Identification

Name
Pimozide
Accession Number
DB01100  (APRD00218)
Type
Small Molecule
Groups
Approved
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
  • Pimozida
  • Pimozide
  • Pimozidum
External IDs
MCN-JR-6238 / R 623 / R-623 / R-6238
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OrapTablet1 mg/1OralTeva Select Brands2000-06-07Not applicableUs57844 0151 01 nlmimage10 9a354d2a
OrapTablet2 mg/1OralTeva Select Brands2014-10-31Not applicableUs
OrapTablet4 mgOralAa Pharma Inc1975-12-31Not applicableCanada
OrapTablet2 mg/1OralTeva Select Brands1990-09-302017-10-31Us57844 0187 01 nlmimage10 a73553ba
OrapTablet2 mgOralAa Pharma Inc1975-12-31Not applicableCanada
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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PimozideTablet2 mg/1OralPar Pharmaceutical2014-12-01Not applicableUs
PimozideTablet1 mg/1OralPar Pharmaceutical2014-12-01Not applicableUs
PimozideTablet2 mg/1OralAvera Mc Kennan Hospital2016-01-07Not applicableUs
PMS-pimozideTablet10 mgOralPharmascience IncNot applicableNot applicableCanada
PMS-pimozideTablet2 mgOralPharmascience Inc2002-10-18Not applicableCanada
PMS-pimozideTablet4 mgOralPharmascience Inc2002-10-18Not applicableCanada
International/Other Brands
Neoperidole / Opiran
Categories
UNII
1HIZ4DL86F
CAS number
2062-78-4
Weight
Average: 461.5462
Monoisotopic: 461.227868975
Chemical Formula
C28H29F2N3O
InChI Key
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

Pharmacology

Indication

Used for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment.

Structured Indications
Pharmacodynamics

Pimozide 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 action

The 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.

TargetActionsOrganism
AD(2) dopamine receptor
antagonist
Human
AD(3) dopamine receptor
antagonist
Human
APotassium voltage-gated channel subfamily H member 2
inhibitor
Human
UCalmodulin
inhibitor
Human
Absorption

Greater than 50% absorption after oral administration. Serum peak appears 6-8 hours post ingestion.

Volume of distribution
Not Available
Protein binding
Not 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 elimination
Not Available
Half life

29 ± 10 hours (single-dose study of healthy volunteers).

Clearance
Not Available
Toxicity

LD50 = 1100 mg/kg (rat, oral), 228 mg/kg (mouse, oral)

