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Identification
NamePimozide
Accession NumberDB01100  (APRD00218)
TypeSmall Molecule
GroupsApproved
Description

A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to haloperidol for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)

Structure
Thumb
Synonyms
SynonymLanguageCode
HalomonthNot AvailableNot Available
NeoperidoleNot AvailableNot Available
OpiranNot AvailableNot Available
OrapNot AvailableNot Available
PimozidaSpanishINN
PimozideNot AvailableNot Available
PimozidumLatinINN
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Oraptablet1 mgoralTeva Select Brands2000-06-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Oraptablet2 mgoralTeva Select Brands1990-09-302017-10-31Us 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Oraptablet2 mgoralTeva Select Brands2014-10-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Oraptablet4 mgoralPendopharm Division Of De Pharmascience IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Oraptablet2 mgoralPendopharm Division Of De Pharmascience IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pimozidetablet2 mgoralAa Pharma IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Pimozidetablet4 mgoralAa Pharma IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot Available
International Brands
NameCompany
NeoperidoleNot Available
OpiranNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number2062-78-4
WeightAverage: 461.5462
Monoisotopic: 461.227868975
Chemical FormulaC28H29F2N3O
InChI KeyYVUQSNJEYSNKRX-UHFFFAOYSA-N
InChI
InChI=1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34)
IUPAC Name
1-{1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
SMILES
FC1=CC=C(C=C1)C(CCCN1CCC(CC1)N1C(=O)NC2=CC=CC=C12)C1=CC=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylbutylamine
  • Benzimidazole
  • Aralkylamine
  • Halobenzene
  • Fluorobenzene
  • 4-aminopiperidine
  • Piperidine
  • N-substituted imidazole
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment.
PharmacodynamicsPimozide is an orally active antipsychotic drug product which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide's therapeutic and untoward effects. In addition, pimozide, in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized. Pimozide also has less potential for inducing sedation and hypotension as it has more specific dopamine receptor blocking activity than other neuroleptic agents (and is therefore a suitable alternative to haloperidol).
Mechanism of actionThe ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be primarily a function of its dopaminergic blocking activity. Pimozide binds and inhibits the dopamine D2 receptor in the CNS.
AbsorptionGreater than 50% absorption after oral administration. Serum peak appears 6-8 hours post ingestion.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Notable first-pass metabolism in the liver, primarily by N-dealkylation via the cytochrome P450 isoenzymes CYP3A and CYP1A2 (and possibly CYP2D6). The activity of the two major metabolites has not been determined.

