl. 1990;358:14-20. Pubmed
  2. Assie MB, Sleight AJ, Koek W: Biphasic displacement of [3H]YM-09151-2 binding in the rat brain by thioridazine, risperidone and clozapine, but not by other antipsychotics. Eur J Pharmacol. 1993 Jun 24;237(2-3):183-9. Pubmed
  3. Dimpfel W, Spuler M, Wessel K: Different neuroleptics show common dose and time dependent effects in quantitative field potential analysis in freely moving rats. Psychopharmacology (Berl). 1992;107(2-3):195-202. Pubmed
  4. Barth VN, Chernet E, Martin LJ, Need AB, Rash KS, Morin M, Phebus LA: Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer. Life Sci. 2006 May 22;78(26):3007-12. Epub 2006 Jan 24. Pubmed
  5. Carey GJ, Bergman J: Discriminative-stimulus effects of clozapine in squirrel monkeys: comparison with conventional and novel antipsychotic drugs. Psychopharmacology (Berl). 1997 Aug;132(3):261-9. Pubmed

2. D(1A) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details

References:

  1. Hammock RG, Schroeder SR, Levine WR: The effect of clozapine on self-injurious behavior. J Autism Dev Disord. 1995 Dec;25(6):611-26. Pubmed

3. Alpha-1A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

References:

  1. Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. Pubmed
  2. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. Pubmed

4. Alpha-1B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1B adrenergic receptor P35368 Details

References:

  1. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. Pubmed

5. 5-hydroxytryptamine receptor 2A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

References:

  1. Andree TH, Mikuni M, Tong CY, Koenig JI, Meltzer HY: Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex. J Neurochem. 1986 Jan;46(1):191-7. Pubmed
  2. Canton H, Verriele L, Millan MJ: Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics. Neurosci Lett. 1994 Nov 7;181(1-2):65-8. Pubmed
  3. Burki HR: Binding of psychoactive drugs to rat brain amine receptors, measured ex vivo, and their effects on the metabolism of biogenic amines. Naunyn Schmiedebergs Arch Pharmacol. 1986 Mar;332(3):258-66. Pubmed
  4. Costall B, Naylor RJ: Behavioural interactions between 5-hydroxytryptophan, neuroleptic agents and 5-HT receptor antagonists in modifying rodent responding to aversive situations. Br J Pharmacol. 1995 Dec;116(7):2989-99. Pubmed
  5. Morisset S, Sahm UG, Traiffort E, Tardivel-Lacombe J, Arrang JM, Schwartz JC: Atypical neuroleptics enhance histamine turnover in brain via 5-Hydroxytryptamine2A receptor blockade. J Pharmacol Exp Ther. 1999 Feb;288(2):590-6. Pubmed

6. Potassium voltage-gated channel subfamily H member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Potassium voltage-gated channel subfamily H member 2 Q12809 Details

References:

  1. Milnes JT, Witchel HJ, Leaney JL, Leishman DJ, Hancox JC: hERG K+ channel blockade by the antipsychotic drug thioridazine: An obligatory role for the S6 helix residue F656. Biochem Biophys Res Commun. 2006 Dec 8;351(1):273-80. Epub 2006 Oct 23. Pubmed

Enzymes

1. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

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. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Otani K, Aoshima T: Pharmacogenetics of classical and new antipsychotic drugs. Ther Drug Monit. 2000 Feb;22(1):118-21. Pubmed
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  3. 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. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

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. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

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. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

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. Epub 2009 Nov 24. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11