Drug/Small Molecule:
aripiprazole

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for aripiprazole and CYP2D6

Summary

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group (DPWG) recommends reducing maximum dose of aripiprazole for patients carrying poor metabolizer alleles of CYP2D6.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group (DPWG) has evaluated therapeutic dose recommendations for aripiprazole based on CYP2D6 genotypes [Article:21412232]. They recommend reducing maximum dose of aripiprazole for patients carrying poor metabolizer alleles of CYP2D6.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
PM (two inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) alleles) Reduce maximum dose to 10 mg/day (67% of the maximum recommended daily dose). 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 1.0-1.5x109/l; leucopenia 2.0-3.0x109/l; thrombocytopenia 50-75x109/l.
IM (two decreased-activity (*9, *10, *17, *29, *36, *41) alleles or carrying one active (*1, *2, *33, *35) and one inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) allele, or carrying one decreased-activity (*9, *10, *17, *29, *36, *41) allele and one inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) allele) No recommendations. 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 female, <470 ms male); INR increase < 4.5; Kinetic effect (S)
UM (a gene duplication in absence of inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) or decreased-activity (*9, *10, *17, *29, *36, *41) alleles) No recommendations. -- --
  • *See Methods or PMID: 18253145 for definition of "good quality."
  • S: statistically significant difference.
  • Please see attached PDF for detailed information about the evaluated studies: Aripiprazole CYP2D6

PharmGKB annotates drug labels containing pharmacogenetic information approved by the US Food and Drug Administration (FDA), European Medicines Agency (EMA) and the Pharmaceuticals and Medical Devices Agency, Japan (PMDA). PharmGKB annotations provide a brief summary of the PGx in the label, an excerpt from the label and a downloadable highlighted label PDF file. A list of genes and phenotypes found within the label is mapped to label section headers and listed at the end of each annotation. PharmGKB also attempts to interpret the level of action implied in each label with the "PGx Level" tag.

Sources:

  • FDA Information is gathered from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" and from FDA-approved labels brought to our attention. Please note that drugs may be removed from or added to the FDA's Table without our knowledge. We periodically check the Table for changes and update PharmGKB accordingly. Drugs listed on the Table to our knowledge are tagged with the Biomarker icon. A drug label that has been removed from the Table will not have the Biomarker icon but will continue to have an annotation on PharmGKB stating the label has been removed from the FDA's Table. We acquire label PDF files from DailyMed.
  • EMA European Public Assessment Reports (EPARs) that contain PGx information were identified from [Article:24433361] and also by searching for drugs for which we have PGx-containing FDA drug labels.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA, PMDA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for aripiprazole and CYP2D6

Actionable PGx

Summary

Elimination of aripiprazole is mainly via metabolism by CYP2D6 and CYP3A4 - the FDA-approved drug label contains information regarding dose adjustment in patients who are CYP2D6 poor metabolizers, or in patients taking concomittant drugs that may inhibit or induce CYP2D6 or CYP3A4.

Annotation

Aripiprazole is an atypical antipsychotic medication mainly used for the treatment of schizophrenia. It is also indicated for the acute and maintenance treatment of manic and mixed episodes associated with bipolar I disorder and for an adjunctive therapy treatment to antidepressants for the treatment of major depressive disorder. The mechanism of action is unknown, but aripiprazole shows partial agonist activity at DRD2 and HTR1A receptors and antagonist activity at HTR2A receptors. Aripiprazole undergoes hepatic metabolization, primarily by the cytochrome P450 enzymes CYP3A4 and CYP2D6.

CYP2D6 poor metabolizers have about an 80% increase in aripiprazole exposure and about a 30% decrease in exposure to the active metabolite compared extensive metabolizers, resulting in about a 60% higher exposure to the total active moieties from a given dose of aripiprazole. Co-administration with known inhibitors of CYP2D6 or CYP3A4 can inhibit aripiprazole elimination and cause increased blood concentration levels.

