Drug/Small Molecule:
risperidone

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for risperidone and CYP2D6

Summary

Select an alternative drug or be extra alert to adverse drug events (ADR) for patients who are CYP2D6 poor metabolizers, intermediate metabolizers, or ultrarapid metabolizers with risperidone. Adjust risperidone dose to clinical response.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for risperidone based on CYP2D6 genotypes [Article:21412232]. For patients who are CYP2D6 poor metabolizers, intermediate metabolizers, or ultrarapid metabolizers, they recommend selecting an alternative drug or being extra alert to Adverse Drug Events and adjusting dose to clinical response.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
PM (two inactive (*3-*8, *11-*16, *19-*21, *38, *40, *42) alleles) Insufficient data to allow calculation of dose adjustment. Select alternative drug (e.g., quetiapine,olanzapine, clozapine) or be extra alert to ADEs and adjust dose to clinical response. 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 (> 168 hr), permanent symptom or invalidating injury e.g. failure of prophylaxis of atrial fibrillation; venous thromboembolism; decreased effect of clopidogrel on inhibition of platelet aggregation; ADE resulting from increased bioavailability of phenytoin; INR > 6.0; neutropenia 0.5-1.0x109/l; leucopenia 1.0-2.0x109/l; thrombocytopenia 25-50x109/l; severe diarrhea.
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) Insufficient data to allow calculation of dose adjustment. Select alternative drug (e.g., quetiapine, olanzapine, clozapine) or be extra alert to ADEs and adjust dose to clinical response. 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.
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) Insufficient data to allow calculation of dose adjustment. Select alternative drug (e.g., quetiapine, olanzapine, clozapine) or be extra alert to ADEs and adjust dose to clinical response. 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.

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 risperidone and CYP2D6

Informative PGx

Summary

Risperidone is metabolized to 9-hydroxyrisperidone by CYP2D6. Co-administration of drugs that are inhibitors or inducers of CYP2D6 along with risperidone may alter the plasma concentration of risperidone.

Annotation

Risperidone is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I disorder, and autism. CYP2D6 is important in its metabolism.

Excerpts from the risperidone drug label:

Risperidone is metabolized to 9-hydroxyrisperidone by CYP2D6, an enzyme that is polymorphic in the population and that can be inhibited by a variety of psychotropic and other drugs (see Clinical Pharmacology (12.3)). Drug interactions that reduce the metabolism of risperidone to 9-hydroxyrisperidone would increase the plasma concentrations of risperidone and lower the concentrations of 9-hydroxyrisperidone. Analysis of clinical studies involving a modest number of poor metabolizers does not suggest that poor and extensive metabolizers have different rates of adverse effects. No comparison of effectiveness in the two groups has been made.

CYP2D6 is subject to genetic polymorphism (about 6% to 8% of Caucasians, and a very low percentage of Asians, have little or no activity and are "poor metabolizers") and to inhibition by a variety of substrates and some non-substrates, notably quinidine. Extensive CYP2D6 metabolizers convert risperidone rapidly into 9-hydroxyrisperidone, whereas poor CYP2D6 metabolizers convert it much more slowly. Although extensive metabolizers have lower risperidone and higher 9- hydroxyrisperidone concentrations than poor metabolizers, the pharmacokinetics of risperidone and 9-hydroxyrisperidone combined, after single and multiple doses, are similar in extensive and poor metabolizers.

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

  • Bipolar Disorder
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Dyskinesia, Drug-Induced
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Dystonia
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Hyperprolactinemia
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Hypokinesia
    • Adverse reactions section
    • source: PHONT
  • Muscle Rigidity
    • Warnings section
    • source: PHONT
  • Psychotic Disorders
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Schizophrenia
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Tremor
    • Adverse reactions section
    • source: PHONT
  • Weight gain
    • Warnings section, Adverse reactions section
    • source: PHONT
  • CYP2D6
    • Drug interactions section, Clinical pharmacology section, metabolism/PK
    • source: FDA Label

