Identification
- Summary
Risperidone is a second-generation antipsychotic medication used to treat a number of mental health disorders including schizophrenia, bipolar mania, psychosis, or as an adjunct in severe depression.
- Brand Names
- Perseris, Risperdal, Rykindo, Uzedy
- Generic Name
- Risperidone
- DrugBank Accession Number
- DB00734
- Background
Risperidone is a second-generation antipsychotic (SGA) medication used in the treatment of a number of mood and mental health conditions including schizophrenia and bipolar disorder.16 It is one of the most widely used SGAs. Paliperidone, another commonly used SGA, is the primary active metabolite of risperidone (i.e. 9-hydroxyrisperidone).16
Schizophrenia and various mood disorders are thought to be caused by an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively. Risperidone is thought to reduce this overactivity through inhibition of dopaminergic D2 receptors and serotonergic 5-HT2A receptors in the brain.16
Risperidone binds with a very high affinity to 5-HT2A receptors, approximately 10-20 fold greater than the drug's binding affinity to D2 receptors, and carries lesser activity at several off-targets which may responsible for some of its undesirable effects.16
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Risperidone (DB00734)
- Weight
- Average: 410.4845
Monoisotopic: 410.211804333 - Chemical Formula
- C23H27FN4O2
- Synonyms
- Risperidona
- Rispéridone
- Risperidone
- Risperidonum
- External IDs
- R-64,766
- R-64766
- RCN-3028
- RCN3028
Pharmacology
- Indication
Risperidone is indicated for the treatment of schizophrenia 16,20,21 and irritability associated with autistic disorder.16 It is also indicated as monotherapy, or adjunctly with lithium or valproic acid, for the treatment of acute mania or mixed episodes associated with bipolar I disorder.16,20
Risperidone is additionally indicated in Canada for the short-term symptomatic management of aggression or psychotic symptoms in patients with severe dementia of the Alzheimer type unresponsive to nonpharmacological approaches.19
Risperidone is also used off-label for a number of conditions including as an adjunct to antidepressants in treatment-resistant depression.11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute mania •••••••••••• Adjunct therapy in treatment of Acute mania •••••••••••• Adjunct therapy in treatment of Acute mania •••••••••••• Treatment of Irritability •••••••••••• ••••••••• ••••••• ••••••• •••••• •••••••••••••• Treatment of Mixed manic depressive episode •••••••••••• - Contraindications & Blackbox Warnings
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The primary action of risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders.3,4
Risperidone has a high binding affinity for serotonergic 5-HT2A receptors when compared to dopaminergic D2 receptors in the brain.2,3 Risperidone binds to D2 receptors with a lower affinity than first-generation antipsychotic drugs, which bind with very high affinity. A reduction in extrapyramidal symptoms with risperidone, when compared to its predecessors, is likely a result of its moderate affinity for dopaminergic D2 receptors.7,5
- Mechanism of action
Though its precise mechanism of action is not fully understood, current focus is on the ability of risperidone to inhibit the D2 dopaminergic receptors and 5-HT2A serotonergic receptors in the brain. Schizophrenia is thought to result from an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively.3,4,5
D2 dopaminergic receptors are transiently inhibited by risperidone, reducing dopaminergic neurotransmission, therefore decreasing positive symptoms of schizophrenia, such as delusions and hallucinations.14 Risperidone binds transiently and with loose affinity to the dopaminergic D2 receptor, with an ideal receptor occupancy of 60-70% for optimal effect.7,10 Rapid dissociation of risperidone from the D2 receptors contributes to decreased risk of extrapyramidal symptoms (EPS), which occur with permanent and high occupancy blockade of D2 dopaminergic receptors.6,7 Low-affinity binding and rapid dissociation from the D2 receptor distinguish risperidone from the traditional antipsychotic drugs. A higher occupancy rate of D2 receptors is said to increase the risk of extrapyramidal symptoms and is therefore to be avoided.6,7,8
Increased serotonergic mesocortical activity in schizophrenia results in negative symptoms, such as depression and decreased motivation. The high-affinity binding of risperidone to 5-HT2A receptors leads to a decrease in serotonergic activity. In addition, 5-HT2A receptor blockade results in decreased risk of extrapyramidal symptoms, likely by increasing dopamine release from the frontal cortex, and not the nigrostriatal tract. Dopamine level is therefore not completely inhibited.5,7 Through the above mechanisms, both serotonergic and D2 blockade by risperidone are thought to synergistically work to decrease the risk of extrapyramidal symptoms.