Excerpts from the Aripiprazole drug label:

Dosing recommendation in patients who are classified as CYP2D6 poor metabolizers (PM): The aripiprazole dose in PM patients should initially be reduced to one-half (50%) of the usual dose and then adjusted to achieve a favorable clinical response. The dose of aripiprazole for PM patients who are administered a strong CYP3A4 inhibitor should be reduced to one-quarter (25%) of the usual dose.


Strong CYP3A4 (eg, ketoconazole) or CYP2D6 (eg, fluoxetine) inhibitors will increase ABILIFY drug concentrations; reduce ABILIFY dose to one-half of the usual dose when used concomitantly (2.6, 7.1), except when used as adjunctive treatment with antidepressants


CYP3A4 inducers (eg, carbamazepine) will decrease ABILIFY drug concentrations; double ABILIFY dose when used concomitantly

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Aripiprazole drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Movement Disorders
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Weight gain
    • Adverse reactions section
    • source: PHONT
  • CYP2D6
    • Dosage & administration section, Drug interactions section, Pharmacokinetics section, dosage, metabolism/PK
    • source: FDA Label
  • CYP3A4
    • Dosage & administration section, Drug interactions section, Pharmacokinetics section, dosage, metabolism/PK
    • source: FDA Label
  • HTR1A
    • Pharmacodynamics section
    • source: FDA Label
  • HTR2A
    • Pharmacodynamics section, other
    • source: FDA Label

last updated 10/25/2013

European Medicines Agency (EMA) Label for aripiprazole and CYP2D6, CYP3A4

Actionable PGx

Summary

The EMA European Public Assessment Report (EPAR) recommends dose adjustments when aripiprazole is taken with CYP3A4 inhibitors in CYP2D6 poor metabolizers, or concomitant use of CYP3A4 or CYP2D6 inhibitors, or CYP3A4 inducers.

Annotation

Excerpt from the aripiprazole (Abilify) EPAR:

Dose adjustments due to interactions: When concomitant administration of potent CYP3A4 or CYP2D6 inhibitors with aripiprazole occurs, the aripiprazole dose should be reduced. When the CYP3A4 or CYP2D6 inhibitor is withdrawn from the combination therapy, aripiprazole dose should then be increased (see section 4.5).
When concomitant administration of potent CYP3A4 inducers with aripiprazole occurs, the aripiprazole dose should be increased. When the CYP3A4 inducer is withdrawn from the combination therapy, the aripiprazole dose should then be reduced to the recommended dose (see section 4.5).

In a clinical trial in healthy subjects, a potent inhibitor of CYP3A4 (ketoconazole) increased aripiprazole AUC and Cmax by 63% and 37%, respectively. The AUC and Cmax of dehydro-aripiprazole 6 increased by 77% and 43%, respectively. In CYP2D6 poor metabolisers, concomitant use of potent inhibitors of CYP3A4 may result in higher plasma concentrations of aripiprazole compared to that in CYP2D6 extensive metabolizers. When considering concomitant administration of ketoconazole or other potent CYP3A4 inhibitors with ABILIFY, potential benefits should outweigh the potential risks to the patient. When concomitant administration of ketoconozole with ABILIFY occurs, ABILIFY dose should be reduced to approximately one-half of its prescribed dose. Other potent inhibitors of CYP3A4, such as itraconazole and HIV protease inhibitors, may be expected to have similar effects and similar dose reductions should therefore be applied.

This information is highlighted in the following sections:
Posology and method of administration, Interaction with other medicinal products and other forms of interaction, Pharmacokinetic properties, Before you use abilify.

For the complete EPAR text with sections containing pharmacogenetic information highlighted, see the aripiprazole EMA EPAR

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.


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.

? = Mouse-over for quick help

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 , CYP2D6 *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.