Route of eliminationNot Available
Half life29 ± 10 hours (single-dose study of healthy volunteers).
ClearanceNot Available
ToxicityLD50 = 1100 mg/kg (rat, oral), 228 mg/kg (mouse, oral)
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+0.9974
Blood Brain Barrier+0.9685
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6639
P-glycoprotein inhibitor IInhibitor0.8842
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterInhibitor0.7255
CYP450 2C9 substrateNon-substrate0.7829
CYP450 2D6 substrateNon-substrate0.9112
CYP450 3A4 substrateSubstrate0.6579
CYP450 1A2 substrateInhibitor0.9062
CYP450 2C9 substrateNon-inhibitor0.907
CYP450 2D6 substrateInhibitor0.8932
CYP450 2C19 substrateNon-inhibitor0.9026
CYP450 3A4 substrateInhibitor0.686
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9217
Ames testNon AMES toxic0.7856
CarcinogenicityNon-carcinogens0.9348
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5907 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6925
hERG inhibition (predictor II)Inhibitor0.9192
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg
Tabletoral2 mg
Tabletoral4 mg
Prices
Unit descriptionCostUnit
Orap 1 mg tablet1.22USD tablet
Orap 2 mg tablet1.17USD tablet
Orap 4 mg Tablet0.47USD tablet
Apo-Pimozide 4 mg Tablet0.43USD tablet
Apo-Pimozide 2 mg Tablet0.24USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point214-218 °CPhysProp
water solubility10 mg/L (at 25 °C)MERCK INDEX (1996)
logP6.30HANSCH,C ET AL. (1995)
pKa8.63EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.00173 mg/mLALOGPS
logP6.36ALOGPS
logP5.83ChemAxon
logS-5.4ALOGPS
pKa (Strongest Acidic)12.9ChemAxon
pKa (Strongest Basic)8.38ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area35.58 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity132.21 m3·mol-1ChemAxon
Polarizability50.04 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraMS
References
Synthesis ReferenceNot Available
General ReferenceNot Available
External Links
ATC CodesN05AG02
AHFS Codes
  • 28:16.08.92
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (29 KB)
Interactions
Drug Interactions
Drug
AbirateroneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
AcetaminophenCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
AcetazolamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
AmiodaroneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
AmlodipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
AnastrozoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
ApomorphineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
AprepitantAprepitant may increase the serum concentration of Pimozide.
AtazanavirProtease Inhibitors may increase the serum concentration of Pimozide.
AtomoxetineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
AtorvastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
AzelastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
BatimastatMay increase the serum concentration of Pimozide.
BenzphetamineMay diminish the stimulatory effect of Amphetamines.
BicalutamideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
BiotinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
BoceprevirMay increase the serum concentration of Pimozide.
BortezomibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
BromocriptineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
BuprenorphineCNS Depressants may enhance the CNS depressant effect of Buprenorphine.
BupropionCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
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.
ButalbitalCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
CanagliflozinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
CarfilzomibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
CathinoneAntipsychotic Agents may diminish the stimulatory effect of Amphetamines.
ChlorzoxazoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
CimetidineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
CinacalcetCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
CisaprideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
ClarithromycinMacrolide Antibiotics may enhance the QTc-prolonging effect of Pimozide. Macrolide Antibiotics may decrease the metabolism of Pimozide. This mechanism may not apply to azithromycin.
ClemastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
ClotrimazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
ClozapineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
CocaineCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimozide.
CrizotinibMay enhance the QTc-prolonging effect of Pimozide. Crizotinib may increase the serum concentration of Pimozide.
CrofelemerCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
CyclophosphamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
Cyproterone acetateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DalfopristinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DanazolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DarifenacinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DarunavirProtease Inhibitors may increase the serum concentration of Pimozide.
DasatinibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
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.
DesogestrelCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
DiazepamCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DihydrocodeineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
DiltiazemCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
DisulfiramCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DocetaxelCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DonepezilAcetylcholinesterase Inhibitors (Central) may enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients.
DoxycyclineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
DoxylamineMay enhance the CNS depressant effect of CNS Depressants.
DronabinolMay enhance the CNS depressant effect of CNS Depressants.
DronedaroneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
DrospirenoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
EliglustatCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
EntacaponeCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
EnzalutamideMay decrease the serum concentration of Pimozide.
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.
EribulinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
Ethinyl EstradiolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
EthynodiolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
EtoposideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
FelodipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
FluconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the arrhythmogenic effect of Pimozide. Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Pimozide. This increase in serum concentrations may lead to QTc interval prolongation and ventricular arrhythmias. Applicable Isavuconazonium considerations are addressed in separate monographs.
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.
Fluticasone PropionateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
FluvastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
FosamprenavirProtease Inhibitors may increase the serum concentration of Pimozide.
FosaprepitantMay increase the serum concentration of Pimozide. The active metabolite aprepitant is likely responsible for this effect.
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.
GlyburideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
Glycerol PhenylbutyrateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
HydralazineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
HydrocodoneCNS Depressants may enhance the CNS depressant effect of Hydrocodone.
IfosfamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
IloperidoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
IndinavirProtease Inhibitors may increase the serum concentration of Pimozide.
IrbesartanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
IsavuconazoniumCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
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.
IsoflurophateMay increase the serum concentration of Pimozide.
IsomethepteneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
IsoniazidCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
IsradipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
ItoprideAnticholinergic Agents may diminish the therapeutic effect of Itopride.
ItraconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the arrhythmogenic effect of Pimozide. Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Pimozide. This increase in serum concentrations may lead to QTc interval prolongation and ventricular arrhythmias. Applicable Isavuconazonium considerations are addressed in separate monographs.
IvacaftorCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
LansoprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
LapatinibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
LomitapideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
LomustineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
LopinavirProtease Inhibitors may increase the serum concentration of Pimozide.
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.
LosartanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
LovastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
LurasidoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
MefloquineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MestranolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
MethimazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MethotrimeprazineCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
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.
MethylprednisoloneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MetoclopramideMay enhance the adverse/toxic effect of Antipsychotic Agents.
MetyrosineMetyrosine may enhance the adverse/toxic effect of Antipsychotic Agents.
MicafunginCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MidazolamCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MifepristoneMifepristone may enhance the QTc-prolonging effect of Pimozide. Mifepristone may increase the serum concentration of Pimozide.
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.
MirabegronCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MirtazapineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
MitoxantroneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
MoclobemideSerotonin 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.
ModafinilCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
NefazodoneMay increase the serum concentration of Pimozide.
NelfinavirProtease Inhibitors may increase the serum concentration of Pimozide.
NevirapineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
NifedipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
NilotinibCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
NisoldipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
NizatidineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
NorelgestrominCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
NorfloxacinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
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.
OlanzapineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
OmeprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
OrphenadrineCNS Depressants may enhance the CNS depressant effect of Orphenadrine.
OspemifeneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
OxybutyninCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
PazopanibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
Peginterferon alfa-2bMay decrease the serum concentration of CYP2D6 Substrates. Peginterferon Alfa-2b may increase the serum concentration of CYP2D6 Substrates.
PentamidineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
PilocarpineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
PosaconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the arrhythmogenic effect of Pimozide. Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Pimozide. This increase in serum concentrations may lead to QTc interval prolongation and ventricular arrhythmias. Applicable Isavuconazonium considerations are addressed in separate monographs.
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.
PravastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
PrimaquineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
ProgesteroneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
PropofolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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 (Strong) may increase the serum concentration of Pimozide.
QuinineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
QuinupristinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
RabeprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
RanolazineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
RisperidoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
RitonavirProtease Inhibitors may increase the serum concentration of Pimozide.
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.
SaquinavirProtease Inhibitors may increase the serum concentration of Pimozide.
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.
SildenafilCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of Pimozide.
SirolimusCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
Sodium phenylbutyrateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
SulconazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
SulfisoxazoleMacrolide Antibiotics may enhance the QTc-prolonging effect of Pimozide. Macrolide Antibiotics may decrease the metabolism of Pimozide. This mechanism may not apply to azithromycin.
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.
TamoxifenCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
TelaprevirMay increase the serum concentration of Pimozide.
TelithromycinMacrolide Antibiotics may enhance the QTc-prolonging effect of Pimozide. Macrolide Antibiotics may decrease the metabolism of Pimozide. This mechanism may not apply to azithromycin.
TemsirolimusCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
TeniposideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
TeriflunomideMay decrease the serum concentration of CYP1A2 Substrates.
TetrabenazineTetrabenazine may enhance the adverse/toxic effect of Antipsychotic Agents.
TetracyclineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide.
ThalidomideCNS Depressants may enhance the CNS depressant effect of Thalidomide.
ThioridazineCYP2D6 Inhibitors (Strong) may increase the serum concentration of Pimozide.
TiclopidineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
TiotropiumAnticholinergic Agents may enhance the anticholinergic effect of Tiotropium.
TipranavirProtease Inhibitors may increase the serum concentration of Pimozide.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TolvaptanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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.
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.
VinblastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
VincristineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
VinorelbineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
VoriconazoleAntifungal Agents (Azole Derivatives, Systemic) may enhance the arrhythmogenic effect of Pimozide. Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Pimozide. This increase in serum concentrations may lead to QTc interval prolongation and ventricular arrhythmias. Applicable Isavuconazonium considerations are addressed in separate monographs.
ZafirlukastCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
ZileutonZileuton may increase the serum concentration of Pimozide.
ZiprasidoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
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 Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
  • Take without regard to meals.

