| 词条 | Risperidone | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 释义 |
| Watchedfields = changed | verifiedrevid = 464382756 | IUPAC_name = 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one | image = Risperidone.svg | width = 250px | image2 = Risperidone-3D-balls.png | width2 = 250px | pronounce = | tradename = Risperdal, others[1] | Drugs.com = {{drugs.com|monograph|risperidone}} | MedlinePlus = a694015 | pregnancy_AU = B3 | pregnancy_US = C | legal_AU = S4 | legal_US = Rx-only | legal_UK = POM | routes_of_administration = By mouth (tablets and liquid form), intramuscular injection | class = Atypical antipsychotic[2] | bioavailability = 70% (by mouth)[2] | metabolism = Liver (CYP2D6 mediated to 9-hydroxyrisperidone)[2] | elimination_half-life = 20 hours (by mouth), 3–6 days (IM)[2] | excretion = Urinary (70%) feces (14%)[2] | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 106266-06-2 | ATC_prefix = N05 | ATC_suffix = AX08 | PubChem = 5073 | IUPHAR_ligand = 96 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00734 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 4895 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = L6UH7ZF8HC | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00426 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 8871 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 85 | PDB_ligand = 8NU | C=23 | H=27 | F=1 | N=4 | O=2 | molecular_weight = 410.485 g/mol | smiles = Cc1c(c(=O)n2c(n1)CCCC2)CCN3CCC(CC3)c4c5ccc(cc5on4)F | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = RAPZEAPATHNIPO-UHFFFAOYSA-N |drug_name=|alt=|caption=|type=|legal_status=|licence_EU=|pregnancy_category=|licence_US=|legal_CA=Rx-only}}Risperidone, sold under the brand name Risperdal among others, is an antipsychotic.[1] It is used to treat schizophrenia, bipolar disorder, and irritability associated with autism.[1] It is taken either by mouth or by injection into a muscle.[1] The injectable version is long-acting and lasts for about two weeks.[2] Common side effects include movement problems, sleepiness, dizziness, trouble seeing, constipation, and increased weight.[1][3] Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and high blood sugar levels.[1][2] In older people with psychosis as a result of dementia, it may increase the risk of dying.[1] It is unclear if it is safe for use in pregnancy.[1] Risperidone is an atypical antipsychotic.[1] Its mechanism of action is not entirely clear, but is believed to be related to its action as a dopamine antagonist and serotonin antagonist.[1] Study of risperidone began in the late 1980s and it was approved for sale in the United States in 1993.[1][4] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[5] It is available as a generic medication.[2] The wholesale price in the developing world is between $US 0.01 and $US 0.60 per day as of 2014.[6] The cost for a typical month of medication in the United States is between $US 100-200 as of 2015.[2] In 2016, it was the 159th most prescribed medication in the United States, with more than 3 million prescriptions.[7] Medical usesRisperidone is mainly used for the treatment of schizophrenia, bipolar disorder, and irritability associated with autism.[8] SchizophreniaRisperidone is effective in treating the acute exacerbations of schizophrenia.[9][10] A 2013 study compared 15 antipsychotic drugs in treating schizophrenia. Risperidone was ranked fourth, 11% more effective than paliperidone (fifth), 20-23% more effective than haloperidol, quetiapine, and aripiprazole, and 36% less effective than clozapine (first).[9] Studies evaluating the utility of risperidone by mouth for maintenance therapy have reached varying conclusions. A 2012 systematic review concluded that evidence is strong that risperidone is more effective than all first-generation antipsychotics other than haloperidol, but that evidence directly supporting its superiority to placebo is equivocal.[11] 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.[12] A 2016 Cochrane review suggests that risperidone reduces the overall symptoms of schizophrenia, but firm conclusions are difficult to make due to very low-quality evidence. Data and information are scarce, poorly reported, and probably biased in favour of risperidone, with about half of the included trials developed by drug companies. The article raises concerns regarding the serious side effects of risperidone, such as parkinsonism.[13] A 2011 Cochrane review compared risperidone with other atypical antipsychotics such as olanzapine for schizophrenia:[14]
