Risperidone – Wikipedia, the free encyclopedia

Posted: Published on December 13th, 2014

This post was added by Dr Simmons

Risperidone Systematic (IUPAC) name 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)- 1-piperidyl]ethyl]-3-methyl- 2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one Clinical data Trade names Risperdal,Risperdal Consta,Risperdal M-Tab,Risperdal Quicklets AHFS/Drugs.com monograph MedlinePlus a694015 Pregnancy cat. Legal status Routes Oral (tablets and liquid form), IM Pharmacokinetic data Bioavailability 70% (oral)[1] Metabolism Hepatic (CYP2D6 mediated to 9-hydroxyrisperidone)[1] Half-life 20 hours (Oral), 2.96 days (IM) [1] Excretion Urinary (70% (adults), 4.3% (children), 7.4% (adolescents)), faecal (14%) [1] Identifiers CAS number 106266-06-2Y ATC code N05AX08 PubChem CID 5073 IUPHAR ligand 96 DrugBank DB00734 ChemSpider 4895Y UNII L6UH7ZF8HCY KEGG D00426Y ChEBI CHEBI:8871Y ChEMBL CHEMBL85Y Chemical data Formula C23H27FN4O2 Mol. mass 410.485 g/mol Cc1c(c(=O)n2c(n1)CCCC2)CCN3CCC(CC3)c4c5ccc(cc5on4)F Y(what is this?)(verify)

Risperidone (// ri-SPAIR-i-dohn) (trade name Risperdal, and generics) is an antipsychotic drug mainly used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states of bipolar disorder, and irritability in people with autism.

Risperidone is a second-generation atypical antipsychotic.[2] It is a dopamine antagonist possessing anti-serotonergic, anti-adrenergic and anti-histaminergic properties.

Adverse effects of risperidone include significant weight gain and metabolic problems such as diabetes mellitus type 2,[3] as well as tardive dyskinesia and neuroleptic malignant syndrome. Risperidone and other antipsychotics also increase the risk of death in people with dementia.[4]

The drug was developed by Janssen-Cilag, subsidiary of Johnson & Johnson, from 1988 to 1992 as an improvement from the typical antipsychotic and first approved by the FDA in 1994.[5] Today many generic versions are available. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[6]

Risperidone is used for the treatment of schizophrenia, bipolar disorder also including behavior problems in autistic people.[7]

Risperidone is effective in treating the acute exacerbations of schizophrenia.[8][9]

Studies evaluating the utility of the oral form of risperidone for maintenance therapy have reached varying conclusions. A 2012 systematic review concluded that there is strong evidence that risperidone is more effective than all first generation antipsychotics other than haloperidol, but that evidence directly supporting its superiority to placebo is equivocal.[10] A 2011 review concluded that risperidone is more effective in relapse prevention than other first and second generation antipsychotics with the exception of olanzapine and clozapine.[11] A 2010 Cochrane review found a slight benefit during the first few weeks of treatment of schizophrenia but the article raised concerns regarding bias favoring risperidone.[12]

Long-acting injectable formulations of antipsychotic drugs provide improved compliance with therapy and reduce relapse rates relative to oral formulations.[13][14] The efficacy of risperidone long acting injection appears to be similar to that of long acting injectable forms of first generation antipsychotics.[15]

Second generation antipsychotics, including risperidone, are effective in the treatment of manic symptoms in acute manic or mixed exacerbations of bipolar disorder.[16][17][18] In children and adolescents, risperidone may be more effective than lithium or divalproex, but has more metabolic side effects.[19] As maintenance therapy, aripiprazole is effective for the prevention of manic episodes but not depression.[20] The long-acting injectable form of risperidone may be advantageous over long acting first generation antipsychotics, as it is better tolerated (fewer extrapyramidal effects) and because long acting injectable formulations of first generation antipsychotics may increase the risk of depression.[21]

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Risperidone - Wikipedia, the free encyclopedia

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