| 词条 | Perospirone |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464199317 | IUPAC_name = (3aS,7aR)-2-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-3a,4,5,6,7,7a-hexahydroisoindole-1,3-dione | image = Perospirone.svg | width = 300 | image2 = Perospirone-optimized-ball-and-stick.png | width2 = 300 | tradename = Lullan | Drugs.com = {{drugs.com|international|perospirone}} | pregnancy_category = | legal_status = Rx-only | routes_of_administration = Oral | bioavailability = | metabolism = Hepatic[1] | protein_bound = 92%[1] | elimination_half-life = 1.9-2.5 hours[1][1] | excretion = Renal (0.4% as unchanged drug)[1] | IUPHAR_ligand = 7556 | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 150915-41-6 | ATC_prefix = none | ATC_suffix = | PubChem = 115368 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 16737064 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = N303OK87DT | C=23 | H=30 | N=4 | O=2 | S=1 | molecular_weight = 426.57 g/mol | smiles = O=C4N(CCCCN1CCN(CC1)C\\3=N\\SCc2ccccc2/3)C(=O)[C@@H]5CCCC[C@H]45 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C24H32N4O2S/c29-23-20-9-3-4-10-21(20)24(30)28(23)12-6-5-11-26-13-15-27(16-14-26)22-19-8-2-1-7-18(19)17-31-25-22/h1-2,7-8,20-21H,3-6,9-17H2/t20-,21+ | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = GTAIPSDXDDTGBZ-OYRHEFFESA-N }}Perospirone (Lullan) is an atypical antipsychotic of the azapirone family.[2] It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania.[3][4] Medical usesIts primary uses are in the treatment of schizophrenia and bipolar mania.[3][4] SchizophreniaIn a clinical trial that compared it to haloperidol in the treatment of schizophrenia it was found to produce significantly superior overall symptom control.[5] In another clinical trial perospirone was compared with mosapramine and produced a similar reduction in total PANSS score, except with respect to the blunted affect part of the PANSS negative score, in which perospirone produced a significantly greater improvement.[6] In an open-label clinical trial comparing aripiprazole with perospirone there was no significant difference between the two treatments discovered in terms of both efficacy and tolerability.[7] In 2009 a clinical trial found that perospirone produced a similar reduction of PANSS score than risperidone and the extrapyramidal side effects was similar in both frequency and severity between groups.[8] A meta-analysis published in 2013 found that it is statistically significantly less efficacious than other second-generation antipsychotics.[9] Adverse effectsHas a higher incidence of extrapyramidal side effects than the other atypical antipsychotics, but still less than that seen with typical antipsychotics.[2][10] A trend was observed in a clinical trial comparing mosapramine with perospirone that favoured perospirone for producing less prominent extrapyramidal side effects than mosapramine although statistical significant was not reached.[6] It may produce less QT interval prolongation than zotepine, as in one patient who had previously been on zotepine switching to perospirone corrected their prolonged QT interval.[11] It also tended to produce less severe extrapyramidal side effects than haloperidol in a clinical trial comparing the two (although statistical significance was not reached).[5] PharmacologyPerospirone binds to the following receptors with very high affinity (as an antagonist unless otherwise specified):[9][22][12][13][14][15][16]
And the following receptor with high affinity:[9]
And the following with moderate affinity:[9]
And with low affinity for the following receptor:[9]
See also
References1. ^{{cite journal|title=Steady-State Pharmacokinetics of a New Antipsychotic Agent Perospirone and Its Active Metabolite, and Its Relationship|journal=Therapeutic Drug Monitoring|date=August 2004|volume=26|issue=4|pages=361–365|author1=Yasui-Furukori, N |author2=Furukori, H |author3=Nakagami, T |author4=Saito, M |author5=Inoue, Y |author6=Kaneko, S |author7=Tateishi, T |doi=10.1097/00007691-200408000-00004|pmid=15257064}} {{Antipsychotics}}{{Navboxes2. ^1 2 3 4 5 {{cite journal |author1=Onrust, SV |author2=McClellan, K | title = Perospirone | journal = CNS Drugs | volume = 15 | issue = 4 | pages = 329–37; discussion 338 | year = 2001 | pmid = 11463136 | doi = 10.2165/00023210-200115040-00006 }} 3. ^1 {{cite journal | author = de Paulis, T | title = Perospirone (Sumitomo Pharmaceuticals) | journal = Current Opinion in Investigational Drugs | volume = 3 | issue = 1 | pages = 121–9 |date=January 2002 | pmid = 12054062}} 4. ^1 {{cite web | url = http://www.ds-pharma.co.jp/english/news/sumitomo_2001/no_002.html | title = Sumitomo Pharmaceuticals 2001 | News Release | Dainippon Sumitomo Pharma | website = | accessdate = | deadurl = yes | archiveurl = https://web.archive.org/web/20060224145409/http://www.ds-pharma.co.jp/english/news/sumitomo_2001/no_002.html | archivedate = 24 February 2006 | df = dmy-all }} 5. ^1 {{cite journal|last=Murasaki|first=M|author2=Koyama, T |author3=Machiyama, Y |title=Clinical evaluation of a new antipsychotic, perospirone HCl, on schizophrenia: a comparative double-blind study with haloperidol|journal=Rinsho Hyoka|year=1997|volume=24|issue=2–3|pages=159–205|display-authors=etal}} 6. ^1 {{cite journal|last=Kudo|first=Y|author2=Nakajima, T |author3=Saito, M |title=Clinical evaluation of a serotonin-2 and dopamine-2 receptor antagonist (SDA), perospirone HCl on schizophrenia: a comparative double-blind study with mosapramine HCl|journal=Rinsho Hyoka|year=1997|volume=24|issue=2–3|pages=207–48|display-authors=etal}} 7. ^{{cite journal|title=A 12-week randomized, open-label study of perospirone versus aripiprazole in the treatment of Japanese schizophrenia patients|journal=Progress in Neuro-Psychopharmacology and Biological Psychiatry|date=January 2013|volume=40|pages=110–114|doi=10.1016/j.pnpbp.2012.09.010|pmid=23022672|author1=Takekita, Y |author2=Kato, M |author3=Wakeno, M |author4=Sakai, S |author5=Suwa, A |author6=Nishida, K |author7=Okugawa, G |author8=Kinoshita, T }} 8. ^{{cite journal|last=Okugawa|first=G|author2=Kato, M |author3=Wakeno, M |author4=Koh, J |author5=Morikawa, M |author6=Matsumoto, N |author7=Shinosaki, K |author8=Yoneda, H |author9=Kishimoto, T |author10= Kinoshita, T |title=Randomized clinical comparison of perospirone and risperidone in patients with schizophrenia: Kansai Psychiatric Multicenter Study|journal=Psychiatry and Clinical Neurosciences|date=June 2009|volume=63|issue=3|pages=322–328|doi=10.1111/j.1440-1819.2009.01947.x|pmid=19566763}} 9. ^1 2 3 4 {{cite journal|title=Efficacy and Tolerability of Perospirone in Schizophrenia: A Systematic Review and Meta-Analysis of Randomized Controlled Trials|journal=CNS Drugs|date=September 2013|volume=27|issue=9|pages=731–741|doi=10.1007/s40263-013-0085-7|pmid=23812802|author1=Kishi, T |author2=Iwata, N }} 10. ^{{cite book|title=Perospirone Hydrochloride|work=Martindale: The Complete Drug Reference|publisher = The Royal Pharmaceutical Society of Great Britain|date=23 September 2011|accessdate=3 November 2013|url=http://www.medicinescomplete.com/mc/martindale/current/15232-k.htm}} 11. ^{{cite journal|last=Suzuki|first=Y|author2=Watanabe, J |author3=Sugai, T |author4=Fukui, N |author5=Ono, S |author6=Tsuneyama, N |author7=Saito, M |author8= Someya T |title=Improvement in QTc prolongation induced by zotepine following a switch to perospirone|journal=Psychiatry and Clinical Neurosciences|date=March 2012|volume=66|issue=3|page=244|doi=10.1111/j.1440-1819.2012.02321.x|pmid=22443250}} 12. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | url = http://pdsp.med.unc.edu/pdsp.php | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 3 November 2013 | date = 12 January 2011 | deadurl = yes | archiveurl = https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php | archivedate = 8 November 2013 | df = dmy-all }} 13. ^1 {{cite journal |author1=Hirose, A |author2=Kato, T |author3=Ohno, Y |author4=Shimizu, H |author5=Tanaka, H |author6=Nakamura, M |author7=Katsube, J | title = Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions | journal = Japanese Journal of Pharmacology | volume = 53 | issue = 3 | pages = 321–9 |date=July 1990| pmid = 1975278 | doi = 10.1254/jjp.53.321|url=https://www.jstage.jst.go.jp/article/jphs1951/53/3/53_3_321/_pdf }} 14. ^{{cite journal |author1=Kato, T |author2=Hirose, A |author3=Ohno, Y |author4=Shimizu, H |author5=Tanaka, H |author6=Nakamura, M | title = Binding profile of SM-9018, a novel antipsychotic candidate | journal = Japanese Journal of Pharmacology| volume = 54 | issue = 4 | pages = 478–81 |date=December 1990 | pmid = 1982326 | doi = 10.1254/jjp.54.478}} 15. ^{{cite journal |author1=Odagaki, Y |author2=Toyoshima, R | title = 5-HT1A receptor agonist properties of antipsychotics determined by [35S]GTPgammaS binding in rat hippocampal membranes | journal = Clinical and Experimental Pharmacology & Physiology |volume = 34 | issue = 5–6 | pages = 462–6 | year = 2007 | pmid = 17439416 | doi = 10.1111/j.1440-1681.2007.04595.x}} 16. ^{{cite journal |author1=Seeman, P |author2=Tallerico, T | title = Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors | journal = Molecular Psychiatry |volume = 3 | issue = 2 | pages = 123–34 |date=March 1998 | pmid = 9577836 | doi = 10.1038/sj.mp.4000336}} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Histamine receptor modulators}}{{Serotonin receptor modulators}} }}{{Use dmy dates|date=April 2017}} 5 : Atypical antipsychotics|Azapirones|Benzoisothiazoles|Imides|Piperazines |
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