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?
Roche AmpliChip CYP450 Test CYP2D6*1, CYP2D6*10A, CYP2D6*10B, CYP2D6*11, CYP2D6*15, CYP2D6*17, CYP2D6*19, CYP2D6*20, CYP2D6*29, CYP2D6*2A, CYP2D6*2B, CYP2D6*2D, CYP2D6*3, CYP2D6*40, CYP2D6*41, CYP2D6*4A, CYP2D6*4B, CYP2D6*4D, CYP2D6*4J, CYP2D6*4K, CYP2D6*5, CYP2D6*6A, CYP2D6*6B, CYP2D6*6C, CYP2D6*7, CYP2D6*8, CYP2D6*9 , CYP2D6 CYP2D6*1XN , CYP2D6 CYP2D6*2XN , CYP2D6 CYP2D6*4XN , CYP2D6 CYP2D6*10XN , CYP2D6 CYP2D6*17XN , CYP2D6 CYP2D6*35XN , CYP2D6 CYP2D6*41XN , CYP2D6 *35 , CYP2D6 *36
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 risperidone variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2C19 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *4 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *3 N/A N/A N/A
VIP CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA VA CYP2D6 *1XN N/A N/A N/A
VIP No VIP available No VIP available 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 CA VA 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 CA VA CYP2D6 *14 N/A N/A N/A
VIP No VIP available No VIP available 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 CYP3A4 *1 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *1B N/A N/A N/A
No VIP available No VIP available VA CYP3A7 *1A N/A N/A N/A
No VIP available No VIP available VA CYP3A7 *1C 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 CA VA SLC6A4 HTTLPR long form (L allele) N/A N/A N/A
No VIP available CA VA SLC6A4 HTTLPR short form (S allele) N/A N/A N/A
No VIP available CA VA
rs10042486 13855688C>T, 1791G>A, 63261329C>T
C > T
Not Available
No VIP available CA VA
rs1042713 148206440G>A, 148206440G>G, 46A>A, 46A>G, 46G>A, 5285A>A, 5285A>G, 9369367G>A, 9369367G>G, ADRB2:16Arg>Gly, ADRB2:Arg16Gly, ADRB2:Gly16Arg, Arg16, Arg16=
G > A
Missense
Arg16Gly
No VIP available No Clinical Annotations available VA
rs1045642 208920T>A, 208920T>C, 25171488A>G, 25171488A>T, 3435T>A, 3435T>C, 87138645A>G, 87138645A>T, ABCB1*6, ABCB1: 3435C>T, ABCB1: C3435T, ABCB1: c.3435C>T, ABCB1:3435C>T, Ile1145=, Ile1145Ile, MDR1 3435C>T, MDR1 C3435T, PGP C3435T, c.3435C>T, mRNA 3853C>T
A > T
A > G
Synonymous
Ile1145Ile
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 No Clinical Annotations available VA
rs10514062 26072575T>A, 75478216T>A
T > A
Not Available
rs1065852 100C>T, 21917263G>A, 42526694G>A, 5190C>T, CYP2D6:100C>T, Pro34Ser, part of CYP2D6*4 and CYP2D6*10
G > A
Missense
Pro34Ser
No VIP available No Clinical Annotations available VA
rs10917670 14521484C>T, 163032842C>T
C > T
Not Available
No VIP available CA VA
rs1128503 1236T>C, 167964T>C, 25043506A>G, 87550285A>G, ABCB1 1236C>T, ABCB1*8, ABCB1: c.1236T>C, ABCB1:1236C>T, ABCB1:1236T>C, Gly412=, Gly412Gly, mRNA 1654T>C, p.Gly412Gly
A > G
Not Available
Gly412Gly
No VIP available No Clinical Annotations available VA
rs1315115 140+42550G>A, 14567750G>A, 164292G>A, 33567750G>A, 51-116638G>A
G > A
Intronic
No VIP available CA VA
rs1414334 114138144C>G, 324594C>G, 456-3008C>G, 551-3008C>G, 570476C>G
C > G
Intronic
No VIP available CA VA
rs165599 *522G>A, 19956781G>A, 3108931G>A, 32519G>A, 52529C>T
G > A
3' UTR
No VIP available CA VA
rs167771 113876275G>A, 20371421G>A, 26625C>T, 383+2327C>T, rs167771:G>A
G > A
Intronic
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
No VIP available CA VA
rs1799732 -487_-486insC, 113346252_113346253insG, 16908668_16908669insG, 4749_4750insC, DRD2: -141C Ins/Del
- > G
5' Flanking
No VIP available CA VA
rs1799978 -585A>G, 113346351T>C, 16908767T>C, 4651A>G, DRD2: -241A>G, DRD2:A-241G
T > C
5' Flanking
No VIP available CA 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
rs1805054 19992513C>T, 267C>T, 6672601C>T, Tyr89=
C > T
Not Available
No VIP available CA VA
rs1806201 13717508G>A, 2664C>T, 420515C>T, 6477632G>A, Thr888=
G > A
Synonymous
Thr888Thr
No VIP available No Clinical Annotations available VA
rs1869295 1956-33791G>C, 2115-33791G>C, 236995045G>C, 2941304G>C, 597313G>C
G > C
Intronic
No VIP available No Clinical Annotations available VA
rs1995380 26107016G>C, 75512657G>C
G > C
Not Available
No VIP available No Clinical Annotations available VA
rs2020917 -628C>T, 103+340G>A, 19928884C>T, 3081034C>T, 4622C>T, 5476G>A
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs2032582 186947T>A, 186947T>G, 25193461A>C, 25193461A>T, 2677A, 2677G, 2677T, 2677T>A, 2677T>G, 3095G>T/A, 87160618A>C, 87160618A>T, 893 Ala, 893 Ser, 893 Thr, ABCB1*7, ABCB1: 2677G>T/A, ABCB1: 2677T/A>G, ABCB1: A893S, ABCB1: G2677T/A, ABCB1: c.2677G>T/A, ABCB1:2677G>A/T, ABCB1:2677G>T/A, ABCB1:A893T, Ala893Ser/Thr, MDR1, MDR1 G2677T/A, Ser893Ala, Ser893Thr, mRNA 3095G>T/A, p.Ala893Ser/Thr
A > T
A > C
Missense
Ser893Ala
Ser893Thr
No VIP available No Clinical Annotations available VA