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details

Interactions

Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetaminePimozide may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.Experimental, Illicit
2,5-Dimethoxy-4-ethylthioamphetaminePimozide may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.Experimental
3,4-MethylenedioxyamphetaminePimozide may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetaminePimozide may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.Experimental, Illicit
7-NitroindazoleThe risk or severity of adverse effects can be increased when Pimozide is combined with 7-Nitroindazole.Experimental
AbirateroneThe serum concentration of Pimozide can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Pimozide is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Pimozide is combined with Aceprometazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Pimozide is combined with Adipiplon.Investigational
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Pimozide.Approved
AgomelatineThe risk or severity of adverse effects can be increased when Pimozide is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Pimozide is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Pimozide is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Pimozide.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Pimozide is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Pimozide is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Pimozide is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Pimozide.Approved, Illicit, Investigational
AmiodaroneThe serum concentration of Pimozide can be increased when it is combined with Amiodarone.Approved, Investigational
AmisulpridePimozide may increase the antipsychotic activities of Amisulpride.Approved, Investigational
AmobarbitalThe risk or severity of adverse effects can be increased when Pimozide is combined with Amobarbital.Approved, Illicit
AmperozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Amperozide.Experimental
AmphetaminePimozide may decrease the stimulatory activities of Amphetamine.Approved, Illicit
AprepitantThe serum concentration of Pimozide can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Pimozide is combined with Aripiprazole.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Pimozide is combined with Asenapine.Approved
AtazanavirThe serum concentration of Pimozide can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Pimozide can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Pimozide is combined with Atorvastatin.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Azaperone.Investigational, Vet Approved
AzelastinePimozide may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzithromycinThe risk or severity of ventricular arrhythmias can be increased when Azithromycin is combined with Pimozide.Approved
BarbitalThe risk or severity of adverse effects can be increased when Pimozide is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Pimozide is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Pimozide.Approved
BenzphetaminePimozide may decrease the stimulatory activities of Benzphetamine.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Pimozide is combined with Benzyl alcohol.Approved
BoceprevirThe serum concentration of Pimozide can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe serum concentration of Pimozide can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Pimozide can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Pimozide.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Pimozide.Approved
BrigatinibThe serum concentration of Pimozide can be decreased when it is combined with Brigatinib.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
BromazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Bromazepam.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Pimozide is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Pimozide is combined with Bromperidol.Investigational
BrotizolamThe risk or severity of adverse effects can be increased when Pimozide is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Pimozide.Approved, Investigational
BuprenorphinePimozide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Pimozide can be increased when it is combined with Bupropion.Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Pimozide.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Pimozide.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Butacaine.Vet Approved
ButambenThe risk or severity of adverse effects can be increased when Pimozide is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Pimozide is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Pimozide.Approved, Illicit, Vet Approved
CaffeineThe metabolism of Pimozide can be decreased when combined with Caffeine.Approved
CanertinibThe risk or severity of adverse effects can be increased when Pimozide is combined with Canertinib.Investigational
CarbamazepineThe metabolism of Pimozide can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Pimozide is combined with Carfentanil.Illicit, Investigational, Vet Approved
CeritinibThe serum concentration of Pimozide can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Pimozide.Withdrawn
Chloral hydrateThe risk or severity of adverse effects can be increased when Pimozide is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Pimozide.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Chlormezanone.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Chloroprocaine.Approved
ChlorphenterminePimozide may decrease the stimulatory activities of Chlorphentermine.Illicit, Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Pimozide.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Pimozide is combined with Chlorprothixene.Approved, Investigational, Withdrawn
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Pimozide.Approved
CinacalcetThe serum concentration of Pimozide can be increased when it is combined with Cinacalcet.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Pimozide.Approved, Vet Approved
CitalopramThe risk or severity of QTc prolongation can be increased when Citalopram is combined with Pimozide.Approved
CitalopramThe metabolism of Pimozide can be decreased when combined with Citalopram.Approved
ClarithromycinThe risk or severity of ventricular arrhythmias can be increased when Clarithromycin is combined with Pimozide.Approved
ClemastineThe serum concentration of Pimozide can be increased when it is combined with Clemastine.Approved
clomethiazoleThe risk or severity of adverse effects can be increased when Pimozide is combined with clomethiazole.Investigational
ClopenthixolThe risk or severity of adverse effects can be increased when Pimozide is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Pimozide.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Pimozide is combined with Clothiapine.Experimental
ClotrimazoleThe serum concentration of Pimozide can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Pimozide.Approved
CobicistatThe serum concentration of Pimozide can be increased when it is combined with Cobicistat.Approved
CocaineThe serum concentration of Pimozide can be increased when it is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Pimozide.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Pimozide.Approved
ConivaptanThe serum concentration of Pimozide can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibCrizotinib may increase the QTc-prolonging activities of Pimozide.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Pimozide.Approved
CyclosporineThe serum concentration of Pimozide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Pimozide can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Pimozide.Approved
DabrafenibThe serum concentration of Pimozide can be decreased when it is combined with Dabrafenib.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Pimozide.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dapoxetine.Investigational
DarunavirThe serum concentration of Pimozide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Pimozide can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Pimozide can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Pimozide can be increased when it is combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Pimozide is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Pimozide is combined with Desflurane.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Pimozide is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Detomidine.Vet Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Pimozide.Approved, Vet Approved