Long-acting injectable formulations of antipsychotic drugs provide improved compliance with therapy and reduce relapse rates relative to oral formulations.[15][16] The efficacy of risperidone long-acting injection appears to be similar to that of long acting injectable forms of first generation antipsychotics.[17] Bipolar disorderSecond-generation antipsychotics, including risperidone, are effective in the treatment of manic symptoms in acute manic or mixed exacerbations of bipolar disorder.[18][19][20] In children and adolescents, risperidone may be more effective than lithium or divalproex, but has more metabolic side effects.[21] As maintenance therapy, long-acting injectable risperidone is effective for the prevention of manic episodes but not depressive episodes.[22] 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.[23] AutismCompared to placebo, risperidone treatment reduces certain problematic behaviors in autistic children, including aggression toward others, self-injury, temper tantrums, and rapid mood changes. The evidence for its efficacy appears to be greater than that for alternative pharmacological treatments.[24] Weight gain is an important adverse effect.[25][26] Some authors recommend limiting the use of risperidone and aripiprazole to those with the most challenging behavioral disturbances in order to minimize the risk of drug-induced adverse effects.[27] Evidence for the efficacy of risperidone in autistic adolescents and young adults is less persuasive.[28] Other usesRisperidone has shown promise in treating therapy-resistant obsessive–compulsive disorder, when serotonin reuptake inhibitors are not sufficient.[29] Risperidone has not demonstrated a benefit in the treatment of eating disorders or personality disorders.[30] While antipsychotic medications such as risperidone have a slight benefit in people with dementia, they have been linked to higher incidences of death and stroke.[30] Because of this increased risk of death, treatment of dementia-related psychosis with risperidone is not FDA approved.[31] Adverse effects{{See also|List of adverse effects of risperidone}}Common side effects include movement problems, sleepiness, dizziness, trouble seeing, constipation, and increased weight.[1][3] Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and high blood sugar levels.[1][2] In older people with psychosis as a result of dementia, it may increase the risk of dying.[1] While atypical antipsychotics appear to have a lower rate of movement problems as compared to typical antipsychotics, risperidone has a high risk of movement problems among the atypicals.[32][33] Atypical antipsychotics however are associated with a greater amount of weight gain.[33] Drug interactions
DiscontinuationThe British National Formulary recommends a gradual withdrawal when discontinuing antipsychotic treatment to avoid acute withdrawal syndrome or rapid relapse.[35] Some have argued the additional somatic and psychiatric symptoms associated with dopaminergic super-sensitivity, including dyskinesia and acute psychosis, are common features of withdrawal in individuals treated with neuroleptics.[36][37][38][39] This has led some to suggest the withdrawal process might itself be schizomimetic, producing schizophrenia-like symptoms even in previously healthy patients, indicating a possible pharmacological origin of mental illness in a yet unknown percentage of patients currently and previously treated with antipsychotics. This question is unresolved, and remains a highly controversial issue among professionals in the medical and mental health communities, as well the public.[40] DementiaOlder people with dementia-related psychosis are at a higher risk of death if they take risperidone compared to those who do not. Most deaths are related to heart problems or infections.[41] PharmacologyPharmacodynamics{{See also|Atypical antipsychotic#Pharmacodynamics|Antipsychotic#Comparison of medications}}
Risperidone has been classified as a "qualitatively atypical" antipsychotic agent with a relatively low incidence of extrapyramidal side effects (when given at low doses) that has more pronounced serotonin antagonism than dopamine antagonism. Risperidone contains the functional groups of benzisoxazole and piperidine as part of its molecular structure. Although not a butyrophenone, it was developed with the structures of benperidol and ketanserin as a basis. It has actions at several 5-HT (serotonin) receptor subtypes. These are 5-HT2C, linked to weight gain, 5-HT2A, linked to its antipsychotic action and relief of some of the extrapyramidal side effects experienced with the typical neuroleptics.