List of all aripiprazole variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA VA CYP2D6 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *3 N/A N/A N/A
No VIP available CA VA CYP2D6 *4 N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
No VIP available CA VA CYP2D6 *6 N/A N/A N/A
No VIP available CA VA CYP2D6 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *21 N/A N/A N/A
No VIP available CA VA CYP2D6 *41 N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1011313 -22+4543A>G, 117+4543A>G, 15573432T>C, 15633432T>C, 171+4543A>G, 222+4543A>G, 34840A>G, 550+4543A>G
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs1049353 1260G>A, 1359G>A, 26973469C>T, 88853635C>T, Thr420=, Thr453=
C > T
Synonymous
Thr453Thr
No VIP available CA VA
rs1799732 -487_-486insC, 113346252_113346253insG, 16908668_16908669insG, 4749_4750insC, DRD2: -141C Ins/Del
- > G
5' Flanking
No VIP available No Clinical Annotations available VA
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 No Clinical Annotations available VA
rs1801028 113283484G>C, 16845900G>C, 67518C>G, 845C>G, 932C>G, DRD2:1097C>G, DRD2:Ser311Cys, Ser282Cys, Ser311Cys
G > C
Missense
Ser282Cys
No VIP available No Clinical Annotations available VA
rs2005976 -83+742G>A, 110+1516G>A, 15590802C>T, 15650802C>T, 161+742G>A, 17470G>A, 489+742G>A, 56+12243G>A
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2304865 10548+168G>C, 112073084C>G, 187525363C>G
C > G
Intronic
No VIP available No Clinical Annotations available VA
rs2306987 112064376T>A, 13138+188A>T, 187516655T>A
T > A
Intronic
No VIP available No Clinical Annotations available VA
rs2306990 112066697C>T, 12258-30G>A, 187518976C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2391191 -105G>A, -125G>A, 106119446G>A, 19209122G>A, 506-677C>T, 6231G>A, 89G>A, Arg30Lys
G > A
Intronic
Arg30Lys
No VIP available No Clinical Annotations available VA
rs2619522 -232-1278T>G, 14623T>G, 15593649A>C, 15653649A>C, 385-1278T>G, 56+9396T>G, 57-1278T>G
A > C
Intronic
No VIP available No Clinical Annotations available VA
rs2637777 10660T>G, 112072741A>C, 187525020A>C, Ser3554Ala
A > C
Missense
Ser3554Ala
No VIP available No Clinical Annotations available VA
rs3213207 -21-396A>G, 118-396A>G, 15568102T>C, 15628102T>C, 172-396A>G, 223-396A>G, 40170A>G, 551-396A>G
T > C
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
No VIP available No Clinical Annotations available VA
rs6277 113283459G>A, 16845875G>A, 67543C>T, 870C>T, 957C>T, C957T, DRD2: C957T, DRD2:1035C>T, DRD2:1122C>T, DRD2:957C>T, Pro290=, Pro319=
G > A
Synonymous
Pro290Pro
No VIP available No Clinical Annotations available VA
rs6280 113890815C>T, 12085G>A, 20385961C>T, 25G>A, DRD3 Ser9Gly, DRD3 rs6280, DRD3: 9 Ser>Gly, DRD3: Gly9Ser, DRD3: Ser9Gly, DRD3:Ser9Gly, Gly9Ser, c.25T>C, p.S9G
C > T
Missense
Gly9Ser
No VIP available No Clinical Annotations available VA
rs760761 -83+412C>T, 110+1186C>T, 15591132G>A, 15651132G>A, 161+412C>T, 17140C>T, 489+412C>T, 56+11913C>T
G > A
Intronic
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
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • OPC 31
  • OPC-14597
  • aripiprazole
Trade Names
  • Abilify
  • Abilitat
Brand Mixture Names

PharmGKB Accession Id:
PA10026

Description

Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.

Source: Drug Bank

Indication

For the treatment of schizophrenia and related psychotic disorders.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.

Source: Drug Bank

Pharmacology

Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.

Source: Drug Bank

Food Interaction

Avoid alcohol (possible additive effect to CNS).|Food has no significant effect on absorption.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic.

Source: Drug Bank

Protein Binding

>99%

Source: Drug Bank

Half-Life

75-146 hours

Source: Drug Bank

Route of Elimination

Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.

