Perospirone
Atypical antipsychotic medication
From Wikipedia, the free encyclopedia
Perospirone (Lullan) is an atypical antipsychotic of the azapirone family.[1] It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania.[3][4]
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| Trade names | Lullan |
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| Routes of administration | Oral |
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| Protein binding | 92%[1] |
| Metabolism | Hepatic[1] |
| Elimination half-life | 1.9–2.5 hours[1][2] |
| Excretion | Renal (0.4% as unchanged drug)[1] |
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| Formula | C23H30N4O2S |
| Molar mass | 426.58 g·mol−1 |
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Medical uses
Its primary uses are in the treatment of schizophrenia and bipolar mania.[3][4]
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.[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 effects
Has a higher incidence of extrapyramidal side effects than the other atypical antipsychotics, but still less than that seen with typical antipsychotics.[1][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]
Discontinuation
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse.[12] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite.[13] Other symptoms may include restlessness, increased sweating, and trouble sleeping.[13] Less commonly there may be a felling of the world spinning, numbness, or muscle pains.[13] Symptoms generally resolve after a short period of time.[13]
There is tentative evidence that discontinuation of antipsychotics can result in psychosis.[14] It may also result in reoccurrence of the condition that is being treated.[15] Rarely tardive dyskinesia can occur when the medication is stopped.[13]
Pharmacology
Perospirone binds to the following receptors with very high affinity (as an antagonist unless otherwise specified):[9][16][17][18][19][20]
And the following receptor with high affinity:[9]
- H1 (inverse agonist)
And the following with moderate affinity:[9]
And with low affinity for the following receptor:[9]
See also
- Azapirone
- Blonanserin — another second-generation antipsychotic that's only approved for clinical use in East Asia
- Mosapramine
- Zotepine