Drug/Small Molecule:
haloperidol

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for haloperidol and CYP2D6

Summary

Reduce haloperidol dose by 50% or select an alternative drug for CYP2D6 poor metabolizer (PM) genotype patients.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for haloperidol based on CYP2D6 genotype (PMID:21412232). They recommend dose reduction for poor metabolizer patients.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
PM (2 inactive alleles) Reduce dose by 50% or select alternative drug (e.g., pimozide, flupenthixol, fluphenazine, quetiapine, olanzapine, clozapine). Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Clinical effect (S): long-standing discomfort (48-168 hr) without permanent injury e.g. failure of therapy with tricyclic antidepressants, atypical antipsychotic drugs; extrapyramidal side effects; parkinsonism; ADE resulting from increased bioavailability of tricyclic antidepressants, metoprolol, propafenone (central effects e.g. dizziness); INR 4.5-6.0; neutropenia 1.0-1.5x10^9/l; leucopenia 2.0-3.0x10^9/l; thrombocytopenia 50-75x10^9/l.
IM (2 decreased activity alleles, or 1 active and 1 inactive allele, or 1 decreased activity and 1 inactive allele) None. Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Minor clinical effect (S): QTc prolongation (<450 ms women, <470 ms men); INR increase < 4.5 Kinetic effect (S).
UM (gene duplication in absence of inactive or decreased activity alleles) Insufficient data to allow calculation of dose adjustent. Be alert to decreased haloperidol plasma concentration and adjust maintenance dose in response to haloperidol plasma concentration or select alternative drug (e.g., pimozide, flupenthixol, fluphenazine, quetiapine, olanzapine, clozapine). Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints. Clinical effect (S): long-standing discomfort (48-168 hr) without permanent injury e.g. failure of therapy with tricyclic antidepressants, atypical antipsychotic drugs; extrapyramidal side effects; parkinsonism; ADE resulting from increased bioavailability of tricyclic antidepressants, metoprolol, propafenone (central effects e.g. dizziness); INR 4.5-6.0; neutropenia 1.0-1.5x10^9/l; leucopenia 2.0-3.0x10^9/l; thrombocytopenia 50-75x10^9/l.
Allele Type Alleles
active *1, *2, *33, *35
decreased activity *9, *10, *17, *29, *36, *41
inactive *3-*8, *11-*16, *19-*21, *38, *40, *42

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with haloperidol that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105151

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
GenoChip CYP2D6 (PharmGenomics, GmbH) CYP2D6*5 , rs59421388 , rs28371725 , rs5030867 , rs5030656 , rs35742686 , rs3892097 , rs5030865 , rs5030655 , rs28371706 , rs5030863 , rs1065852 , *xN (gene duplication)