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. Pubmed
  3. Silva MR, Bernardi MM, Cruz-Casallas PE, Felicio LF: Pimozide injections into the Nucleus accumbens disrupt maternal behaviour in lactating rats. Pharmacol Toxicol. 2003 Jul;93(1):42-7. Pubmed
  4. Muscat R, Sampson D, Willner P: Dopaminergic mechanism of imipramine action in an animal model of depression. Biol Psychiatry. 1990 Aug 1;28(3):223-30. Pubmed
  5. Zarrindast MR, Heidari MR: On the mechanisms by which theophylline changes core body temperature in mice. Eur J Pharmacol. 1994 May 12;257(1-2):13-20. Pubmed
  6. Freedman SB, Patel S, Marwood R, Emms F, Seabrook GR, Knowles MR, McAllister G: Expression and pharmacological characterization of the human D3 dopamine receptor. J Pharmacol Exp Ther. 1994 Jan;268(1):417-26. Pubmed
  7. Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. Pubmed
  8. Murphy LL, Adrian BA, Kohli M: Inhibition of luteinizing hormone secretion by delta9-tetrahydrocannabinol in the ovariectomized rat: effect of pretreatment with neurotransmitter or neuropeptide receptor antagonists. Steroids. 1999 Sep;64(9):664-71. Pubmed

