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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
Halomonth
Neoperidole
Opiran
Orap
Pimozida
Pimozide
Pimozidum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Oraptablet1 mg/1oralTeva Select Brands2000-06-07Not applicableUs
Oraptablet4 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Oraptablet2 mgoralAa Pharma Inc1975-12-31Not applicableCanada
Oraptablet2 mg/1oralTeva Select Brands2014-10-31Not applicableUs
Oraptablet2 mg/1oralTeva Select Brands1990-09-30Not applicableUs
Orap Tab 10mgtablet10 mgoralMcneil Pharmaceutical, Division Of Ortho Mcneil Inc.1983-12-311996-08-19Canada
Pimozidetablet4 mgoralAa Pharma Inc2003-04-01Not applicableCanada
Pimozidetablet2 mgoralAa Pharma Inc2003-04-01Not applicableCanada
PMS-pimozidetablet4 mgoralPharmascience Inc2002-10-18Not applicableCanada
PMS-pimozidetablet2 mgoralPharmascience Inc2002-10-18Not applicableCanada
PMS-pimozidetablet10 mgoralPharmascience IncNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pimozidetablet1 mg/1oralPar Pharmaceutical Inc.2014-12-01Not applicableUs
Pimozidetablet2 mg/1oralPar Pharmaceutical Inc.2014-12-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NeoperidoleNot Available
OpiranNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII1HIZ4DL86F
CAS number2062-78-4
WeightAverage: 461.5462
Monoisotopic: 461.227868975
Chemical FormulaC28H29F2N3O
InChI KeyInChIKey=YVUQSNJEYSNKRX-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.
Related Articles
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 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.686
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
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg/1
Tabletoral2 mg
Tabletoral2 mg/1
Tabletoral4 mg
Tabletoral10 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
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-001i-4890100000-ff909df45204eac82c46View in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05AG02
AHFS Codes
  • 28:16.08.92
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (29 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Pimozide can be increased when it is combined with Abiraterone.
AclidiniumAclidinium may increase the anticholinergic activities of Pimozide.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Pimozide.
AlprazolamThe serum concentration of Pimozide can be increased when it is combined with Alprazolam.
AmiodaroneThe serum concentration of Pimozide can be increased when it is combined with Amiodarone.
AmisulprideThe risk or severity of adverse effects can be increased when Pimozide is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Pimozide.
AmlodipineThe serum concentration of Pimozide can be increased when it is combined with Amlodipine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Pimozide.
AmphetaminePimozide may decrease the stimulatory activities of Amphetamine.
AprepitantThe serum concentration of Pimozide can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Pimozide can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Pimozide can be increased when it is combined with Atorvastatin.
AzelastinePimozide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Pimozide.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Pimozide.
BatimastatThe serum concentration of Pimozide can be increased when it is combined with Batimastat.
BenzphetaminePimozide may decrease the stimulatory activities of Benzphetamine.
BexaroteneThe serum concentration of Pimozide can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Pimozide can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Pimozide can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Pimozide can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Pimozide can be decreased when it is combined with Bosentan.
Botulinum Toxin Type APimozide may increase the anticholinergic activities of Botulinum Toxin Type A.
Botulinum Toxin Type BPimozide may increase the anticholinergic activities of Botulinum Toxin Type B.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
BromocriptineThe therapeutic efficacy of Pimozide can be decreased when used in combination with Bromocriptine.
BuprenorphinePimozide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BupropionThe serum concentration of Pimozide can be increased when it is combined with Bupropion.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Pimozide.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pimozide.
CarbamazepineThe metabolism of Pimozide can be increased when combined with Carbamazepine.
CathinonePimozide may decrease the stimulatory activities of Cathinone.
CeritinibThe serum concentration of Pimozide can be increased when it is combined with Ceritinib.
CilostazolThe serum concentration of Pimozide can be increased when it is combined with Cilostazol.
CimetidineThe serum concentration of Pimozide can be increased when it is combined with Cimetidine.
Cimetropium BromidePimozide may increase the anticholinergic activities of Cimetropium Bromide.
CinacalcetThe serum concentration of Pimozide can be increased when it is combined with Cinacalcet.
CiprofloxacinThe serum concentration of Pimozide can be increased when it is combined with Ciprofloxacin.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Pimozide.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Pimozide.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Pimozide.
ClotrimazoleThe serum concentration of Pimozide can be increased when it is combined with Clotrimazole.