rs2228622 414G>A, 4554432G>A, 4564432G>A, 79006G>A, Exon 4, SLC1A1:rs2228622G>A, SNP2, Thr138=, syn
G > A
Synonymous
Thr138Thr
No VIP available No Clinical Annotations available VA
rs2358531 26074145G>A, 75479786G>A
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs2412459 11086516C>T, 3357+444C>T, 40295959C>T
C > T
Intronic
No VIP available CA VA
rs2494732 105239192T>C, 1172+23A>G, 27890A>G, 86239192T>C
T > C
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 CA VA
rs2661319 -2167T>C, 14528419T>C, 163039777T>C, 335+459T>C, 44+459T>C, 6382T>C
T > C
Intronic
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
rs2842030 -1449G>T, 14529137G>T, 163040495G>T, 335+1177G>T, 44+1177G>T, 7100G>T
G > 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
rs3738883 192922256T>G, 43131674T>G, 536+149A>C
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs3780412 4562480T>C, 4572480T>C, 767+92T>C, 87054T>C, Intron 7, SLC1A1:rs3780412A>G, SNP4
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs3780413 4557353C>G, 4567353C>G, 484-316C>G, 81927C>G, Intron 5, SLC1A1:rss3780413C>G, SNP3
C > G
Intronic
No VIP available No Clinical Annotations available VA
rs3787429 30987496C>T, 60791404C>T, 996G>A, Ser332=
C > T
Synonymous
Ser332Ser
No VIP available No Clinical Annotations available VA
rs3787430 30987514C>T, 60791422C>T, 978G>A, Pro326=
C > T
Synonymous
Pro326Pro
No VIP available CA VA
rs3803300 *976T>C, 105269779T>C, 86269779T>C
T > C
3' UTR
No VIP available CA VA
rs3813928 -1088G>A, -995, -997G>A, 113818282G>A, 250614G>A, 4732G>A, HTR2C c.-995G>A
G > A
5' Flanking
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
No VIP available No Clinical Annotations available VA
rs4436578 -31-11361G>A, 113306765C>T, 16869181C>T, 44237G>A
C > T
Intronic
No VIP available CA VA
rs4483927 193+3515G>T, 22044400G>T, 3533502G>T
G > T
Intronic
No VIP available No Clinical Annotations available VA
rs4633 -1041C>T, 186C>T, 19950235C>T, 25973C>T, 3102385C>T, 36C>T, COMT: His62His, His12=, His62=
C > T
5' Flanking
His62His
No VIP available No Clinical Annotations available VA
rs4646437 21726C>T, 37397926G>A, 671-202C>T, 671-205C>T, 99365083G>A
G > A
Intronic
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
No VIP available No Clinical Annotations available VA
rs5443 10501C>T, 47295C>T, 6894875C>T, 6954875C>T, 825C>T, GNB3:825C>T, GNB3:Ser275Ser, Ser275=
C > T
Synonymous
Ser275Ser
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
rs6265 196G>A, 220G>A, 241G>A, 27619916C>T, 27679916C>T, 283G>A, 434C>T, 442G>A, 503C>T, 68690G>A, BDNF:Val66Met, Val148Met, Val66Met, Val74Met, Val81Met, Val95Met
C > T
Missense
Val66Met
No VIP available CA 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
rs6295 1-1019C>G, 1-1019G>C, 13852924C>C, 13852924C>G, 4555G>C, 4555G>G, 63258565C>C, 63258565C>G, HTR1A: -1019C/G
C > G
5' Flanking
No VIP available CA VA
rs6311 -1438, -510G>A, -998G>A, 28451478C>T, 4692G>A, 47471478C>T, G>A, HTR2A c.-1438G>A, HTR2A:, HTR2A: -1438G/A, HTR2A:-1438G>A
C > T
5' Flanking
No VIP available CA VA
rs6313 102C>T, 160+869C>T, 28449940G>A, 47469940G>A, 6230C>T, HTR2A:102C>T, HTR2A:T102C, Ser34=
G > A
Intronic
Ser34Ser
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
No VIP available No Clinical Annotations available VA
rs6882321 26158189A>C, 75563830A>C
A > C
Intronic
No VIP available CA VA
rs724226 -141+51186A>G, 24358217A>G, 86325374A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs7643645 -22-579A>G, 119525497A>G, 26020643A>G, 31167A>G, 96-579A>G
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs7732173 26072022A>G, 75477663A>G
A > G
Not Available
No VIP available No Clinical Annotations available VA
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 CA VA
rs7799039 127878783G>A, 2453G>A, 65911626G>A, LEP: -2548G/A
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs7912580 14720436G>A, 63915972G>A
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs874295 142488592G>A, 205+79256C>T, 32237255G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs933271 -92+1987T>C, 19931407T>C, 2953A>G, 3083557T>C, 7145T>C
T > C
Intronic
No VIP available CA VA
rs951439 14522333C>T, 163033691C>T, 296C>T
C > T
Not Available
No VIP available No Clinical Annotations available VA
rs9606186 104-1738G>C, 14001G>C, 19920359C>G, 3072509C>G
C > G
Intronic
No VIP available No Clinical Annotations available VA
rs9713 -245A>T, 12374426A>T, 162165008A>T
A > T
5' UTR
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Risperidona [Spanish]
  • Risperidonum [Latin]
  • risperdone
  • risperidone
Trade Names
  • Risperdal
  • Risperdal Consta
  • Risperdal M-Tab
  • Risperidal M-Tab
  • Risperin
  • Rispolept
  • Rispolin
  • Sequinan
Brand Mixture Names