Source: Drug Bank

Volume of Distribution

  • 4.9 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C23H27Cl2N3O2

Source: Drug Bank

Isomeric SMILES

c1cc(c(c(c1)Cl)Cl)N2CCN(CC2)CCCCOc3ccc4c(c3)NC(=O)CC4

Source: OpenEye

Canonical SMILES

ClC1=CC=CC(N2CCN(CCCCOC3=CC4=C(CCC(=O)N4)C=C3)CC2)=C1Cl

Source: Drug Bank

Average Molecular Weight

448.385

Source: Drug Bank

Monoisotopic Molecular Weight

447.148032537

Source: Drug Bank

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
ADRA1A (source: Drug Bank)
ADRA1B (source: Drug Bank)
ADRA2A (source: Drug Bank)
ADRA2B (source: Drug Bank)
ADRA2C (source: Drug Bank)
CHRM1 (source: Drug Bank)
CHRM2 (source: Drug Bank)
CHRM3 (source: Drug Bank)
CHRM4 (source: Drug Bank)
CHRM5 (source: Drug Bank)
DRD1 (source: Drug Bank)
DRD2 (source: Drug Bank)
DRD3 (source: Drug Bank)
DRD4 (source: Drug Bank)
DRD5 (source: Drug Bank)
HRH1 (source: Drug Bank)
HTR1A (source: Drug Bank)
HTR1B (source: Drug Bank)
HTR1D (source: Drug Bank)
HTR1E (source: Drug Bank)
HTR2A (source: Drug Bank)
HTR2C (source: Drug Bank)
HTR3A (source: Drug Bank)
HTR6 (source: Drug Bank)
HTR7 (source: Drug Bank)

Drug Interactions

Drug Description
carbamazepine Carbamazepine decreases the effect of aripiprazole (source: Drug Bank)
carbamazepine Carbamazepine decreases the effect of aripiprazole (source: Drug Bank)
itraconazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
itraconazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
ketoconazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
ketoconazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
quinidine Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank)
quinidine Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank)
quinidine Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank)
aripiprazole Decreases the effect of aripiprazole (source: Drug Bank)
aripiprazole Decreases the effect of aripiprazole (source: Drug Bank)
aripiprazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
aripiprazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
aripiprazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
aripiprazole The imidazole increases the effect of aripiprazole (source: Drug Bank)
aripiprazole Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank)
aripiprazole Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank)
aripiprazole Tacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Aripiprazole. Monitor for extrapyramidal symptoms. (source: Drug Bank)
aripiprazole Telithromycin may reduce clearance of Aripiprazole. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aripiprazole if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
aripiprazole Terbinafine may reduce the metabolism and clearance of Aripiprazole. Consider alternate therapy or monitor for therapeutic/adverse effects of Aripiprazole if Terbinafine is initiated, discontinued or dose changed. (source: Drug Bank)
aripiprazole May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. (source: Drug Bank)
aripiprazole The 2D6 inhibitor, Trazodone, may increase the efficacy of Aripiprazole by decreasing Ariprazole metabolism and clearance. Monitor for changes in Aripiprazole efficacy if Trazodone is initiated, discontinued or dose changed. (source: Drug Bank)
aripiprazole The 2D6 inhibitor, Trazodone, may increase the efficacy of Aripiprazole by decreasing Ariprazole metabolism and clearance. Monitor for changes in Aripiprazole efficacy if Trazodone is initiated, discontinued or dose changed. (source: Drug Bank)
aripiprazole The CNS depressants, Triprolidine and Aripiprazole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
aripiprazole The CNS depressants, Triprolidine and Aripiprazole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
aripiprazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of aripiprazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of aripiprazole if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to aripiprazole: 28