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP CA VA CYP2D6 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *1XN N/A N/A N/A
VIP CA VA CYP2D6 *2 N/A N/A N/A
VIP CA VA CYP2D6 *3 N/A N/A N/A
VIP CA VA CYP2D6 *4 N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *6 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *9 N/A N/A N/A
VIP CA VA CYP2D6 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *10A N/A N/A N/A
VIP CA VA CYP2D6 *17 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *29 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *41 N/A N/A N/A
No VIP available No VIP available VA HTR2C 2--1--1 N/A N/A N/A
No VIP available No VIP available VA SLC6A4 HTTLPR long form (L allele) N/A N/A N/A
No VIP available No VIP available VA SLC6A4 HTTLPR short form (S allele) N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1003641 113273636A>G, 16836052A>G
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs1049353 1260G>A, 1359G>A, 26973469C>T, 88853635C>T, Thr420=, Thr453=
C > T
Synonymous
Thr453Thr
rs1065852 100C>T, 21917263G>A, 42526694G>A, 5190C>T, CYP2D6:100C>T, Pro34Ser, part of CYP2D6*4 and CYP2D6*10
G > A
Missense
Pro34Ser
VIP No Clinical Annotations available No Variant Annotations available
rs16947 21914512A>G, 42523943A>G, 733C>C, 7941C>C, 886C>C, Arg245=, Arg296=, CYP2D6:2850C>T
A > G
Not Available
rs1800497 113270828G>A, 16833244G>A, 17316G>A, 2137G>A, 32806C>T, DRD2 Taq1A, DRD2:32806C>T, DRD2:Taq1A, DRD2:Taq1A A1, DRD2:TaqIA allele, Glu713Lys, Taq1A
G > A
Missense
Glu713Lys
No VIP available CA VA
rs2298826 1870-248G>A, 20599757G>A, 20659757G>A, 43812G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs2412459 11086516C>T, 3357+444C>T, 40295959C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs25531 -1936A>G, 28564346T>C, 3301340T>C, 3609A>G
T > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs2587550 113272925G>A, 16835341G>A, 19413G>A
G > A
Not Available
rs28371706 21916341G>A, 320C>T, 42525772G>A, 6112C>T, CYP2D6:1023 C>T, Thr107Ile
G > A
Missense
Thr107Ile
rs28371725 21914374C>T, 42523805C>T, 8079G>A, 832+39G>A, 985+39G>A, CYP2D6*41, CYP2D6:2988G>A, part of CYP2D6*41
C > T
Intronic
No VIP available CA VA
rs324420 15823C>A, 16842679C>A, 385C>A, 46870761C>A, C385A, FAAH:385C>A, FAAH:Pro129Thr, Pro129Thr
C > A
Missense
Pro129Thr
rs35742686 -1793delT, -1830delT, -1940delT, 23418678delT, 40+2664delT, 42128242delT, 50569delT, 50583delT, 598delA, 622delA, 6750delA, 775delA, Arg200Glyfs, Arg208Glyfs, Arg259Glyfs
T > -
Not Available
Arg208Gly
No VIP available No Clinical Annotations available VA
rs3813929 -759, -759C>T, -850C>T, 113818520C>T, 250852C>T, 4970C>T, HTR2C:, HTR2C: -759C/T
C > T
5' Flanking
rs3892097 21915516C>T, 353-1G>A, 42524947C>T, 506-1G>A, 6937G>A, CYP2D6*4, CYP2D6:1846G>A, part of CYP2D6*4
C > T
Acceptor
rs4680 1-5G>A, 19951271G>A, 27009G>A, 3103421G>A, 322G>A, 472G>A, COMP: Val158Met, COMT:Val108Met, Val108Met, Val158Met
G > A
5' Flanking
Val158Met
rs5030655 -1098delA, -1563delA, -951delA, -988delA, 23419520delA, 277delT, 353-140delT, 40+3506delA, 42129084delA, 454delT, 51411delA, 51425delA, 5908delT, CYP2D6*6, CYP2D6:1707 del T, Trp152Glyfs, Trp93Glyfs, part of CYP2D6*6
A > -
Not Available
Trp152Gly
rs5030656 21914745_21914747delCTT, 42524176_42524178delCTT, 688_690delAAG, 7706_7708delAAG, 841_843delAAG, Lys230del, Lys281del
CTT > -
CTT > TTC
Non-synonymous
No VIP available No Clinical Annotations available VA
rs518147 -697G>C, -788G>C, 113818582G>C, 250914G>C, 5032G>C, HTR2C: -697G/C
C > G
5' UTR
rs59421388 1012G>A, 21914179C>T, 3271G>A, 42523610C>T, 8274G>A, 859G>A, CYP2D6: 3183G>A, Val287Met, Val338Met
G > T
G > C
Missense
Val287Met
VIP No Clinical Annotations available No Variant Annotations available
rs61736512 1747G>A, 21915703C>T, 353-188G>A, 406G>A, 42525134C>T, 6750G>A, CYP2D6: 1659G>A, Val136Met
G > T
G > C
Intronic
Val136Met
No VIP available No Clinical Annotations available VA
rs6318 113965735G>C, 152185G>C, 398067G>C, 68G>C, Cys23Ser, HTR2C:23Ser, HTR2C:Cys23Ser
C > G
Missense
Cys23Ser
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
No VIP available No Clinical Annotations available VA
rs7912580 14720436G>A, 63915972G>A
G > A
Not Available
No VIP available CA VA
rs909706 -233+2174A>G, 15600871T>C, 15660871T>C, 246-119A>G, 56+2174A>G, 7401A>G
T > C
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
Trade Names
  • ALDO
  • Aloperidin
  • Aloperidol
  • Aloperidolo
  • Aloperidon
  • Apo-Haloperidol
  • Bioperidolo
  • Brotopon
  • Dozic
  • Dozix
  • Einalon S
  • Eukystol
  • Galoperidol
  • Haldol
  • Haldol Decanoate
  • Haldol La
  • Haldol Solutab
  • Halidol
  • Halojust
  • Halol
  • Halopal
  • Haloperido
  • Haloperidol Decanoate
  • Haloperidol Intensol
  • Haloperidol Lactate
  • Halopidol
  • Halopoidol
  • Halosten
  • Keselan
  • Lealgin Compositum
  • Linton
  • Mixidol
  • Novo-Peridol
  • Pekuces
  • Peluces
  • Peridol
  • Pernox
  • Pms Haloperidol
  • Serenace
  • Serenase
  • Serenelfi
  • Sernas
  • Sernel
  • Sigaperidol
  • Ulcolind
  • Uliolind
  • Vesalium
Brand Mixture Names