Risperidone has also been said to be an antagonist of alpha-1 (α1), alpha-2 (α2), and histamine (H1) receptors.13 Blockade of these receptors is thought to improve symptoms of schizophrenia, however the exact mechanism of action on these receptors is not fully understood at this time.16
Target Actions Organism A5-hydroxytryptamine receptor 2A antagonistHumans ADopamine D2 receptor antagonistHumans UAlpha-1B adrenergic receptor antagonistHumans UAlpha-2B adrenergic receptor antagonistHumans UAlpha-1A adrenergic receptor antagonistHumans UAlpha-2C adrenergic receptor antagonistHumans UHistamine H1 receptor antagonistHumans U5-hydroxytryptamine receptor 2C antagonistHumans U5-hydroxytryptamine receptor 1D antagonistHumans U5-hydroxytryptamine receptor 1A antagonistHumans U5-hydroxytryptamine receptor 7 antagonistHumans UD(2L) dopamine receptor antagonistHumans UDopamine D1 receptor antagonistHumans - 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.16
- Volume of distribution
The volume of distribution of risperidone is approximately 1 to 2 L/kg.16
- Protein binding
Risperidone and its active metabolite, 9-hydroxyrisperidone, are ~88% and ~77% protein-bound in human plasma, respectively.9,16 They each bind to both serum albumin and alpha-1-acid glycoprotein.16
- Metabolism
Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone (i.e. paliperidone), which has approximately the same receptor binding affinity as risperidone.6,9 Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase.7,9 Risperidone also undergoes N-dealkylation to a lesser extent.7,9
Hover over products below to view reaction partners
- 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 are prolonged compared to young healthy subjects.9,15
- Half-life
3 hours in extensive metabolizers9 Up to 20 hours in poor metabolizers9
- Clearance
Risperidone is cleared by the kidneys. Clearance is decreased in the elderly and those with a creatinine clearance (ClCr) between 15-59 mL/min, in whom clearance is decreased by approximately 60%.15
- Adverse Effects
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Symptoms of overdose include lethargy, dystonia/spasm, tachycardia, bradycardia, and seizures. LD50=57.7 mg/kg (rat, oral) and 34 mg/kg (rat, intravenous).5,6,7
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Risperidone is combined with 1,2-Benzodiazepine. Abaloparatide Abaloparatide may increase the hypotensive activities of Risperidone. Abametapir The serum concentration of Risperidone can be increased when it is combined with Abametapir. Abatacept The metabolism of Risperidone can be increased when combined with Abatacept. Abiraterone The metabolism of Risperidone can be decreased when combined with Abiraterone. - Food Interactions
- Take with or without food. Food does not affect the rate or extent of absorption.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Risperidone tartrate 0S6B72E3LK 666179-92-6 KSWIOGDSXUFKOC-LREBCSMRSA-N - Product Images
- International/Other Brands
- Risperidal M-Tab (Janssen) / Risperin (Gador) / Rispolept / Rispolin / Sequinan
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Risperidone Tablet 3 mg Oral Actavis Pharma Company 2006-07-05 2018-06-26 Canada 
Act Risperidone Tablet 0.5 mg Oral Actavis Pharma Company 2006-07-05 2018-06-26 Canada Act Risperidone Tablet 2 mg Oral Actavis Pharma Company 2006-07-05 2018-06-26 Canada Act Risperidone Tablet 0.25 mg Oral Actavis Pharma Company 2006-07-05 2018-06-26 Canada Act Risperidone Tablet 4 mg Oral Actavis Pharma Company 2006-07-05 2018-06-26 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ag-risperidone Tablet 3 mg Oral Angita Pharma Inc. 2018-09-06 Not applicable Canada Ag-risperidone Tablet 0.5 mg Oral Angita Pharma Inc. 2018-09-06 Not applicable Canada Ag-risperidone Tablet 2 mg Oral Angita Pharma Inc. 2018-09-06 Not applicable Canada Ag-risperidone Tablet 0.25 mg Oral Angita Pharma Inc. 2018-09-06 Not applicable Canada Ag-risperidone Tablet 4 mg Oral Angita Pharma Inc. 2018-09-06 Not applicable Canada