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Serum concentrations of risperidone and aripiprazole in subgroups encoding CYP2D6 intermediate metabolizer phenotype. Therapeutic drug monitoring. 2014. Hendset Magnhild, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The relationship between clinical pharmacokinetics of aripiprazole and CYP2D6 genetic polymorphism: effects of CYP enzyme inhibition by coadministration of paroxetine or fluvoxamine. European journal of clinical pharmacology. 2012. Azuma Junichi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphisms of the LEP, LEPR and HTR2C gene: obesity and BMI change in patients using antipsychotic medication in a naturalistic setting. Pharmacogenomics. 2011. Gregoor Jochem G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics: From Bench to Byte- An Update of Guidelines. Clinical pharmacology and therapeutics. 2011. Swen J J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Weight gain related to treatment with atypical antipsychotics is due to activation of PKC-beta. The pharmacogenomics journal. 2010. Pavan C, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
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
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Influence of DAOA gene variants on antipsychotic response after switch to aripiprazole. Psychiatry research. 2010. Pae Chi-Un, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
D2 receptor genetic variation and clinical response to antipsychotic drug treatment: a meta-analysis. The American journal of psychiatry. 2010. Zhang Jian-Ping, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
No influence of FAT polymorphisms in response to aripiprazole. Journal of human genetics. 2010. Pae Chi-Un, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
No influence of DTNBP1 polymorphisms on the response to aripiprazole. Neuropsychobiology. 2010. Pae Chi-Un, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ADME pharmacogenetics: current practices and future outlook. Expert opinion on drug metabolism & toxicology. 2009. Grossman Iris. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Effects of the DRD3 Ser9Gly polymorphism on aripiprazole efficacy in schizophrenic patients as modified by clinical factors. Progress in neuro-psychopharmacology & biological psychiatry. 2009. Chen Shih-Fen, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients. Journal of psychiatric research. 2009. Shen Yu-Chih, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Movement disorders associated with aripiprazole use: a case series. The International journal of neuroscience. 2009. Hall Deborah A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Taq1A polymorphism in the dopamine D2 receptor gene predicts brain metabolic response to aripiprazole in healthy male volunteers. Pharmacogenetics and genomics. 2008. Kim Euitae, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of the CYP2D6 genotype on steady-state serum concentrations of aripiprazole and dehydroaripiprazole. European journal of clinical pharmacology. 2007. Hendset Magnhild, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacokinetics of aripiprazole, a new antipsychotic, following oral dosing in healthy adult Japanese volunteers: influence of CYP2D6 polymorphism. Drug metabolism and pharmacokinetics. 2007. Kubo Masanori, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
The relationship between the therapeutic response to risperidone and the dopamine D2 receptor polymorphism in Chinese schizophrenia patients. The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 2007. Xing Qinghe, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients. The American journal of psychiatry. 2006. Lencz Todd, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association study of 12 polymorphisms spanning the dopamine D(2) receptor gene and clozapine treatment response in two treatment refractory/intolerant populations. Psychopharmacology. 2005. Hwang Rudi, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Response to chlorpromazine treatment may be associated with polymorphisms of the DRD2 gene in Chinese schizophrenic patients. Neuroscience letters. 2005. Wu Shengnan, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
The -141C Ins/Del polymorphism in the dopamine D2 receptor gene promoter region is associated with anxiolytic and antidepressive effects during treatment with dopamine antagonists in schizophrenic patients. Pharmacogenetics. 2001. Suzuki A, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Lack of association between a polymorphism in the promoter region of the dopamine-2 receptor gene and clozapine response. Pharmacogenetics. 1998. Arranz M J, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Functional polymorphism of -141C Ins/Del in the dopamine D2 receptor gene promoter and schizophrenia. Psychiatry research. 1998. Ohara K, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
59148-013-15
DrugBank:
DB01238
ChEBI:
31236
KEGG Compound:
C12564
KEGG Drug:
D01164
PubChem Compound:
60795
PubChem Substance:
46505745
582954
IUPHAR Ligand:
34
ChemSpider:
54790
Therapeutic Targets Database:
DAP000076
FDA Drug Label at DailyMed:
c040bd1d-45b7-49f2-93ea-aed7220b30ac

Clinical Trials

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

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

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