DextroamphetaminePimozide may decrease the stimulatory activities of Dextroamphetamine.Approved, Illicit
DextromoramideThe risk or severity of adverse effects can be increased when Pimozide is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Pimozide.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dezocine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Pimozide.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Pimozide is combined with Diethyl ether.Experimental
DiethylpropionPimozide may decrease the stimulatory activities of Diethylpropion.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dihydrocodeine.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Pimozide.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Pimozide.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Pimozide.Experimental
DihydroergotamineThe serum concentration of Pimozide can be increased when it is combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe serum concentration of Pimozide can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Pimozide.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Pimozide.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Pimozide is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Pimozide is combined with Doramectin.Vet Approved
DosulepinThe serum concentration of Pimozide can be increased when it is combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Pimozide.Approved, Investigational
DoxycyclineThe serum concentration of Pimozide can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Pimozide is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Illicit
DronedaroneThe serum concentration of Pimozide can be increased when it is combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Pimozide is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Pimozide is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Pimozide.Approved
EcgonineThe risk or severity of adverse effects can be increased when Pimozide is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Pimozide is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Pimozide.Approved
EltanoloneThe risk or severity of adverse effects can be increased when Pimozide is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Pimozide.Approved, Investigational, Vet Approved
EnzalutamideThe serum concentration of Pimozide can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe serum concentration of Pimozide can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Pimozide is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Pimozide is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Pimozide.Approved
EthanolPimozide may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Pimozide.Approved, Illicit, Withdrawn
Ethyl carbamateThe risk or severity of adverse effects can be increased when Pimozide is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Pimozide is combined with Ethyl chloride.Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Pimozide is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Pimozide is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Pimozide is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Pimozide is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Pimozide.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Pimozide is combined with Etorphine.Illicit, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Pimozide.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Pimozide is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Pimozide.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Pimozide.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Fluanisone.Experimental
FluconazoleThe serum concentration of Pimozide can be increased when it is combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Fludiazepam.Approved, Illicit
FlunitrazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Flunitrazepam.Approved, Illicit
FluoxetineFluoxetine may increase the QTc-prolonging activities of Pimozide.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Pimozide.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Pimozide.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Pimozide.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Pimozide is combined with Fluspirilene.Approved, Investigational
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Pimozide.Approved
FluvoxamineThe serum concentration of Pimozide can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Pimozide can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Pimozide can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Pimozide can be increased when combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Pimozide is combined with Fospropofol.Approved, Illicit, Investigational
Fusidic AcidThe serum concentration of Pimozide can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Pimozide.Approved, Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Pimozide is combined with Gamma Hydroxybutyric Acid.Approved, Illicit, Investigational
GepefrinePimozide may decrease the stimulatory activities of Gepefrine.Experimental
GepironeThe risk or severity of adverse effects can be increased when Pimozide is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Pimozide is combined with Glutethimide.Approved, Illicit
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Pimozide.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Pimozide.Approved
HalothaneThe risk or severity of adverse effects can be increased when Pimozide is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Pimozide is combined with Heroin.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Pimozide is combined with Hexobarbital.Approved
HydrocodonePimozide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Pimozide.Approved, Illicit
HydroxyamphetaminePimozide may decrease the stimulatory activities of Hydroxyamphetamine.Approved
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Pimozide.Approved
IdelalisibThe serum concentration of Pimozide can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Pimozide can be increased when it is combined with Imatinib.Approved
IndalpineThe risk or severity of adverse effects can be increased when Pimozide is combined with Indalpine.Investigational, Withdrawn
IndinavirThe serum concentration of Pimozide can be increased when it is combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Pimozide is combined with Indiplon.Investigational
Iofetamine I-123Pimozide may decrease the stimulatory activities of Iofetamine I-123.Approved
IsavuconazoniumThe serum concentration of Pimozide can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Pimozide.Approved, Vet Approved
IsradipineThe serum concentration of Pimozide can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Pimozide can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Pimozide can be increased when it is combined with Ivacaftor.Approved
KetamineThe risk or severity of adverse effects can be increased when Pimozide is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Pimozide is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe serum concentration of Pimozide can be increased when it is combined with Ketoconazole.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Pimozide.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Pimozide.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Pimozide is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Pimozide is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Pimozide.Approved
LidocaineThe metabolism of Pimozide can be decreased when combined with Lidocaine.Approved, Vet Approved
LisdexamfetaminePimozide may decrease the stimulatory activities of Lisdexamfetamine.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Pimozide.Approved, Investigational
LithiumLithium may increase the neurotoxic activities of Pimozide.Approved
LobeglitazoneThe metabolism of Pimozide can be decreased when combined with Lobeglitazone.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Pimozide is combined with Lofentanil.Illicit
LopinavirThe serum concentration of Pimozide can be increased when it is combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Pimozide is combined with Loprazolam.Experimental
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Pimozide.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Lormetazepam.Approved