PharmGKB Accession Id:
PA449841

Description

A phenyl-piperidinyl-butyrophenone that is used primarily to treat schizophrenia and other psychoses. It is also used in schizoaffective disorder, delusional disorders, ballism, and tourette syndrome (a drug of choice) and occasionally as adjunctive therapy in mental retardation and the chorea of huntington disease. It is a potent antiemetic and is used in the treatment of intractable hiccups. (From AMA Drug Evaluations Annual, 1994, p279)

Source: Drug Bank

Indication

For the management of psychotic disorders (eg. schizophrenia) and delirium, as well as to control tics and vocal utterances of Tourette's syndrome (Gilles de la Tourette's syndrome). Also used for the treatment of severe behavioural problems in children with disrubtive behaviour disorder or ADHD (attention-deficit hyperactivity disorder). Haloperidol has been used in the prevention and control of severe nausea and vomiting.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known, but the drug appears to depress the CNS at the subcortical level of the brain, midbrain, and brain stem reticular formation. Haloperidol seems to inhibit the ascending reticular activating system of the brain stem (possibly through the caudate nucleus), thereby interrupting the impulse between the diencephalon and the cortex. The drug may antagonize the actions of glutamic acid within the extrapyramidal system, and inhibitions of catecholamine receptors may also contribute to haloperidol's mechanism of action. Haloperidol may also inhibit the reuptake of various neurotransmitters in the midbrain, and appears to have a strong central antidopaminergic and weak central anticholinergic activity. The drug produces catalepsy and inhibits spontaneous motor activity and conditioned avoidance behaviours in animals. The exact mechanism of antiemetic action of haloperidol has also not been fully determined, but the drug has been shown to directly affect the chemoreceptor trigger zone (CTZ) through the blocking of dopamine receptors in the CTZ.

Source: Drug Bank

Pharmacology

Haloperidol is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Haloperidol principal pharmacological effects are similar to those of piperazine-derivative phenothiazines. The drug has action at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Haloperidol has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.

Source: Drug Bank

Food Interaction

Take with food to reduce irritation, limit caffeine intake. Avoid alcohol.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

92%

Source: Drug Bank

Absorption

Oral-60%

Source: Drug Bank

Half-Life

3 weeks

Source: Drug Bank

Toxicity

LD 50=165 mg/kg (rats, oral)

Source: Drug Bank

Chemical Properties

Chemical Formula

C21H23ClFNO2

Source: Drug Bank

Isomeric SMILES

c1cc(ccc1C(=O)CCCN2CCC(CC2)(c3ccc(cc3)Cl)O)F

Source: OpenEye

Canonical SMILES

OC1(CCN(CCCC(=O)C2=CC=C(F)C=C2)CC1)C1=CC=C(Cl)C=C1

Source: Drug Bank

Average Molecular Weight

375.864

Source: Drug Bank

Monoisotopic Molecular Weight

375.140134897

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Antiarrhythmic Pathway, Pharmacodynamics
    Pharmacodynamic pathway of antiarrhythmic drugs in a stylized cardiac myocyte.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
DRD1 (source: Drug Bank)
DRD2 (source: Drug Bank)
DRD3 (source: Drug Bank)
GRIN2B (source: Drug Bank)
HTR2A (source: Drug Bank)