CobicistatThe serum concentration of Pimozide can be increased when it is combined with Cobicistat.
CocaineThe serum concentration of Pimozide can be increased when it is combined with Cocaine.
ConivaptanThe serum concentration of Pimozide can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Pimozide.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Pimozide.
CyclosporineThe serum concentration of Pimozide can be increased when it is combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Pimozide can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Pimozide can be decreased when it is combined with Dabrafenib.
DanazolThe serum concentration of Pimozide can be increased when it is combined with Danazol.
DarunavirThe serum concentration of Pimozide can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Pimozide can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Pimozide can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Pimozide can be increased when it is combined with Delavirdine.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Pimozide.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Pimozide.
DextroamphetaminePimozide may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Pimozide.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Pimozide.
DiltiazemThe serum concentration of Pimozide can be increased when it is combined with Diltiazem.
DofetilideDofetilide may increase the QTc-prolonging activities of Pimozide.
DonepezilDonepezil may increase the central neurotoxic activities of Pimozide.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Pimozide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
DronedaroneThe serum concentration of Pimozide can be increased when it is combined with Dronedarone.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Pimozide.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Pimozide.
EluxadolinePimozide may increase the activities of Eluxadoline.
EnzalutamideThe serum concentration of Pimozide can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Pimozide.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Pimozide.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Pimozide.
ErythromycinErythromycin may increase the QTc-prolonging activities of Pimozide.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Pimozide.
EthanolPimozide may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Pimozide.
FluconazoleFluconazole may increase the arrhythmogenic activities of Pimozide.
FluoxetineFluoxetine may increase the QTc-prolonging activities of Pimozide.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Pimozide.
FosamprenavirThe serum concentration of Pimozide can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Pimozide can be increased when it is combined with Fosaprepitant.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Pimozide.
Fusidic AcidThe serum concentration of Pimozide can be increased when it is combined with Fusidic Acid.
GalantamineGalantamine may increase the central neurotoxic activities of Pimozide.
Glucagon recombinantThe risk or severity of adverse effects can be increased when Pimozide is combined with Glucagon recombinant.
Glycerol PhenylbutyrateThe serum concentration of Pimozide can be increased when it is combined with Glycerol Phenylbutyrate.
GoserelinGoserelin may increase the QTc-prolonging activities of Pimozide.
HydrocodonePimozide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
IdelalisibThe serum concentration of Pimozide can be increased when it is combined with Idelalisib.
IloperidoneThe serum concentration of Pimozide can be increased when it is combined with Iloperidone.
ImatinibThe serum concentration of Pimozide can be increased when it is combined with Imatinib.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Pimozide.
IndinavirThe serum concentration of Pimozide can be increased when it is combined with Indinavir.
Ipratropium bromideIpratropium bromide may increase the anticholinergic activities of Pimozide.
IsavuconazoniumThe serum concentration of Pimozide can be increased when it is combined with Isavuconazonium.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Pimozide.
IsoflurophateThe serum concentration of Pimozide can be increased when it is combined with Isoflurophate.
IsoniazidThe serum concentration of Pimozide can be increased when it is combined with Isoniazid.
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Pimozide.
ItraconazoleItraconazole may increase the arrhythmogenic activities of Pimozide.
IvabradineIvabradine may increase the QTc-prolonging activities of Pimozide.
IvacaftorThe serum concentration of Pimozide can be increased when it is combined with Ivacaftor.
KetoconazoleKetoconazole may increase the arrhythmogenic activities of Pimozide.
LapatinibThe serum concentration of Pimozide can be increased when it is combined with Lapatinib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Pimozide.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Pimozide.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Pimozide.
LisdexamfetaminePimozide may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Pimozide.
LomitapideThe serum concentration of Pimozide can be increased when it is combined with Lomitapide.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Pimozide.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Pimozide.
LuliconazoleThe serum concentration of Pimozide can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Pimozide can be increased when it is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Pimozide.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Pimozide.
MethamphetaminePimozide may decrease the stimulatory activities of Methamphetamine.
MethotrimeprazineThe serum concentration of Pimozide can be increased when it is combined with Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Pimozide is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Pimozide.
MetyrosinePimozide may increase the sedative activities of Metyrosine.
MexiletineThe metabolism of Pimozide can be decreased when combined with Mexiletine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Pimozide.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Pimozide.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
MitotaneThe serum concentration of Pimozide can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Pimozide.