Categories
- ATC Codes
- N05AX08 — Risperidone
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents that produce hypertension
- Agents that reduce seizure threshold
- Antidepressive Agents
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Histamine Antagonists
- Histamine H1 Antagonists
- Hyperglycemia-Associated Agents
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- P-glycoprotein substrates
- Potential QTc-Prolonging Agents
- Psycholeptics
- Psychotropic Drugs
- Pyrimidines
- Pyrimidinones
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Antagonists
- Serotonin 5-HT1A Receptor Antagonists
- Serotonin 5-HT1D Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as pyridopyrimidines. These are compounds containing a pyridopyrimidine, which consists of a pyridine fused to a pyrimidine. Pyridine is 6-membered ring consisting of five carbon atoms and a nitrogen atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridopyrimidines
- Sub Class
- Not Available
- Direct Parent
- Pyridopyrimidines
- Alternative Parents
- Benzisoxazoles / Pyrimidones / Aralkylamines / Pyridines and derivatives / Piperidines / Aryl fluorides / Benzenoids / Heteroaromatic compounds / Isoxazoles / Trialkylamines show 8 more
- Substituents
- Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Benzisoxazole / Heteroaromatic compound show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organofluorine compound, pyridopyrimidine, 1,2-benzoxazoles, heteroarylpiperidine (CHEBI:8871)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- L6UH7ZF8HC
- CAS number
- 106266-06-2
- InChI Key
- RAPZEAPATHNIPO-UHFFFAOYSA-N
- InChI
- InChI=1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3
- IUPAC Name
- 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
- SMILES
- CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCCC2=N1
References
- Synthesis Reference
- US4804663
- General References
- Altschuler EL, Kast RE: The atypical antipsychotic agents ziprasidone [correction of zisprasidone], risperdone and olanzapine as treatment for and prophylaxis against progressive multifocal leukoencephalopathy. Med Hypotheses. 2005;65(3):585-6. [Article]
- Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. doi: 10.1592/phco.29.1.64. [Article]
- Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [Article]
- Kemp DE, Canan F, Goldstein BI, McIntyre RS: Long-acting risperidone: a review of its role in the treatment of bipolar disorder. Adv Ther. 2009 Jun;26(6):588-99. doi: 10.1007/s12325-009-0039-0. Epub 2009 Jun 26. [Article]
- Szarfman A, Tonning JM, Levine JG, Doraiswamy PM: Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy. 2006 Jun;26(6):748-58. [Article]
- Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
- Yamanouchi Y, Iwata N, Suzuki T, Kitajima T, Ikeda M, Ozaki N: Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone. Pharmacogenomics J. 2003;3(6):356-61. [Article]
- Acri AA, Henretig FM: Effects of risperidone in overdose. Am J Emerg Med. 1998 Sep;16(5):498-501. [Article]
- Mannens G, Meuldermans W, Snoeck E, Heykants J: Plasma protein binding of risperidone and its distribution in blood. Psychopharmacology (Berl). 1994 May;114(4):566-72. [Article]
- Hall H, Halldin C, Nyberg S, Farde L, Sedvall G: Effect of clozapine and risperidone on 5-HT2 and D2-dopamine receptor binding in the post-mortem human brain. An autoradiographic study. Eur Neuropsychopharmacol. 1995 Mar;5(1):19-25. [Article]
- Kennedy SH, Lam RW, McIntyre RS, Tourjman SV, Bhat V, Blier P, Hasnain M, Jollant F, Levitt AJ, MacQueen GM, McInerney SJ, McIntosh D, Milev RV, Muller DJ, Parikh SV, Pearson NL, Ravindran AV, Uher R: Canadian Network for Mood and Anxiety Treatments (CANMAT) 2016 Clinical Guidelines for the Management of Adults with Major Depressive Disorder: Section 3. Pharmacological Treatments. Can J Psychiatry. 2016 Sep;61(9):540-60. doi: 10.1177/0706743716659417. Epub 2016 Aug 2. [Article]