Drug Interactions

Drug Description
haloperidol The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank)
haloperidol The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol Decreases the effect of haloperidol (source: Drug Bank)
haloperidol Decreases the effect of haloperidol (source: Drug Bank)
haloperidol Increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol Increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The agent decreases the effect of guanethidine (source: Drug Bank)
haloperidol Haloperidol may decrease the effect of guanethidine. (source: Drug Bank)
atomoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank)
atomoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank)
atropine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
atropine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
benztropine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
benztropine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
biperiden The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
biperiden The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
carbamazepine Carbamazepine decreases the effect of haloperidol (source: Drug Bank)
carbamazepine Carbamazepine decreases the effect of haloperidol (source: Drug Bank)
clidinium The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
clidinium The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
clozapine Clozapine increases the effect and toxicity of haloperidol (source: Drug Bank)
clozapine Clozapine increases the effect and toxicity of haloperidol (source: Drug Bank)
dicyclomine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
dicyclomine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
ethopropazine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
ethopropazine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
fluconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
fluconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
glycopyrrolate The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
glycopyrrolate The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
guanethidine The agent decreases the effect of guanethidine (source: Drug Bank)
guanethidine Haloperidol may decrease the effect of guanethidine. (source: Drug Bank)
hyoscyamine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
hyoscyamine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
isopropamide The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
isopropamide The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
itraconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
itraconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
ketoconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
ketoconazole The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
l-methyldopa Methyldopa increases haloperidol effect or risk of psychosis (source: Drug Bank)
lithium Possible extrapyramidal effects and neurotoxicity with this combination (source: Drug Bank)
lithium Possible extrapyramidal effects and neurotoxicity with this combination (source: Drug Bank)
mepenzolate The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
mepenzolate The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mesoridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
methantheline The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
methantheline The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
Methyldopa Methyldopa increases haloperidol effect or risk of psychosis (source: Drug Bank)
Methyldopa Methyldopa increases haloperidol effect or risk of psychosis (source: Drug Bank)
orphenadrine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
orphenadrine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
oxyphencyclimine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
oxyphencyclimine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
procyclidine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
procyclidine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
propantheline The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
propantheline The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
propranolol Increased effect of both drugs (source: Drug Bank)
rifabutin The rifamycin decreases the effect of haloperidol (source: Drug Bank)
rifabutin The rifamycin decreases the effect of haloperidol (source: Drug Bank)
rifampin The rifamycin decreases the effect of haloperidol (source: Drug Bank)
rifampin The rifamycin decreases the effect of haloperidol (source: Drug Bank)
scopolamine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
scopolamine The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thioridazine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
tridihexethyl The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
tridihexethyl The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
trihexyphenidyl The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
trihexyphenidyl The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol The imidazole increases the effect and toxicity of haloperidol (source: Drug Bank)
haloperidol Methyldopa increases haloperidol effect or risk of psychosis (source: Drug Bank)
haloperidol Methyldopa increases haloperidol effect or risk of psychosis (source: Drug Bank)
haloperidol Possible extrapyramidal effects and neurotoxicity with this combination (source: Drug Bank)
haloperidol Possible extrapyramidal effects and neurotoxicity with this combination (source: Drug Bank)
haloperidol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
haloperidol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
haloperidol Increased effect of both drugs (source: Drug Bank)
haloperidol Increased effect of both drugs (source: Drug Bank)
haloperidol The rifamycin decreases the effect of haloperidol (source: Drug Bank)
haloperidol The rifamycin decreases the effect of haloperidol (source: Drug Bank)
haloperidol The rifamycin decreases the effect of haloperidol (source: Drug Bank)
haloperidol The rifamycin decreases the effect of haloperidol (source: Drug Bank)
haloperidol The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Haloperidol, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank)
haloperidol The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Haloperidol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents. (source: Drug Bank)
haloperidol Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
haloperidol Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
haloperidol Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
haloperidol Haloperidol, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Haloperidol is initiated, discontinued, or dose changed. (source: Drug Bank)
haloperidol Haloperidol, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Haloperidol is initiated, discontinued, or dose changed. (source: Drug Bank)
haloperidol Telithromycin may reduce clearance of Haloperidol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Haloperidol if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol Terbinafine may reduce the metabolism and clearance of Haloperidol. Consider alternate therapy or monitor for therapeutic/adverse effects of Haloperidol if Terbinafine is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. (source: Drug Bank)
haloperidol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
haloperidol Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
haloperidol May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
haloperidol May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
haloperidol Haloperidol may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
haloperidol Haloperidol may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
haloperidol Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank)
haloperidol Haloperidol may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Haloperidol may decrease the effect of Tramadol by decreasing active metabolite production. (source: Drug Bank)
haloperidol The CYP3A4 inhibitor, Haloperidol, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. The CYP2D6 inhibitor, Trazodone, may increase the efficacy of Haloperidol by decreasing Haloperidol metabolism and clearance. Monitor for changes in Trazodone and Haloperidol efficacy/toxicity if either agent is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol The CYP3A4 inhibitor, Haloperidol, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. The CYP2D6 inhibitor, Trazodone, may increase the efficacy of Haloperidol by decreasing Haloperidol metabolism and clearance. Monitor for changes in Trazodone and Haloperidol efficacy/toxicity if either agent is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol Trimethobenzamide and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
haloperidol Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
haloperidol Triprolidine and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank)
haloperidol Triprolidine and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank)
haloperidol Trospium and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
haloperidol Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of haloperidol by decreasing its metabolism. Additive QTc prolongation may also occur. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of haloperidol if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)
haloperidol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank)
haloperidol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to haloperidol: 70