PharmGKB Accession Id:
PA451257

Description

Risperidone, a benzisoxazole derivative, is an atypical antipsychotic drug with high affinity for 5-hydrotryptamine (5-HT) and dopamine D2 receptors. It is used primarily in the management of schizophrenia, inappropriate behavior in severe dementia and manic episodes associated with bipolar I disorder. Risperidone is effective for treating the positive and negative symptoms of schizophrenia owing to its affinity for its "loose" binding affinity for dopamine D2 receptors and additional 5-HT antagonism compared to first generation antipsychotics, which are strong, non-specific dopamine D2 receptor antagonists.

Source: Drug Bank

Indication

For the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropriate behavior due to aggression and/or psychosis in patients with severe dementia.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Blockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. Blockade of serotonergic 5-HT 2 receptors in the mesocortical tract, causes an excess of dopamine and an increase in dopamine transmission, resulting in an increase in dopamine transmission and an elimination of core negative symptoms. Dopamine receptors in the nigrostriatal pathway are not affected by risperidone and extrapyramidal effects are avoided. Like other 5-HT 2 antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors.

Source: Drug Bank

Pharmacology

Risperidone is an atypical antipsychotic medication. It is most often used to treat delusional psychosis (including schizophrenia), but risperidone is also used to treat some forms of bipolar disorder and psychotic depression. It also has shown some success in treating symptoms of Asperger's Syndrome and autism. Risperidone is now the most commonly prescribed antipsychotic medication in the United States.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone, which has approximately the same receptor binding affinity as risperidone. Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase. Risperidone also undergoes N-dealkylation to a lesser extent.

Source: Drug Bank

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone, which has approximately the same receptor binding affinity as risperidone. Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase. Risperidone also undergoes N-dealkylation to a lesser extent.

Source: PharmGKB

Protein Binding

Risperidone, ~88% bound; 9-hydroxyrisperidone, ~77% bound.

Source: Drug Bank

Absorption

Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.

Source: Drug Bank

Half-Life

20-24 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD 50=82.1mg/kg (orally in mice).

Source: Drug Bank

Route of Elimination

Risperidone is extensively metabolized in the liver.In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives were prolonged compared to young healthy subjects.