- Ejsing TB, Pedersen AD, Linnet K: P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments. Hum Psychopharmacol. 2005 Oct;20(7):493-500. doi: 10.1002/hup.720. [Article]
- Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
- McEvoy JP: Efficacy of risperidone on positive features of schizophrenia. J Clin Psychiatry. 1994 May;55 Suppl:18-21. [Article]
- Pharmacokinetics of Risperidone: Clinical Summary [Link]
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
- FDA Approved Drug Products: Risperdal Consta (risperidone) long-acting intramuscular injection [Link]
- FDA Approved Drug Products: Perseris (risperidone) extended-release suspension for subcutaneous injection [Link]
- Health Canada Product Monograph: Risperdal (risperidone) oral tablets [Link]
- FDA Approved Drug Products: RYKINDO (risperidone) for extended-release injectable suspension, for intramuscular use [Link]
- FDA Approved Drug Products: UZEDY (risperidone) extended-release injectable suspension, for subcutaneous use [Link]
- FDA Label - Risperidone [File]
- Health Canada Monograph - Risperidone [File]
- External Links
- Human Metabolome Database
- HMDB0005020
- KEGG Drug
- D00426
- PubChem Compound
- 5073
- PubChem Substance
- 46505850
- ChemSpider
- 4895
- BindingDB
- 50001885
- 35636
- ChEBI
- 8871
- ChEMBL
- CHEMBL85
- ZINC
- ZINC000000538312
- Therapeutic Targets Database
- DAP000003
- PharmGKB
- PA451257
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Risperidone
- FDA label
- Download (2.54 MB)
- MSDS
- Download (25.2 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Schizophrenia 1 4 Completed Not Available Schizoaffective Disorders / Schizophrenia 1 4 Completed Not Available Schizophrenia 1 4 Completed Basic Science Healthy Subjects (HS) / Schizophrenia 1 4 Completed Basic Science Schizophrenia Spectrum and Other Psychotic Disorders 1
Pharmacoeconomics
- Manufacturers
- Ortho mcneil janssen pharmaceuticals inc
- Ortho mcneil janssen pharmaceutical inc
- Apotex inc richmond hill
- Aurobindo pharma ltd
- Dr reddys laboratories ltd
- Precision dose inc
- Roxane laboratories inc
- Teva pharmaceuticals usa inc
- Wockhardt ltd
- Par pharmaceutical inc
- Ranbaxy laboratories inc
- Sandoz inc
- Zydus pharmaceuticals usa inc
- Actavis totowa llc
- Apotex inc
- Cadista pharmaceuticals inc
- Mylan pharmaceuticals inc
- Pliva hrvatska doo
- Ratiopharm
- Synthon pharmaceuticals inc
- Torrent pharmaceuticals ltd
- Vintage pharmaceuticals llc
- Watson laboratories inc
- West ward pharmaceuticals corp
- Packagers
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Apotex Inc.
- Apotheca Inc.
- Atlantic Biologicals Corporation
- Aurobindo Pharma Ltd.
- Barr Pharmaceuticals
- Cadila Healthcare Ltd.
- Cardinal Health
- Cobalt Pharmaceuticals Inc.
- Comprehensive Consultant Services Inc.
- Core Pharmaceuticals
- Dept Health Central Pharmacy
- DispenseXpress Inc.
- Doctor Reddys Laboratories Ltd.
- Greenstone LLC
- Hikma Pharmaceuticals
- Janssen-Ortho Inc.
- Lake Erie Medical and Surgical Supply
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- Nutritional Research Association Inc.
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Par Pharmaceuticals
- Patriot Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Physician Partners Ltd.
- Physicians Total Care Inc.
- Pliva Inc.
- Prepak Systems Inc.
- Qualitest
- Quality Care
- Ratiopharm Inc.
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Roxane Labs
- Sandoz
- Southwood Pharmaceuticals
- Stat Rx Usa
- Sun Pharmaceutical Industries Ltd.
- Teva Pharmaceutical Industries Ltd.
- Torrent Pharmaceuticals
- UDL Laboratories
- Va Cmop Dallas
- Vangard Labs Inc.
- Vintage Pharmaceuticals Inc.
- West-Ward Pharmaceuticals
- Wockhardt Ltd.