LorpiprazoleThe serum concentration of Pimozide can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Pimozide can be increased when it is combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Pimozide.Approved
LuliconazoleThe serum concentration of Pimozide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Pimozide can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Pimozide.Illicit, Investigational, Withdrawn
MacimorelinPimozide may increase the QTc-prolonging activities of Macimorelin.Approved, Investigational
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Vet Approved
MebicarThe risk or severity of adverse effects can be increased when Pimozide is combined with Mebicar.Experimental
MedazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Pimozide.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Melperone.Approved, Investigational
MephedronePimozide may decrease the stimulatory activities of Mephedrone.Investigational
MephenterminePimozide may decrease the stimulatory activities of Mephentermine.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Pimozide.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Pimozide.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Pimozide is combined with Meptazinol.Experimental
MequitazinePimozide may increase the arrhythmogenic activities of Mequitazine.Approved
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Pimozide.Approved, Investigational
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Pimozide.Experimental
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Pimozide.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Pimozide is combined with Methadyl Acetate.Approved, Illicit
MethamphetaminePimozide may decrease the stimulatory activities of Methamphetamine.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Pimozide is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Methaqualone.Illicit, Withdrawn
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Pimozide.Approved
MethotrimeprazinePimozide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Pimozide.Approved, Investigational, Vet Approved
MethoxyphenaminePimozide may decrease the stimulatory activities of Methoxyphenamine.Experimental
MethylecgonineThe risk or severity of adverse effects can be increased when Pimozide is combined with Methylecgonine.Experimental
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Pimozide.Approved
MethylphenidateThe risk or severity of adverse effects can be increased when Pimozide is combined with Methylphenidate.Approved, Investigational
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Pimozide.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Pimozide.Approved
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Pimozide.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Pimozide.Approved, Investigational
MetyrosinePimozide may increase the sedative activities of Metyrosine.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Pimozide.Experimental
MexiletineThe metabolism of Pimozide can be decreased when combined with Mexiletine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Pimozide.Approved, Illicit
MidomafetaminePimozide may decrease the stimulatory activities of Midomafetamine.Experimental, Illicit, Investigational
MidostaurinThe serum concentration of Pimozide can be increased when it is combined with Midostaurin.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Pimozide.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Pimozide is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Investigational
MirtazapinePimozide may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Pimozide can be decreased when it is combined with Mitotane.Approved
MMDAPimozide may decrease the stimulatory activities of MMDA.Experimental, Illicit
MolindoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Pimozide.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Pimozide.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Pimozide.Approved
NefazodoneThe serum concentration of Pimozide can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Pimozide can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Pimozide can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Pimozide can be increased when it is combined with Nevirapine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Pimozide.Approved, Investigational
NilotinibThe serum concentration of Pimozide can be increased when it is combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Pimozide.Approved
NitrazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Pimozide is combined with Nitrous oxide.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Pimozide is combined with Norflurane.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Pimozide.Approved, Investigational
OlaparibThe serum concentration of Pimozide can be increased when it is combined with Olaparib.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Pimozide.Approved
OpiumThe risk or severity of adverse effects can be increased when Pimozide is combined with Opium.Approved, Illicit
OrphenadrinePimozide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Pimozide is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Pimozide can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Pimozide.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Oxethazaine.Approved, Investigational
OxprenololThe risk or severity of adverse effects can be increased when Pimozide is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Pimozide.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Pimozide.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Oxymorphone.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Pimozide can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Paliperidone.Approved
ParaldehydePimozide may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParoxetineThe serum concentration of Pimozide can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Pimozide.Approved
Peginterferon alfa-2bThe serum concentration of Pimozide can be increased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Pimozide is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Pimozide.Approved, Vet Approved
PentobarbitalThe metabolism of Pimozide can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
PerazineThe risk or severity of adverse effects can be increased when Pimozide is combined with Perazine.Investigational
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Pimozide.Approved, Investigational, Vet Approved, Withdrawn
PerospironeThe risk or severity of adverse effects can be increased when Pimozide is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Pimozide.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Pimozide.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Pimozide is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Pimozide is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Pimozide can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Pimozide is combined with Phenoxyethanol.Approved
PhenterminePimozide may decrease the stimulatory activities of Phentermine.Approved, Illicit
PhenytoinThe metabolism of Pimozide can be increased when combined with Phenytoin.Approved, Vet Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pimozide is combined with Pipamperone.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Pimozide is combined with Piritramide.Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Pimozide.Approved
PosaconazoleThe serum concentration of Pimozide can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexolePimozide may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Pramocaine.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Pimozide.Approved
PrazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Prazepam.Approved, Illicit
PregabalinThe therapeutic efficacy of Pimozide can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Pimozide.Approved
PrimidoneThe metabolism of Pimozide can be increased when combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Pimozide.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Pimozide.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Pimozide.Approved, Vet Approved
PropanididThe risk or severity of adverse effects can be increased when Pimozide is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Pimozide.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Pimozide.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Propoxycaine.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Pimozide is combined with Proxibarbal.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Pimozide.Approved