Source: Drug Bank

Volume of Distribution

  • 1 to 2 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C23H27FN4O2

Source: Drug Bank

Isomeric SMILES

Cc1c(c(=O)n2c(n1)CCCC2)CCN3CCC(CC3)c4c5ccc(cc5on4)F

Source: OpenEye

Canonical SMILES

CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCCC2=N1

Source: Drug Bank

Average Molecular Weight

410.4845

Source: Drug Bank

Monoisotopic Molecular Weight

410.211804333

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)
ADRB1 (source: Drug Bank)
DRD1 (source: Drug Bank)
DRD2 (source: Drug Bank)
DRD3 (source: Drug Bank)
DRD4 (source: Drug Bank)
HRH1 (source: Drug Bank)
HTR1A (source: Drug Bank)
HTR1D (source: Drug Bank)
HTR2A (source: Drug Bank)
HTR2C (source: Drug Bank)

Drug Interactions

Drug Description
risperidone Decreases the effect of risperidone (source: Drug Bank)
risperidone Decreases the effect of risperidone (source: Drug Bank)
risperidone Risperidone increases the effect and toxicity of valproic acid (source: Drug Bank)
risperidone Possible antagonism of action (source: Drug Bank)
risperidone Possible antagonism of action (source: Drug Bank)
risperidone The SSRI increases the effect and toxicity of risperidone (source: Drug Bank)
risperidone The SSRI, fluoxetine, increases the effect and toxicity of risperidone. (source: Drug Bank)
risperidone Possible antagonism of action (source: Drug Bank)
risperidone Possible antagonism of action (source: Drug Bank)
risperidone Increased risk of extrapyramidal symptoms (source: Drug Bank)
risperidone Increased risk of extrapyramidal symptoms (source: Drug Bank)
risperidone Increases the level of risperidone (source: Drug Bank)
risperidone Increases the level of risperidone (source: Drug Bank)
risperidone Paliperidone is the active metabolite of risperidone, 9-OH-risperidone. Concomitant therapy may increase the adverse effects of paliperidone due to additive paliperidone exposure. Consider alternate therapy. (source: Drug Bank)
risperidone The SSRI increases the effect and toxicity of risperidone (source: Drug Bank)
risperidone The SSRI, paroxetine, increases the effect and toxicity of risperidone. (source: Drug Bank)
risperidone The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Risperidone, 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)
risperidone The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Risperidone, 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)
risperidone Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
risperidone Terbinafine may reduce the metabolism and clearance of Risperidone. Consider alternate therapy or monitor for therapeutic/adverse effects of Risperidone if Terbinafine is initiated, discontinued or dose changed. (source: Drug Bank)
risperidone May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. (source: Drug Bank)
risperidone 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)
risperidone 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)
risperidone 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)
risperidone The 2D6 inhibitor, Trazodone, may increase the efficacy of Risperidone by decreasing Risperidone metabolism and clearance. Monitor for changes in Risperidone efficacy if Trazodone is initiated, discontinued or dose changed. (source: Drug Bank)
risperidone The 2D6 inhibitor, Trazodone, may increase the efficacy of Risperidone by decreasing Risperidone metabolism and clearance. Monitor for changes in Risperidone efficacy if Trazodone is initiated, discontinued or dose changed. (source: Drug Bank)
risperidone Trimethobenzamide and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
risperidone Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank)
risperidone Triprolidine and Risperidone, 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)
risperidone Triprolidine and Risperidone, 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)
risperidone Trospium and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
risperidone 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)
risperidone 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)
risperidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank)
risperidone 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 risperidone: 110