- Zydus Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral 0.50 mg Solution Oral 1.0 mg/ml Solution / drops Oral Tablet, coated Oral 4 mg Tablet, soluble Oral 0.5 mg Tablet, soluble Oral 2 mg Tablet Oral 3.000 mg Tablet, delayed release Oral 1 mg Tablet, delayed release Oral 2 mg Tablet, effervescent Solution Oral Tablet, film coated Oral Tablet, orally disintegrating Oral Tablet Injection, powder, for suspension, extended release Intramuscular 100 mg Injection, powder, for suspension, extended release Intramuscular 75 mg Injection, powder, for suspension, extended release; kit Subcutaneous 120 mg / syr Injection, powder, for suspension, extended release; kit Subcutaneous 90 mg / syr Kit Subcutaneous 120 mg/0.8mL Kit Subcutaneous 90 mg/0.6mL Tablet Oral 1.0 mg Tablet Oral 2.0 mg Tablet Oral 3.0 mg Tablet Oral 4.0 mg Tablet, orally disintegrating Oral 3 mg Tablet, orally disintegrating Oral 4 mg Solution Oral 0.100 g Tablet Oral 1.000 mg Syrup Oral Tablet, film coated Oral 0.50 mg Tablet Oral 1 MG Tablet, film coated Oral 2.00 mg Injection, powder, for suspension, extended release Parenteral 25 MG/2ML Injection, powder, for suspension, extended release Parenteral 37.5 MG/2ML Injection, powder, for suspension, extended release Parenteral 50 MG/2ML Solution Oral 100.000 mg Solution / drops Oral 1 MG/ML Tablet Oral 0.25 mg Tablet Oral 0.5 mg Tablet Oral 3 mg Tablet Oral 4 mg Tablet Oral 5 mg Solution Oral 100 mg Injection, powder, for solution Intramuscular Injection, powder, for suspension, extended release; kit Intramuscular 12.5 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 12.5 mg/2mL Injection, powder, for suspension, extended release; kit Intramuscular 25 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 25 mg/2mL Injection, powder, for suspension, extended release; kit Intramuscular 37.5 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 37.5 mg/2mL Injection, powder, for suspension, extended release; kit Intramuscular 50 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 50 mg/2mL Suspension Intramuscular 25.000 mg Injection, suspension, extended release Intramuscular 25 mg Injection, powder, for suspension, extended release Parenteral 25 mg Injection, powder, for suspension, extended release Intramuscular Injection Intramuscular Injection, suspension, extended release Intramuscular 37.5 mg Injection, powder, for suspension, extended release Parenteral 37.5 mg Injection, suspension, extended release Intramuscular 50 mg Injection, powder, for suspension, extended release Parenteral 50 mg Injection, powder, for solution Intramuscular 25 mg Injection, powder, for solution Intramuscular 37.5 mg Injection, powder, for suspension Intramuscular 37.5 mg Solution Oral 1 mg / mL Solution Oral 1 mg/ml Tablet, orally disintegrating Oral 0.5 mg Tablet, orally disintegrating Oral 1 mg Tablet, orally disintegrating Oral 2 mg Tablet, soluble Oral 4 mg Tablet Buccal; Oral 0.5 mg Tablet Oral 2 mg Tablet, film coated Oral 3 mg Injection, powder, for suspension Intramuscular 25 mg Tablet, soluble Buccal 1 mg Tablet, film coated Oral 0.5 MG Tablet, film coated Oral 1.0 MG Tablet, film coated Oral 2.0 MG Tablet, film coated Oral 4.0 MG Tablet, film coated Oral 6 MG Tablet, film coated Oral 0.25 MG Injection, powder, for suspension Parenteral 25 mg Tablet, film coated Oral 3.0 MG Injection, powder, for suspension Parenteral 37.5 mg Injection, powder, for suspension Parenteral 50 mg Tablet, film coated Oral 8 MG Film, soluble Oral Tablet, coated Oral 3 mg Tablet, soluble Oral 1 mg Solution Oral 1 mg/1mL Tablet Oral Tablet Oral .25 mg/1 Tablet Oral .5 mg/1 Tablet Oral 0.25 mg/1 Tablet Oral 0.5 mg/1 Tablet Oral 1 mg/1 Tablet Oral 2 mg/1 Tablet Oral 3 mg/1 Tablet Oral 4 mg/1 Tablet, coated Oral .25 mg/1 Tablet, coated Oral .5 mg/1 Tablet, coated Oral 1 mg/1 Tablet, coated Oral 2 mg/1 Tablet, coated