PSD502The risk or severity of adverse effects can be increased when Pimozide is combined with PSD502.Investigational
PseudoephedrinePimozide may decrease the stimulatory activities of Pseudoephedrine.Approved
QuazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Pimozide is combined with Quetiapine.Approved
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Pimozide.Approved
QuinidineThe serum concentration of Pimozide can be increased when it is combined with Quinidine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Pimozide is combined with Raclopride.Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Pimozide.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Pimozide.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Pimozide.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Pimozide.Approved, Investigational
RibociclibThe serum concentration of Pimozide can be increased when it is combined with Ribociclib.Approved
RifabutinThe metabolism of Pimozide can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Pimozide can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Pimozide can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Pimozide.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Pimozide.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Pimozide.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Pimozide is combined with Ritanserin.Investigational
RitobegronPimozide may decrease the stimulatory activities of Ritobegron.Investigational
RitonavirThe serum concentration of Pimozide can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Pimozide can be increased when it is combined with Rolapitant.Approved
RomifidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Romifidine.Vet Approved
RopinirolePimozide may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Pimozide.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Pimozide.Approved
RotigotinePimozide may increase the sedative activities of Rotigotine.Approved
RucaparibThe serum concentration of Pimozide can be increased when it is combined with Rucaparib.Approved, Investigational
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pimozide.Approved
SaquinavirThe serum concentration of Pimozide can be increased when it is combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Pimozide can be decreased when used in combination with Sarilumab.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Pimozide.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Pimozide is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Pimozide is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Pimozide is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Pimozide is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe serum concentration of Pimozide can be increased when it is combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Pimozide.Approved
SiltuximabThe serum concentration of Pimozide can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Pimozide can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Pimozide.Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
St. John's WortThe serum concentration of Pimozide can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Pimozide can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Pimozide.Approved, Investigational
SulfisoxazoleThe serum concentration of Pimozide can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulpiridePimozide may increase the antipsychotic activities of Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Pimozide is combined with Sultopride.Experimental
SuvorexantPimozide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Pimozide is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pimozide.Approved
TelaprevirThe serum concentration of Pimozide can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Pimozide can be increased when it is combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Pimozide.Approved
Tenofovir disoproxilThe metabolism of Pimozide can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe serum concentration of Pimozide can be increased when it is combined with Terbinafine.Approved, Investigational, Vet Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Pimozide.Experimental
TeriflunomideThe serum concentration of Pimozide can be decreased when it is combined with Teriflunomide.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Pimozide.Approved
TetracaineThe risk or severity of adverse effects can be increased when Pimozide is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Pimozide is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Pimozide is combined with Tetrodotoxin.Investigational
ThalidomidePimozide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Pimozide can be decreased when combined with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Pimozide is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Pimozide.Approved, Vet Approved
ThioridazineThe serum concentration of Pimozide can be increased when it is combined with Thioridazine.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Pimozide is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Pimozide is combined with Tiapride.Approved, Investigational
TiclopidineThe serum concentration of Pimozide can be increased when it is combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Pimozide is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Tilidine.Experimental
TipranavirThe serum concentration of Pimozide can be increased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Pimozide can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Pimozide.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Pimozide.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Pimozide.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Pimozide is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Pimozide.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Pimozide.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Pimozide.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Pimozide is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Pimozide is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Pimozide.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Pimozide is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Pimozide.Approved, Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Pimozide.Approved, Investigational, Nutraceutical
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Pimozide.Approved, Investigational
VemurafenibThe serum concentration of Pimozide can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Pimozide can be increased when it is combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Pimozide is combined with Veralipride.Experimental
VerapamilThe serum concentration of Pimozide can be increased when it is combined with Verapamil.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Pimozide.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Pimozide.Approved, Investigational
Vinyl etherThe risk or severity of adverse effects can be increased when Pimozide is combined with Vinyl ether.Experimental
VoriconazoleThe serum concentration of Pimozide can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Pimozide is combined with Vortioxetine.Approved
XenonThe risk or severity of adverse effects can be increased when Pimozide is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Pimozide is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Pimozide.Approved, Illicit, Investigational
ZileutonThe serum concentration of Pimozide can be increased when it is combined with Zileuton.Approved, Investigational, Withdrawn
ZimelidineThe risk or severity of adverse effects can be increased when Pimozide is combined with Zimelidine.Withdrawn
ZiprasidoneThe serum concentration of Pimozide can be increased when it is combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Pimozide is combined with Zolazepam.Vet Approved
ZolpidemPimozide may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZopicloneThe risk or severity of adverse effects can be increased when Pimozide is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Pimozide is combined with Zotepine.Approved, Investigational
ZucapsaicinThe metabolism of Pimozide can be decreased when combined with Zucapsaicin.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Pimozide is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
  • Take without regard to meals.

