Perospirone

Quality 0.50 · 2 views · Updated 2 months ago

Atypical antipsychotic medication

title: "Perospirone" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["atypical-antipsychotics", "azapirones", "piperazinylbenzisothiazoles"] description: "Atypical antipsychotic medication" topic_path: "general/atypical-antipsychotics" source: "https://en.wikipedia.org/wiki/Perospirone" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Atypical antipsychotic medication ::

| C=23 | H=30 | N=4 | O=2 | S=1 | smiles = O=C4N(CCCCN1CCN(CC1)C\3=N\SCc2ccccc2/3)C(=O)[C@@H]5CCCC[C@H]45 | StdInChI_Ref = | 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 = | StdInChIKey = GTAIPSDXDDTGBZ-OYRHEFFESA-N

Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania.

Medical uses

Its primary uses are in the treatment of schizophrenia and bipolar mania.

Schizophrenia

In a clinical trial that compared it to haloperidol in the treatment of schizophrenia it was found to produce significantly superior overall symptom control. 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. 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. 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.

A meta-analysis published in 2013 found that it is statistically significantly less efficacious than other second-generation antipsychotics.

Adverse effects

Has a higher incidence of extrapyramidal side effects than the other atypical antipsychotics, but still less than that seen with typical antipsychotics. 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. 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. 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).

Discontinuation

The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse. Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite. Other symptoms may include restlessness, increased sweating, and trouble sleeping. Less commonly there may be a felling of the world spinning, numbness, or muscle pains. Symptoms generally resolve after a short period of time.

There is tentative evidence that discontinuation of antipsychotics can result in psychosis. It may also result in reoccurrence of the condition that is being treated. Rarely tardive dyskinesia can occur when the medication is stopped.

Pharmacology

Perospirone binds to the following receptors with very high affinity (as an antagonist unless otherwise specified):

5-HT1A (partial agonist; Ki = 2.9 nM)
5-HT2A (inverse agonist; Ki = 1.3 nM)
D2 (Ki = 0.6 nM)

And the following receptor with high affinity:

H1 (inverse agonist)

And the following with moderate affinity:

D4
α1 adrenoceptor

And with low affinity for the following receptor:

References

(August 2004). "Steady-state pharmacokinetics of a new antipsychotic agent perospirone and its active metabolite, and its relationship with prolactin response". Therapeutic Drug Monitoring.
(2001). "Perospirone". CNS Drugs.
(January 2002). "Perospirone (Sumitomo Pharmaceuticals)". Current Opinion in Investigational Drugs.
(8 February 2001). "Now on the Market : New Antipsychotic "Lullan® Tablets" - serotonin-dopamine antagonist originated in Japan". Sumitomo Pharmaceuticals 2001 | News Release | Dainippon Sumitomo Pharma.
(1997). "Clinical evaluation of a new antipsychotic, perospirone HCl, on schizophrenia: a comparative double-blind study with haloperidol". Rinsho Hyoka.
(1997). "Clinical evaluation of a serotonin-2 and dopamine-2 receptor antagonist (SDA), perospirone HCl on schizophrenia: a comparative double-blind study with mosapramine HCl". Rinsho Hyoka.
(January 2013). "A 12-week randomized, open-label study of perospirone versus aripiprazole in the treatment of Japanese schizophrenia patients". Progress in Neuro-Psychopharmacology & Biological Psychiatry.
(June 2009). "Randomized clinical comparison of perospirone and risperidone in patients with schizophrenia: Kansai Psychiatric Multicenter Study". Psychiatry and Clinical Neurosciences.
(September 2013). "Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials". CNS Drugs.
(23 September 2011). "Martindale: The Complete Drug Reference". The Royal Pharmaceutical Society of Great Britain.
(April 2012). "Improvement in QTc prolongation induced by zotepine following a switch to perospirone". Psychiatry and Clinical Neurosciences.
(March 2009). "British National Formulary". Royal Pharmaceutical Society of Great Britain.
(2004). "Adverse Syndromes and Psychiatric Drugs: A Clinical Guide". OUP Oxford.
(July 2006). "Does antipsychotic withdrawal provoke psychosis? Review of the literature on rapid onset psychosis (supersensitivity psychosis) and withdrawal-related relapse". Acta Psychiatrica Scandinavica.
(2013). "Adherence to Antipsychotics in Schizophrenia". Springer Science & Business Media.
(12 January 2011). "PDSP K_i Database". University of North Carolina at Chapel Hill and the United States National Institute of Mental Health.
(July 1990). "Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions". Japanese Journal of Pharmacology.
(December 1990). "Binding profile of SM-9018, a novel antipsychotic candidate". Japanese Journal of Pharmacology.
(2007). "5-HT1A receptor agonist properties of antipsychotics determined by [35S]GTPgammaS binding in rat hippocampal membranes". Clinical and Experimental Pharmacology & Physiology.
(March 1998). "Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors". Molecular Psychiatry.

::callout[type=info title="Wikipedia Source"] This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page. ::