Oral 3 mg/1 Tablet, coated Oral 4 mg/1 Tablet, film coated Oral 0.25 mg/1 Tablet, film coated Oral 0.5 mg/1 Tablet, film coated Oral 0.50 mg/1 Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 2 mg/1 Tablet, film coated Oral 3 mg/1 Tablet, film coated Oral 4 mg/1 Tablet, orally disintegrating Oral 0.25 mg/1 Tablet, orally disintegrating Oral 0.5 mg/1 Tablet, orally disintegrating Oral 1 mg/1 Tablet, orally disintegrating Oral 2 mg/1 Tablet, orally disintegrating Oral 3 mg/1 Tablet, orally disintegrating Oral 4 mg/1 Tablet, film coated Oral 1 mg Tablet, film coated Oral 2 MG Tablet, film coated Oral 4 MG Injection, powder, for suspension, extended release 25 MG Injection, powder, for suspension, extended release 37.5 MG Injection, powder, for suspension, extended release 50 MG Injection, powder, lyophilized, for suspension, extended release; kit Intramuscular 12.5 mg/2mL Injection, powder, lyophilized, for suspension, extended release; kit Intramuscular 25 mg/2mL Injection, powder, lyophilized, for suspension, extended release; kit Intramuscular 37.5 mg/2mL Injection, powder, lyophilized, for suspension, extended release; kit Intramuscular 50 mg/2mL Solution Oral 0.1 g Solution Oral 1 mg Solution Oral 100000 mg Injection, suspension, extended release Subcutaneous 100 mg/0.28mL Injection, suspension, extended release Subcutaneous 125 mg/0.35mL Injection, suspension, extended release Subcutaneous 150 mg/0.42mL Injection, suspension, extended release Subcutaneous 200 mg/0.56mL Injection, suspension, extended release Subcutaneous 250 mg/0.7mL Injection, suspension, extended release Subcutaneous 50 mg/0.14mL Injection, suspension, extended release Subcutaneous 75 mg/0.21mL Tablet Oral 2.00 mg Capsule, delayed release Oral 3 mg Tablet, coated Oral 1 mg Tablet, coated Oral 2 mg - Prices
Unit description Cost Unit Risperdal consta 50 mg syr 592.93USD syringe Risperdal consta 37.5 mg syr 444.68USD syringe Risperdal consta 25 mg syr 296.46USD syringe Risperdal 1 mg/ml Solution 30ml Bottle 204.42USD bottle Risperdal M-TAB 28 1 mg Dispersible Tablet Box 196.08USD box Risperdal M-TAB 28 0.5 mg Dispersible Tablet Bottle 167.82USD bottle Risperidone 1 mg/ml Solution 30ml Bottle 158.66USD bottle Risperdal consta 12.5 mg syr 148.22USD syringe Risperdal m-tab 4 mg odt 18.55USD tablet Risperdal 4 mg tablet 16.47USD tablet Risperidone m-tab 4 mg odt 15.16USD tablet Risperdal m-tab 3 mg odt 13.81USD tablet Risperdal 3 mg tablet 11.45USD tablet Risperidone m-tab 3 mg odt 11.29USD tablet Risperdal m-tab 2 mg odt 10.95USD tablet Risperidone 4 mg tablet 9.0USD tablet Risperidone m-tab 2 mg odt 8.95USD tablet Risperdal 2 mg tablet 6.94USD tablet Risperdal m-tab 1 mg odt 6.73USD tablet Risperidone 3 mg tablet 6.63USD tablet Risperdal 1 mg tablet 6.12USD tablet Risperdal m-tab 0.5 mg odt 5.76USD tablet Risperidone 2 mg tablet 5.59USD tablet Risperidone m-tab 1 mg odt 5.5USD tablet Risperidone M-TAB 0.5 mg Dispersible Tablet 4.9USD dispersible tablet Risperidone m-tab 0.5 mg odt 4.71USD tablet Risperdal M-Tab 4 mg Disintegrating Tablet 4.6USD tablet Risperdal 0.25 mg tablet 4.56USD tablet Risperidone 0.25 mg odt 4.48USD tablet Risperdal 0.5 mg tablet 3.62USD tablet Risperdal M-Tab 3 mg Disintegrating Tablet 3.44USD tablet Risperidone 1 mg tablet 3.27USD tablet Risperidone 0.5 mg tablet 3.03USD tablet Apo-Risperidone 4 mg Tablet 2.53USD tablet Co Risperidone 4 mg Tablet 2.53USD tablet Mylan-Risperidone 4 mg Tablet 2.53USD tablet Novo-Risperidone 4 mg Tablet 2.53USD tablet Phl-Risperidone 4 mg Tablet 2.53USD tablet Pms-Risperidone 4 mg Tablet 2.53USD tablet Ran-Risperidone 4 mg Tablet 2.53USD tablet Ratio-Risperidone 4 mg Tablet 2.53USD tablet Rbx-Risperidone 4 mg Tablet 2.53USD tablet Sandoz Risperidone 4 mg Tablet 2.53USD tablet Risperdal M-Tab 2 mg Disintegrating Tablet 2.29USD tablet Apo-Risperidone 3 mg Tablet 1.9USD