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Genome-wide association study supports the role of the immunological system and of the neurodevelopmental processes in response to haloperidol treatment. Pharmacogenetics and genomics. 2014. Drago Antonio, et al. PubMed
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The association study of polymorphisms in DAT, DRD2, and COMT genes and acute extrapyramidal adverse effects in male schizophrenic patients treated with haloperidol. Journal of clinical psychopharmacology. 2013. Zivković Maja, et al. PubMed
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Role of ethnicity in antipsychotic-induced weight gain and tardive dyskinesia: genes or environment?. Pharmacogenomics. 2013. Chan Lai Fong, et al. PubMed
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Influence of ANKK1 and DRD2 polymorphisms in response to haloperidol. European archives of psychiatry and clinical neuroscience. 2013. Giegling Ina, et al. PubMed
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Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed
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The AmpliChip® CYP450 test and response to treatment in schizophrenia and obsessive compulsive disorder: a pilot study and focus on cases with abnormal CYP2D6 drug metabolism. Genetic testing and molecular biomarkers. 2012. Müller Daniel J, et al. PubMed
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PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
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Genetic association study between antipsychotic-induced weight gain and the melanocortin-4 receptor gene. The pharmacogenomics journal. 2012. Chowdhury N I, et al. PubMed
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Sexual dysfunction in male schizophrenia: influence of antipsychotic drugs, prolactin and polymorphisms of the dopamine D2 receptor genes. Pharmacogenomics. 2011. Zhang Xiang Rong, et al. PubMed
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Glutamatergic gene variants impact the clinical profile of efficacy and side effects of haloperidol. Pharmacogenetics and genomics. 2011. Giegling Ina, et al. PubMed
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Pharmacogenetics: From Bench to Byte- An Update of Guidelines. Clinical pharmacology and therapeutics. 2011. Swen J J, et al. PubMed
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Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
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Drug-induced long QT syndrome. Pharmacological reviews. 2010. Kannankeril Prince, et al. PubMed
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Polymorphisms of the HTR2C gene and antipsychotic-induced weight gain: an update and meta-analysis. Pharmacogenomics. 2010. Sicard Michelle N, et al. PubMed
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Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain. Journal of clinical psychopharmacology. 2010. Monteleone Palmiero, et al. PubMed
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Drug- and non-drug-associated QT interval prolongation. British journal of clinical pharmacology. 2010. van Noord Charlotte, et al. PubMed
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Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
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Human lymphoblastoid cell line panels: novel tools for assessing shared drug pathways. Pharmacogenomics. 2010. Morag Ayelet, et al. PubMed
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Serotonin transporter polymorphisms and early response to antipsychotic treatment in first episode of psychosis. Psychiatry research. 2010. Vázquez-Bourgon Javier, et al. PubMed
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Cytochrome P450 2D6. Pharmacogenetics and genomics. 2009. Owen Ryan P, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
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The efficacies of clozapine and haloperidol in refractory schizophrenia are related to DTNBP1 variation. Pharmacogenetics and genomics. 2009. Zuo Lingjun, et al. PubMed
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Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
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DRD4 48 bp VNTR but not 5-HT 2C Cys23Ser receptor polymorphism is related to antipsychotic-induced weight gain. The pharmacogenomics journal. 2009. Popp J, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
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Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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Influence of cytochrome P450 polymorphisms on drug therapies: pharmacogenetic, pharmacoepigenetic and clinical aspects. Pharmacology & therapeutics. 2007. Ingelman-Sundberg Magnus, et al. PubMed
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HTR2C haplotypes and antipsychotics-induced weight gain: X-linked multimarker analysis. Human psychopharmacology. 2007. De Luca Vincenzo, et al. PubMed
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No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. The pharmacogenomics journal. 2007. Theisen F M, et al. PubMed
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Depot haloperidol treatment in outpatients with schizophrenia on monotherapy: impact of CYP2D6 polymorphism on pharmacokinetics and treatment outcome. Therapeutic drug monitoring. 2007. Panagiotidis Georgios, et al. PubMed