2. D(3) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

References:

  1. Freedman SB, Patel S, Marwood R, Emms F, Seabrook GR, Knowles MR, McAllister G: Expression and pharmacological characterization of the human D3 dopamine receptor. J Pharmacol Exp Ther. 1994 Jan;268(1):417-26. Pubmed

3. Potassium voltage-gated channel subfamily H member 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

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

References:

  1. Kang J, Wang L, Cai F, Rampe D: High affinity blockade of the HERG cardiac K(+) channel by the neuroleptic pimozide. Eur J Pharmacol. 2000 Mar 31;392(3):137-40. Pubmed
  2. Osypenko VM, Degtiar VIe, Naid’onov VG, Shuba IaM: [Blockade of HERG K+ channels expressed in Xenopus oocytes by antipsychotic agents] Fiziol Zh. 2001;47(1):17-25. Pubmed
  3. Shuba YM, Degtiar VE, Osipenko VN, Naidenov VG, Woosley RL: Testosterone-mediated modulation of HERG blockade by proarrhythmic agents. Biochem Pharmacol. 2001 Jul 1;62(1):41-9. Pubmed
  4. Kang J, Chen XL, Rampe D: The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel. Biochem Biophys Res Commun. 2001 Aug 24;286(3):499-504. Pubmed

4. Calmodulin

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Calmodulin P62158 Details

References:

  1. Papadopoulos V, Brown AS, Hall PF: Calcium-calmodulin-dependent phosphorylation of cytoskeletal proteins from adrenal cells. Mol Cell Endocrinol. 1990 Dec 3;74(2):109-23. Pubmed
  2. Wang XB, Sato N, Greer MA, Greer SE, McAdams S: Role of extracellular calcium and calmodulin in prolactin secretion induced by hyposmolarity, thyrotropin-releasing hormone, and high K+ in GH4C1 cells. Acta Endocrinol (Copenh). 1990 Aug;123(2):218-24. Pubmed
  3. Strobl JS, Kirkwood KL, Lantz TK, Lewine MA, Peterson VA, Worley JF 3rd: Inhibition of human breast cancer cell proliferation in tissue culture by the neuroleptic agents pimozide and thioridazine. Cancer Res. 1990 Sep 1;50(17):5399-405. Pubmed
  4. Cimino M, Weiss B: Characteristics of the binding of phenoxybenzamine to calmodulin. Biochem Pharmacol. 1988 Jul 15;37(14):2739-45. Pubmed
  5. Mody I, Baimbridge KG, Miller JJ: Blockade of tetanic- and calcium-induced long-term potentiation in the hippocampal slice preparation by neuroleptics. Neuropharmacology. 1984 Jun;23(6):625-31. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

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

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

5. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

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

6. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 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

7. 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

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. Pubmed
  2. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. Pubmed

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