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Effect of risperidone metabolism and P-glycoprotein gene polymorphism on QT interval in patients with schizophrenia. The pharmacogenomics journal. 2014. Suzuki Y, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effect of polymorphisms on the pharmacokinetics, pharmacodynamics, and safety of risperidone in healthy volunteers. Human psychopharmacology. 2014. Cabaleiro Teresa, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Risperidone metabolic ratio as a biomarker of individual CYP2D6 genotype in schizophrenic patients. European journal of clinical pharmacology. 2014. Mannheimer Buster, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
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
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Resolution of a clinical AmpliChip CYP450 Test™ no call: discovery and characterization of novel CYP2D6*1 haplotypes. Pharmacogenomics. 2014. Gaedigk Andrea, et al. PubMed
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 CA VA No VIP available No VIP available
Effect of CYP2D6 on risperidone pharmacokinetics and extrapyramidal symptoms in healthy volunteers: results from a pharmacogenetic clinical trial. Pharmacogenomics. 2014. Gassó Patricia, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP2D6 poor metabolizer status might be associated with better response to risperidone treatment. Pharmacogenetics and genomics. 2013. Almoguera Berta, 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
Role of ethnicity in antipsychotic-induced weight gain and tardive dyskinesia: genes or environment?. Pharmacogenomics. 2013. Chan Lai Fong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The effect of the Taq1A variant in the dopamine D2 receptor gene and common CYP2D6 alleles on prolactin levels in risperidone-treated boys. Pharmacogenetics and genomics. 2013. Roke Yvette, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers. Pharmacogenomics. 2013. López-Rodríguez Rosario, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genotypic variation in the SV2C gene impacts response to atypical antipsychotics the CATIE Study. Schizophrenia research. 2013. Ramsey Timothy L, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic study on risperidone long-acting injection: influence of cytochrome P450 2D6 and pregnane X receptor on risperidone exposure and drug-induced side-effects. Journal of clinical psychopharmacology. 2013. Choong Eva, 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 CA VA No VIP available No VIP available
Histamine H4 receptor polymorphism: a potential predictor of risperidone efficacy. Journal of clinical psychopharmacology. 2013. Wei Zhiyun, 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 of clinical response to risperidone. Pharmacogenomics. 2013. Llerena Adrián, 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
Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association between a COMT polymorphism and clinical response to risperidone treatment: a pharmacogenetic study. Psychiatric genetics. 2012. Zhao Qing-Zhu, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
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
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Targeted pharmacogenetic analysis of antipsychotic response in the CATIE study. Pharmacogenomics. 2012. Liu Qian, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A pharmacogenetic study of risperidone on histamine H3 receptor gene (HRH3) in Chinese Han schizophrenia patients. Journal of psychopharmacology (Oxford, England). 2012. Wei Zhiyun, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Case-control association study for 10 genes in patients with schizophrenia: influence of 5HTR1A variation rs10042486 on schizophrenia and response to antipsychotics. European archives of psychiatry and clinical neuroscience. 2012. Crisafulli Concetta, 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
Genetic association study between antipsychotic-induced weight gain and the melanocortin-4 receptor gene. The pharmacogenomics journal. 2012. Chowdhury N I, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of common genetic variants with risperidone adverse events in a Spanish schizophrenic population. The pharmacogenomics journal. 2012. Almoguera B, 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
Inter-individual variability of in vivo CYP2D6 activity in different genotypes. Drug metabolism and pharmacokinetics. 2012. Chiba Koji, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Relevance of CYP2D6 variability in first-episode schizophrenia patients treated with risperidone. Neuro endocrinology letters. 2012. Barteček Richard, 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
Pharmacogenetic testing to predict antipsychotic-induced weight gain: a systematic review. Pharmacogenomics. 2011. Risselada Arne 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
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
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
Gene expression in blood is associated with risperidone response in children with autism spectrum disorders. The pharmacogenomics journal. 2011. Lit L, 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
Association study of MDR1 and 5-HT2C genetic polymorphisms and antipsychotic-induced metabolic disturbances in female patients with schizophrenia. The pharmacogenomics journal. 2011. Kuzman M R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Risperidone-induced weight gain in referred children with autism spectrum disorders is associated with a common polymorphism in the 5-hydroxytryptamine 2C receptor gene. Journal of child and adolescent psychopharmacology. 2010. Hoekstra Pieter J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
KCNH2 pharmacogenomics summary. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Intuitive pharmacogenetics: spontaneous risperidone dosage is related to CYP2D6, CYP3A5 and ABCB1 genotypes. The pharmacogenomics journal. 2010. Mas S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Polymorphisms of the HTR2C gene and antipsychotic-induced weight gain: an update and meta-analysis. Pharmacogenomics. 2010. Sicard Michelle N, 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