[44] It was recently found that D-amino acid oxidase, the enzyme that catalyses the breakdown of D-amino acids (e.g. D-alanine and D-serine — the neurotransmitters) is inhibited by risperidone.[45] Risperidone acts on the following receptors: Dopamine receptors: This drug is an antagonist of the D1 (D1, and D5) as well as the D2 family (D2, D3 and D4) receptors, with 70-fold selectivity for the D2 family. This drug has "tight binding" properties, which means it has a long half-life and like other antipsychotics, risperidone blocks the mesolimbic pathway, the prefrontal cortex limbic pathway, and the tuberoinfundibular pathway in the central nervous system. Risperidone may induce extrapyramidal side effects, akathisia and tremors, associated with diminished dopaminergic activity in the striatum. It can also cause sexual side effects, galactorrhoea, infertility, gynecomastia and, with chronic use reduced bone mineral density leading to breaks, all of which are associated with increased prolactin secretion.[44]Serotonin receptors: Its action at these receptors may be responsible for its lower extrapyramidal side effect liability (via the 5-HT2A/2C receptors) and improved negative symptom control compared to typical antipsychotics such as haloperidol for instance. Its antagonistic actions at the 5-HT2C receptor may account, in part, for its weight gain liability. Alpha α1 adrenergic receptors: This action accounts for its orthostatic hypotensive effects and perhaps some of the sedating effects of risperidone.[44]Alpha α2 adrenergic receptors: Perhaps greater positive, negative, affective and cognitive symptom control.[46]Histamine H1 receptors: effects on these receptors account for its sedation and reduction in vigilance. This may also lead to drowsiness and weight gain.[44]Though this medication possesses similar effects to other typical and atypical antipsychotics, it does not possess an affinity for the muscarinic acetylcholine receptors. In many respects, this medication can be useful as an "acetylcholine release-promoter" similar to gastrointestinal drugs such as metoclopramide and cisapride. PharmacokineticsRisperidone undergoes hepatic metabolism and renal excretion. Lower doses are recommended for patients with severe liver and kidney disease.[31] The active metabolite of risperidone, paliperidone, is also used as an antipsychotic.[47] Society and cultureRegulatory statusRisperidone was approved by the United States Food and Drug Administration (FDA) in 1993 for the treatment of schizophrenia.[48] In 2003, the FDA approved risperidone for the short-term treatment of the mixed and manic states associated with bipolar disorder. In 2006, the FDA approved risperidone for the treatment of irritability in autistic children and adolescents.[49] On August 22, 2007, risperidone was approved as the only drug agent available for treatment of schizophrenia in youths, ages 13–17; it was also approved that same day for treatment of bipolar disorder in youths and children, ages 10–17, joining lithium. The FDA's decision was based in part on a study of autistic people with severe and enduring problems of violent meltdowns, aggression, and self-injury; risperidone is not recommended for autistic people with mild aggression and explosive behavior without an enduring pattern.[50] AvailabilityJanssen's patent on risperidone expired on December 29, 2003, opening the market for cheaper generic versions from other companies, and Janssen's exclusive marketing rights expired on June 29, 2004 (the result of a pediatric extension). It is available under many brand names worldwide.[51] Risperidone is available as a tablet, an oral solution, and an ampule, which is a depot injection.[51] LawsuitsOn 11 April 2012, Johnson & Johnson (J&J) and its subsidiary Janssen Pharmaceuticals Inc. were fined $1.2 billion by Judge Timothy Davis Fox of the Sixth Division of the Sixth Judicial Circuit of the U.S. state of Arkansas.[52] The jury found the companies had downplayed multiple risks associated with risperidone (Risperdal). The verdict was later reversed by the Arkansas State Supreme court.[53] In August 2012, Johnson & Johnson agreed to pay $181 million to 36 U.S. states in order to settle claims that it had promoted risperidone and paliperidone for off-label uses including for dementia, anger management, and anxiety.[54] In November 2013, J&J was fined $2.2 billion for illegally marketing risperidone for use in people with dementia.[55] J&J has faced numerous civil lawsuits on behalf of children who were prescribed risperidone who grew breasts (a condition called gynecomastia); as of July 2016 there were about 1,500 cases in Pennsylvania state court in Philadelphia, and there had been a February 2015 verdict against J&J with $2.5 million awarded to a man from Alabama, a $1.75M verdict against J&J that November, and in 2016 a $70 million verdict against J&J.