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Risk of extrapyramidal syndrome in schizophrenic patients treated with antipsychotics: a population-based study. Clinical pharmacology and therapeutics. 2007. Yang S-Y, et al. PubMed
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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
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Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs. The Journal of pharmacology and experimental therapeutics. 2006. Katchman Alexander N, et al. PubMed
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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Antipsychotic drugs activate SREBP-regulated expression of lipid biosynthetic genes in cultured human glioma cells: a novel mechanism of action?. The pharmacogenomics journal. 2005. Fernø J, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Relationship between haloperidol plasma concentration, debrisoquine metabolic ratio, CYP2D6 and CYP2C9 genotypes in psychiatric patients. Pharmacopsychiatry. 2004. LLerena Adrián, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
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Haloperidol plasma concentration in Japanese psychiatric subjects with gene duplication of CYP2D6. British journal of clinical pharmacology. 2003. Ohnuma Tohru, et al. PubMed
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Effects of smoking and cytochrome P450 2D6*10 allele on the plasma haloperidol concentration/dose ratio. Progress in neuro-psychopharmacology & biological psychiatry. 2003. Ohara Koichi, et al. PubMed
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Effect of CYP2D6 genotypes on the metabolism of haloperidol in a Japanese psychiatric population. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2003. Someya Toshiyuki, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Pharmacokinetics and QT interval pharmacodynamics of oral haloperidol in poor and extensive metabolizers of CYP2D6. The pharmacogenomics journal. 2003. Desai M, et al. PubMed
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The impact of the CYP2D6 polymorphism on haloperidol pharmacokinetics and on the outcome of haloperidol treatment. Clinical pharmacology and therapeutics. 2002. Brockmöller Jürgen, et al. PubMed
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Effect of the CYP2D6 genotype on prolactin concentration in schizophrenic patients treated with haloperidol. Schizophrenia research. 2001. Yasui-Furukori N, et al. PubMed
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Plasma concentrations of haloperidol are related to CYP2D6 genotype at low, but not high doses of haloperidol in Korean schizophrenic patients. British journal of clinical pharmacology. 2001. Roh H K, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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Association of short-term response to haloperidol treatment with a polymorphism in the dopamine D(2) receptor gene. The American journal of psychiatry. 2001. Schäfer M, et al. PubMed
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CYP2D6*10 alleles are not the determinant of the plasma haloperidol concentrations in Asian patients. Therapeutic drug monitoring. 2000. Shimoda K, et al. PubMed
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Science, medicine, and the future: Pharmacogenetics. BMJ (Clinical research ed.). 2000. Wolf C R, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Effects of the CYP2D6*10 allele on the steady-state plasma concentrations of haloperidol and reduced haloperidol in Japanese patients with schizophrenia. Clinical pharmacology and therapeutics. 1999. Mihara K, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica; the fate of foreign compounds in biological systems. 1998. Tassaneeyakul W, et al. PubMed
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Effects of the CYP2D6 genotype on the steady-state plasma concentrations of haloperidol and reduced haloperidol in Japanese schizophrenic patients. Pharmacogenetics. 1997. Suzuki A, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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Selective serotonin reuptake inhibitors and CNS drug interactions. A critical review of the evidence. Clinical pharmacokinetics. 1997. Sproule B A, et al. PubMed
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Coadministration of fluvoxamine increases serum concentrations of haloperidol. Journal of clinical psychopharmacology. 1994. Daniel D G, et al. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed
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Oxidation of reduced haloperidol to haloperidol: involvement of human P450IID6 (sparteine/debrisoquine monooxygenase). British journal of clinical pharmacology. 1991. Tyndale R F, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0121-0581-04
DrugBank:
DB00502
ChEBI:
5613
KEGG Compound:
C01814
KEGG Drug:
D00136
PubChem Compound:
3559
PubChem Substance:
148665
46508794
IUPHAR Ligand:
86
Drugs Product Database (DPD):
761745
BindingDB:
21398
ChemSpider:
3438
Therapeutic Targets Database:
DAP000313
FDA Drug Label at DailyMed:
b488c106-f1ee-4b7b-8516-01162fb929f7

Clinical Trials

These are trials that mention haloperidol and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.