tablet Co Risperidone 3 mg Tablet 1.9USD tablet Mylan-Risperidone 3 mg Tablet 1.9USD tablet Novo-Risperidone 3 mg Tablet 1.9USD tablet Phl-Risperidone 3 mg Tablet 1.9USD tablet Pms-Risperidone 3 mg Tablet 1.9USD tablet Ran-Risperidone 3 mg Tablet 1.9USD tablet Ratio-Risperidone 3 mg Tablet 1.9USD tablet Rbx-Risperidone 3 mg Tablet 1.9USD tablet Sandoz Risperidone 3 mg Tablet 1.9USD tablet Risperidone 0.25 mg tablet 1.88USD tablet Apo-Risperidone 2 mg Tablet 1.26USD tablet Co Risperidone 2 mg Tablet 1.26USD tablet Mylan-Risperidone 2 mg Tablet 1.26USD tablet Novo-Risperidone 2 mg Tablet 1.26USD tablet Phl-Risperidone 2 mg Tablet 1.26USD tablet Pms-Risperidone 2 mg Tablet 1.26USD tablet Ran-Risperidone 2 mg Tablet 1.26USD tablet Ratio-Risperidone 2 mg Tablet 1.26USD tablet Rbx-Risperidone 2 mg Tablet 1.26USD tablet Sandoz Risperidone 2 mg Tablet 1.26USD tablet Risperdal M-Tab 1 mg Disintegrating Tablet 1.16USD tablet Risperdal M-Tab 0.5 mg Disintegrating Tablet 0.84USD tablet Apo-Risperidone 1 mg Tablet 0.63USD tablet Co Risperidone 1 mg Tablet 0.63USD tablet Mylan-Risperidone 1 mg Tablet 0.63USD tablet Novo-Risperidone 1 mg Tablet 0.63USD tablet Phl-Risperidone 1 mg Tablet 0.63USD tablet Pms-Risperidone 1 mg Tablet 0.63USD tablet Ran-Risperidone 1 mg Tablet 0.63USD tablet Ratio-Risperidone 1 mg Tablet 0.63USD tablet Rbx-Risperidone 1 mg Tablet 0.63USD tablet Sandoz Risperidone 1 mg Tablet 0.63USD tablet Apo-Risperidone 0.5 mg Tablet 0.46USD tablet Co Risperidone 0.5 mg Tablet 0.46USD tablet Mylan-Risperidone 0.5 mg Tablet 0.46USD tablet Novo-Risperidone 0.5 mg Tablet 0.46USD tablet Phl-Risperidone 0.5 mg Tablet 0.46USD tablet Pms-Risperidone 0.5 mg Tablet 0.46USD tablet Ran-Risperidone 0.5 mg Tablet 0.46USD tablet Ratio-Risperidone 0.5 mg Tablet 0.46USD tablet Rbx-Risperidone 0.5 mg Tablet 0.46USD tablet Sandoz Risperidone 0.5 mg Tablet 0.46USD tablet Apo-Risperidone 0.25 mg Tablet 0.27USD tablet Co Risperidone 0.25 mg Tablet 0.27USD tablet Mylan-Risperidone 0.25 mg Tablet 0.27USD tablet Novo-Risperidone 0.25 mg Tablet 0.27USD tablet Phl-Risperidone 0.25 mg Tablet 0.27USD tablet Pms-Risperidone 0.25 mg Tablet 0.27USD tablet Ran-Risperidone 0.25 mg Tablet 0.27USD tablet Ratio-Risperidone 0.25 mg Tablet 0.27USD tablet Rbx-Risperidone 0.25 mg Tablet 0.27USD tablet Sandoz Risperidone 0.25 mg Tablet 0.27USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6110921 No 2000-08-29 2013-11-19 US 
CA2406536 No 2009-12-22 2021-04-19 Canada CA2194564 No 1998-01-27 2015-07-04 Canada US6667061 Yes 2003-12-23 2020-11-25 US US5792477 Yes 1998-08-11 2017-11-02 US US5916598 Yes 1999-06-29 2017-11-02 US US6379703 Yes 2002-04-30 2019-06-30 US US6403114 Yes 2002-06-11 2017-11-02 US US6596316 Yes 2003-07-22 2019-06-30 US US6194006 Yes 2001-02-27 2019-06-30 US US6224905 Yes 2001-05-01 2017-12-10 US US9186413 No 2015-11-17 2028-02-13 US US10010612 No 2018-07-03 2028-02-13 US US9180197 No 2015-11-10 2028-02-13 US US9597402 No 2017-03-21 2026-09-26 US US10058554 No 2018-08-28 2026-09-26 US US10406160 No 2019-09-10 2026-06-26 US US10376590 No 2019-08-13 2028-02-13 US US11013809 No 2021-05-25 2028-02-13 US US11110093 No 2021-09-07 2026-11-05 US US10406161 No 2019-09-10 2032-04-10 US US10098882 No 2018-10-16 2032-04-10 US US9532991 No 2017-01-03 2032-04-10 US US9446135 No 2016-09-20 2032-04-10 US US11110094 No 2021-09-07 2032-04-10 US US9439905 No 2016-09-13 2025-01-12 US US8221778 No 2012-07-17 2027-11-12 US US8741327 No 2014-06-03 2027-11-12 US US9925268 No 2018-03-27 2025-01-12 US US10736965 No 2020-08-11 2025-01-12 US US8802127 No 2014-08-12 2025-01-12 US US9717799 No 2017-08-01 2025-01-12 US US9023897 No 2015-05-05 2033-04-05 US US9895447 No 2018-02-20 2025-01-12 US US11712475 No 2008-02-13 2028-02-13 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 170 PhysProp boiling point (°C) 442 Not Available water solubility 2.33 mg/mL Not Available - Predicted Properties