Genome-wide association study of antipsychotic-induced QTc interval prolongation. The pharmacogenomics journal. 2010. Aberg K, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetics of risperidone therapy in autism: association analysis of eight candidate genes with drug efficacy and adverse drug reactions. The pharmacogenomics journal. 2010. Correia C T, 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 No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
DRD2 promoter region variation predicts antipsychotic-induced weight gain in first episode schizophrenia. Pharmacogenetics and genomics. 2010. Lencz Todd, 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
Gene-gene interactions of the INSIG1 and INSIG2 in metabolic syndrome in schizophrenic patients treated with atypical antipsychotics. The pharmacogenomics journal. 2010. Liou Y-J, 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 No Variant Annotation available No VIP available No VIP available
PharmGKB summary: dopamine receptor D2. Pharmacogenetics and genomics. 2010. Mi Huaiyu, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association between HTR2C gene polymorphisms and the metabolic syndrome in patients using antipsychotics: a replication study. The pharmacogenomics journal. 2010. Risselada A J, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Systematic analysis of dopamine receptor genes (DRD1-DRD5) in antipsychotic-induced weight gain. The pharmacogenomics journal. 2010. Müller D J, 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 No Variant Annotation available No VIP available No VIP available
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
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Dopamine receptor D2 gene is associated with weight gain in schizophrenic patients under long-term atypical antipsychotic treatment. Pharmacogenetics and genomics. 2010. Hong Chen-Jee, 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
HTR2C promoter polymorphisms are associated with risperidone efficacy in Chinese female patients. Pharmacogenomics. 2010. Liu Bao-Cheng, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Serotonin transporter polymorphisms and early response to antipsychotic treatment in first episode of psychosis. Psychiatry research. 2010. Vázquez-Bourgon Javier, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Leptin gene -2548G/A variants predict risperidone-associated weight gain in children and adolescents. Psychiatric genetics. 2009. Calarge Chadi A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A common variant in DRD3 gene is associated with risperidone-induced extrapyramidal symptoms. The pharmacogenomics journal. 2009. Gassó P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of the glutamate transporter gene SLC1A1 with atypical antipsychotics-induced obsessive-compulsive symptoms. Archives of general psychiatry. 2009. Kwon Jun Soo, 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
Predicting age-specific dosing of antipsychotics. Clinical pharmacology and therapeutics. 2009. Uchida H, 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
Apolipoprotein-E gene variants associated with cardiovascular risk factors in antipsychotic recipients. European psychiatry : the journal of the Association of European Psychiatrists. 2009. Clark D, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Candidate-gene association analysis of response to risperidone in African-American and white patients with schizophrenia. The pharmacogenomics journal. 2009. Fijal B 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
Genetic polymorphisms in dopamine- and serotonin-related genes and treatment responses to risperidone and perospirone. Psychiatry investigation. 2009. Tsutsumi Atsushi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Cytochrome P450 2D6. Pharmacogenetics and genomics. 2009. Owen Ryan P, 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 CA VA No VIP available No VIP available
Delusion symptoms and response to antipsychotic treatment are associated with the 5-HT2A receptor polymorphism (102T/C) in Alzheimer's disease: a 3-year follow-up longitudinal study. Journal of Alzheimer's disease : JAD. 2009. Angelucci Francesco, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Variants of the dopamine D2 receptor gene and risperidone-induced hyperprolactinemia in children and adolescents. Pharmacogenetics and genomics. 2009. Calarge Chadi 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
CYP2D6 genotyping for psychiatric patients treated with risperidone: considerations for cost-effectiveness studies. Pharmacogenomics. 2009. Rodríguez-Antona Cristina, 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
Further evidence for association of the RGS2 gene with antipsychotic-induced parkinsonism: protective role of a functional polymorphism in the 3'-untranslated region. The pharmacogenomics journal. 2009. Greenbaum L, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available 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
Association studies of catechol-O-methyltransferase (COMT) gene with schizophrenia and response to antipsychotic treatment. Pharmacogenomics. 2009. Gupta Meenal, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia: a replication study. Journal of clinical psychopharmacology. 2009. Mulder Hans, 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
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
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 VA No VIP available No VIP available
The --1019 C/G polymorphism of the 5-HT(1)A receptor gene is associated with negative symptom response to risperidone treatment in schizophrenia patients. Journal of psychopharmacology (Oxford, England). 2008. Wang L, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia. Pharmacogenomics. 2008. Ikeda Masashi, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Gene polymorphism influencing treatment response in psychotic patients in a naturalistic setting. Journal of psychiatric research. 2008. Alenius Malin, 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
Association between a polymorphism of the HTR3A gene and therapeutic response to risperidone treatment in drug-naive Chinese schizophrenia patients. Pharmacogenetics and genomics. 2008. Gu Bo, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association between dopamine-related polymorphisms and plasma concentrations of prolactin during risperidone treatment in schizophrenic patients. Progress in neuro-psychopharmacology & biological psychiatry. 2008. Yasui-Furukori Norio, 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