[56] In 2015, Steven Brill posted a 15-part investigative journalism piece on J&J in Huffington Post, called "America's most admired lawbreaker", which was focused on J&J's marketing of risperidone.[57][58] NamesBrand names include Risperdal, Risperdal Consta, Risperdal M-Tab, Risperdal Quicklets, and Risperlet. 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Should I try behavior therapy first? | journal = Journal of Autism and Developmental Disorders | volume = 38 | issue = 6 | pages = 1197–8 | date = July 2008 | pmid = 18463973 | doi = 10.1007/s10803-008-0573-7 }} 51. ^1 2 Drugs.com [https://www.drugs.com/international/risperidone.html International trade names for risperidone] {{webarchive|url=https://web.archive.org/web/20160318043334/http://www.drugs.com/international/risperidone.html |date=2016-03-18 }} Page accessed March 15, 2016 52. ^"Companies belittled risks of Risperdal, slapped with huge fine" {{webarchive|url=https://web.archive.org/web/20120412005624/http://www.latimes.com/news/nation/nationnow/la-na-nn-risperdal-arkansas-20120411,0,3974735.story |date=2012-04-12 }}, Los Angeles Times, 11 April 2012. 53. ^{{cite news|url=https://www.nytimes.com/2014/03/21/business/arkansas-court-reverses-1-2-billion-judgment-against-johnson-johnson.html?_r=0|title=Arkansas Court Reverses $1.2 Billion Judgment Against Johnson & Johnson - NYTimes.com|format=|access-date=|deadurl=no|archive-url=https://web.archive.org/web/20151105132203/http://www.nytimes.com/2014/03/21/business/arkansas-court-reverses-1-2-billion-judgment-against-johnson-johnson.html?_r=0|archive-date=2015-11-05|df=|newspaper=The New York Times|date=2014-03-20|last1=Thomas|first1=Katie}} 54. ^{{cite news|title=NY AG: Janssen pays $181M over drug marketing|date=30 August 2012|newspaper=The Seattle Times|url=http://www.seattletimes.com/seattle-news/ny-ag-janssen-pays-181m-over-drug-marketing/|deadurl=no|archive-url=https://web.archive.org/web/20160407105814/http://www.seattletimes.com/seattle-news/ny-ag-janssen-pays-181m-over-drug-marketing/|archive-date=7 April 2016|df=}} 55. ^{{cite web|url=http://www.justice.gov/opa/pr/johnson-johnson-pay-more-22-billion-resolve-criminal-and-civil-investigations|title=Johnson & Johnson to Pay More Than $2.2 Billion to Resolve Criminal and Civil Investigations | OPA | Department of Justice|format=|date=November 4, 2013|website=|access-date=|deadurl=no|archive-url=https://web.archive.org/web/20150305025106/http://www.justice.gov/opa/pr/johnson-johnson-pay-more-22-billion-resolve-criminal-and-civil-investigations|archive-date=March 5, 2015|df=}} 56. ^{{cite news|last1=Feeley|first1=Jef | name-list-format = vanc |title=J&J Hit With $70 Million Risperdal Verdict Over Male Breasts|url=https://www.bloomberg.com/news/articles/2016-07-01/j-j-faces-record-70-million-verdict-over-male-breasts|work=Bloomberg News|date=1 July 2016|deadurl=no|archive-url=https://web.archive.org/web/20170507080914/https://www.bloomberg.com/news/articles/2016-07-01/j-j-faces-record-70-million-verdict-over-male-breasts|archive-date=7 May 2017|df=}} 57. ^{{cite news|last1=Ashbrook|first1=Tom| name-list-format = vanc |title=Johnson & Johnson And The Big Lies Of Big Pharma|url=http://www.wbur.org/onpoint/2015/09/22/big-pharma-risperdal-steven-brill|work=NPR's "On Point"|date=September 22, 2015|deadurl=no|archive-url=https://web.archive.org/web/20161122224110/http://www.wbur.org/onpoint/2015/09/22/big-pharma-risperdal-steven-brill|archive-date=November 22, 2016|df=}} 58. ^{{cite news|last1=Brill|first1=Steven| name-list-format = vanc |title=America’s Most Admired Lawbreaker|url=http://highline.huffingtonpost.com/miracleindustry/americas-most-admired-lawbreaker/|work=The Huffington Post|date=September 2015|deadurl=no|archive-url=https://web.archive.org/web/20151002123107/http://highline.huffingtonpost.com/miracleindustry/americas-most-admired-lawbreaker/|archive-date=2015-10-02|df=}} External links{{portal bar|Pharmacy and pharmacology|Medicine|Psychiatry}}{{commons category|Risperidone}}
| title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Histamine receptor modulators}}{{Serotonin receptor modulators}} }} 16 : Atypical antipsychotics|Autism|Belgian inventions|Benzisoxazoles|Janssen Pharmaceutica|Lactams|Fluoroarenes|Piperidines|RTT|World Health Organization essential medicines|Alpha blockers|H1 receptor antagonists|Prolactin releasers|Pyrimidones|Serotonin antagonists|Mood disorders |
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