Property Value Source Water Solubility 0.171 mg/mL ALOGPS logP 3.27 ALOGPS logP 2.63 Chemaxon logS -3.4 ALOGPS pKa (Strongest Basic) 8.76 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 61.94 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 114.55 m3·mol-1 Chemaxon Polarizability 45.28 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9925 Caco-2 permeable - 0.5057 P-glycoprotein substrate Substrate 0.6163 P-glycoprotein inhibitor I Inhibitor 0.8564 P-glycoprotein inhibitor II Inhibitor 0.9361 Renal organic cation transporter Inhibitor 0.6491 CYP450 2C9 substrate Non-substrate 0.8235 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.7407 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.82 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8459 Ames test Non AMES toxic 0.5302 Carcinogenicity Non-carcinogens 0.8204 Biodegradation Not ready biodegradable 0.99 Rat acute toxicity 3.8290 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.65 hERG inhibition (predictor II) Inhibitor 0.8062
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 210.5043733 predictedDarkChem Lite v0.1.0 [M-H]- 198.82178 predictedDeepCCS 1.0 (2019) [M+H]+ 210.9869733 predictedDarkChem Lite v0.1.0 [M+H]+ 201.1798 predictedDeepCCS 1.0 (2019) [M+Na]+ 211.7954733 predictedDarkChem Lite v0.1.0 [M+Na]+ 208.26259 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Epinephrine binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Protein homodimerization activity
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- Molecular Weight
- 41906.38 Da
References
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
12. D(2L) dopamine receptor
Unknown
Antagonist
References
- Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Fang J, Bourin M, Baker GB: Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn Schmiedebergs Arch Pharmacol. 1999 Feb;359(2):147-51. [Article]
- Hendset M, Molden E, Refsum H, Hermann M: Impact of CYP2D6 genotype on steady-state serum concentrations of risperidone and 9-hydroxyrisperidone in patients using long-acting injectable risperidone. J Clin Psychopharmacol. 2009 Dec;29(6):537-41. doi: 10.1097/JCP.0b013e3181c17df0. [Article]
- Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: part II. Clin Pharmacokinet. 2009;48(12):761-804. doi: 10.2165/11318070-000000000-00000. [Article]
- Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I. Clin Pharmacokinet. 2009;48(11):689-723. doi: 10.2165/11318030-000000000-00000. [Article]
- Yasui-Furukori N, Hidestrand M, Spina E, Facciola G, Scordo MG, Tybring G: Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001 Oct;29(10):1263-8. [Article]
- Flockhart Table of Drug Interactions [Link]
- Source [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Fang J, Bourin M, Baker GB: Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn Schmiedebergs Arch Pharmacol. 1999 Feb;359(2):147-51. [Article]
- Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
- Prior TI, Baker GB: Interactions between the cytochrome P450 system and the second-generation antipsychotics. J Psychiatry Neurosci. 2003 Mar;28(2):99-112. [Article]
- Flockhart Table of Drug Interactions [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
- Gene Name
- ORM1
- Uniprot ID
- P02763
- Uniprot Name
- Alpha-1-acid glycoprotein 1
- Molecular Weight
- 23511.38 Da
References
- FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Saikachi H, Nakamura S: [Synthesis of the furan derivatives. XLIX. Wittig reaction of organosulfurphosphoranes with some aromatic aldehydes]. Yakugaku Zasshi. 1969 Oct;89(10):1446-56. [Article]
- Ejsing TB, Pedersen AD, Linnet K: P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments. Hum Psychopharmacol. 2005 Oct;20(7):493-500. doi: 10.1002/hup.720. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55