Semi-quantitative CYP2D6 gene doses in relation to metabolic ratios of psychotropics. European journal of clinical pharmacology. 2008. Hinrichs John W J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
RGS4 polymorphisms predict clinical manifestations and responses to risperidone treatment in patients with schizophrenia. Journal of clinical psychopharmacology. 2008. Lane Hsien-Yuan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Ethnic stratification of the association of RGS4 variants with antipsychotic treatment response in schizophrenia. Biological psychiatry. 2008. Campbell Daniel B, 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
Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. Journal of clinical pharmacology. 2008. Kim Kyoung-Ah, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Serum prolactin levels, plasma risperidone levels, polymorphism of cytochrome P450 2D6 and clinical response in patients with schizophrenia. Journal of psychopharmacology (Oxford, England). 2007. Wang Lei, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
HTR2C haplotypes and antipsychotics-induced weight gain: X-linked multimarker analysis. Human psychopharmacology. 2007. De Luca Vincenzo, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA 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 VA No VIP available No VIP available
The association between HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia. Journal of clinical psychopharmacology. 2007. Mulder Hans, 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
Association of the dopamine receptor interacting protein gene, NEF3, with early response to antipsychotic medication. The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 2007. Strous Rael D, 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
Physiogenomic comparison of weight profiles of olanzapine- and risperidone-treated patients. Molecular psychiatry. 2007. Ruaño 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
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
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 ABCB1 gene are associated with the therapeutic response to risperidone in Chinese schizophrenia patients. Pharmacogenomics. 2006. Xing Qinghe, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacokinetics and bioequivalence evaluation of risperidone in healthy male subjects with different CYP2D6 genotypes. Archives of pharmacal research. 2006. Cho Hea-Young, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Risperidone-related weight gain: genetic and nongenetic predictors. Journal of clinical psychopharmacology. 2006. Lane Hsien-Yuan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA 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 VA No VIP available No VIP available
Risperidone plasma levels, clinical response and side-effects. European archives of psychiatry and clinical neuroscience. 2005. Riedel Michael, 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 No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition. Clinical pharmacology and therapeutics. 2005. Nakagami Taku, 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
Metabolic ratios of psychotropics as indication of cytochrome P450 2D6/2C19 genotype. Therapeutic drug monitoring. 2005. van der Weide Jan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Prediction of response to risperidone treatment with respect to plasma concencentrations of risperidone, catecholamine metabolites, and polymorphism of cytochrome P450 2D6. International clinical psychopharmacology. 2005. Kakihara Shingo, 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
Prolactin levels in antipsychotic treatment of patients with schizophrenia carrying the DRD2*A1 allele. The British journal of psychiatry : the journal of mental science. 2004. Young Ross McD, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
QTc interval, CYP2D6 and CYP2C9 genotypes and risperidone plasma concentrations. Journal of psychopharmacology (Oxford, England). 2004. Llerena Adrián, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effects of various factors on steady-state plasma concentrations of risperidone and 9-hydroxyrisperidone: lack of impact of MDR-1 genotypes. British journal of clinical pharmacology. 2004. Yasui-Furukori Norio, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone. The pharmacogenomics journal. 2003. Yamanouchi Y, 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
Association of risperidone treatment response with a polymorphism in the 5-HT(2A) receptor gene. The American journal of psychiatry. 2002. Lane Hsien-Yuan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. European journal of pharmacology. 2002. Kongsamut Sathapana, 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
Cytochrome P450 2D6 deficiency and its clinical relevance in a patient treated with risperidone. Pharmacopsychiatry. 2002. Köhnke M D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
The effect of fluoxetine on the pharmacokinetics and safety of risperidone in psychotic patients. Pharmacopsychiatry. 2002. Bondolfi G, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Risperidone metabolism in relation to CYP2D6*10 allele in Korean schizophrenic patients. European journal of clinical pharmacology. 2001. Roh H K, 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 No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Science, medicine, and the future: Pharmacogenetics. BMJ (Clinical research ed.). 2000. Wolf C R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology. 1999. Scordo M G, 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
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Selective serotonin reuptake inhibitors and CNS drug interactions. A critical review of the evidence. Clinical pharmacokinetics. 1997. Sproule B 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
Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Clinical pharmacology and therapeutics. 1993. Huang M L, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0904-5973-61
DrugBank:
DB00734
ChEBI:
8871
KEGG Drug:
D00426
PubChem Compound:
5073
PubChem Substance:
46505850
7847492
IUPHAR Ligand:
96
Drugs Product Database (DPD):
2247705
ChemSpider:
4895
Therapeutic Targets Database:
DAP000003
FDA Drug Label at DailyMed:
1c572c5b-24f6-46c6-bdd2-6774ebefbb42

Clinical Trials

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

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