References

General References
Not Available
External Links
Human Metabolome Database
HMDB0015232
KEGG Drug
D00560
KEGG Compound
C07566
PubChem Compound
16362
PubChem Substance
46507096
ChemSpider
15520
BindingDB
50334150
ChEBI
8212
ChEMBL
CHEMBL1423
Therapeutic Targets Database
DAP000316
PharmGKB
PA450965
IUPHAR
90
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pimozide
ATC Codes
N05AG02 — Pimozide
AHFS Codes
  • 28:16.08.92 — Miscellaneous Antipsychotics
MSDS
Download (29 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentGilles de la Tourette's Syndrome1
2CompletedTreatmentSchizophrenic Disorders1
2RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3Unknown StatusTreatmentPsychosis Nos/Other1
4Active Not RecruitingTreatmentSchizoaffective Disorders / Schizophrenia and Disorders With Psychotic Features / Schizophrenic Disorders1
4CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableRecruitingNot AvailableSchizophrenic Disorders1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral10 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.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)214-218 °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 FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-001i-4890100000-ff909df45204eac82c46
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03fr-3945500000-63d831a19fe77286e9e1

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Phenylbutylamines / Benzimidazoles / Fluorobenzenes / Aralkylamines / Piperidines / N-substituted imidazoles / Aryl fluorides / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds
show 4 more
Substituents
Diphenylmethane / Phenylbutylamine / Benzimidazole / Aralkylamine / Fluorobenzene / Halobenzene / Aryl fluoride / Aryl halide / Piperidine / N-substituted imidazole
show 17 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, benzimidazoles, heteroarylpiperidine (CHEBI:8212)

Targets

Details
1. D(2) dopamine receptor
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
Uniprot Name
D(2) dopamine receptor
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
Uniprot Name
D(3) dopamine receptor
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 ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
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...
Gene Name
CALM1
Uniprot ID
P0DP23
Uniprot Name
Calmodulin
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

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on January 19, 2018 10:54