MorphineThe risk or severity of adverse effects can be increased when Pimozide is combined with Morphine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Pimozide.
NefazodoneThe serum concentration of Pimozide can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Pimozide can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Pimozide can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Pimozide can be increased when it is combined with Nilotinib.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Pimozide.
OctreotideOctreotide may increase the QTc-prolonging activities of Pimozide.
OrphenadrinePimozide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Pimozide can be increased when it is combined with Palbociclib.
ParaldehydePimozide may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Pimozide.
PazopanibThe serum concentration of Pimozide can be increased when it is combined with Pazopanib.
Peginterferon alfa-2bThe serum concentration of Pimozide can be decreased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Pimozide.
PhendimetrazinePimozide may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Pimozide.
PhenterminePimozide may decrease the stimulatory activities of Phentermine.
PhenytoinThe metabolism of Pimozide can be increased when combined with Phenytoin.
PosaconazolePosaconazole may increase the arrhythmogenic activities of Pimozide.
Potassium ChloridePimozide may increase the ulcerogenic activities of Potassium Chloride.
PramlintidePramlintide may increase the anticholinergic activities of Pimozide.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Pimozide.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Pimozide.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Pimozide.
PropofolThe serum concentration of Pimozide can be increased when it is combined with Propofol.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Pimozide.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Pimozide.
QuinidineThe serum concentration of Pimozide can be increased when it is combined with Quinidine.
RamosetronPimozide may increase the activities of Ramosetron.
RanolazineThe serum concentration of Pimozide can be increased when it is combined with Ranolazine.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Pimozide.
RitonavirThe serum concentration of Pimozide can be increased when it is combined with Ritonavir.
RivastigmineRivastigmine may increase the central neurotoxic activities of Pimozide.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Pimozide.
RolapitantThe serum concentration of Pimozide can be increased when it is combined with Rolapitant.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pimozide.
SaquinavirThe serum concentration of Pimozide can be increased when it is combined with Saquinavir.
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Pimozide.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Pimozide.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Pimozide.
SiltuximabThe serum concentration of Pimozide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Pimozide can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
St. John's WortThe serum concentration of Pimozide can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Pimozide can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Pimozide is combined with Sulpiride.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Pimozide.
SuvorexantPimozide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineThe therapeutic efficacy of Pimozide can be decreased when used in combination with Tacrine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Pimozide.
TelaprevirThe serum concentration of Pimozide can be increased when it is combined with Telaprevir.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Pimozide.
TerbinafineThe serum concentration of Pimozide can be increased when it is combined with Terbinafine.
TeriflunomideThe serum concentration of Pimozide can be decreased when it is combined with Teriflunomide.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Pimozide.
ThalidomidePimozide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe serum concentration of Pimozide can be increased when it is combined with Thioridazine.
TicagrelorThe serum concentration of Pimozide can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Pimozide can be increased when it is combined with Ticlopidine.
TiotropiumPimozide may increase the anticholinergic activities of Tiotropium.
TipranavirThe serum concentration of Pimozide can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Pimozide can be decreased when it is combined with Tocilizumab.
TopiramateThe risk or severity of adverse effects can be increased when Pimozide is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Pimozide.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Pimozide.
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Pimozide.
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Pimozide.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Pimozide.
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Pimozide.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Pimozide.
VerapamilThe serum concentration of Pimozide can be increased when it is combined with Verapamil.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Pimozide.
VoriconazoleVoriconazole may increase the arrhythmogenic activities of Pimozide.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Pimozide.
ZileutonThe serum concentration of Pimozide can be increased when it is combined with Zileuton.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Pimozide.
ZolpidemPimozide may increase the central nervous system depressant (CNS depressant) activities 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

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706 ]
  3. 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:12828573 ]
  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:2378927 ]
  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:8082693 ]
  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:8301582 ]
  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:7855217 ]
  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:10503726 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. 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:8301582 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
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:10762666 ]
  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:11296551 ]
  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:11377395 ]
  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:11511086 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Titin binding
Specific Function:
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
References
  1. 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:1965307 ]
  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:2120879 ]
  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:2386945 ]
  4. Cimino M, Weiss B: Characteristics of the binding of phenoxybenzamine to calmodulin. Biochem Pharmacol. 1988 Jul 15;37(14):2739-45. [PubMed:3134891 ]
  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:6146939 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. 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:12699389 ]
  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:11082465 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13