Melperone in treatment-refractory schizophrenia: a case series

Whiskey, Eromona; Vavrová, Marta; Gaughran, Fiona; Taylor, David

doi:10.1177/2045125311399800

Cited by 8 publications

(3 citation statements)

References 10 publications

(9 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Since haloperidol is a dopamine D2 antagonist, it had a high affinity for D2 dopamine receptors, and moderate affinity for serotonin 5-HT2A, and 5-HT1D receptors in human brain tissue homogenates 2 . Melperone is used for the treatment of schizophrenia, sleep disorders, agitation, and mentally confused states by antagonist activity at D2 dopaminergic and 5HT2A serotonergic receptors 39 . Similarly, pipamperone can be used for the treatment of chronic psychoses and states of aggressiveness of various origins.…”

Section: Discussionmentioning

confidence: 99%

Pirenperone relieves the symptoms of fragile X syndrome in Fmr1 knockout mice

Kim

Jeon

Gonzales

et al. 2022

Sci Rep

View full text Add to dashboard Cite

Fragile X syndrome (FXS) is a neurodevelopmental disorder that is caused by the loss of Fragile X-linked mental retardation protein (FMRP), an RNA binding protein that can bind and recognize different RNA structures and regulate the target mRNAs’ translation involved in neuronal synaptic plasticity. Perturbations of this gene expression network have been related to abnormal behavioral symptoms such as hyperactivity, and impulsivity. Considering the roles of FMRP in the modulation of mRNA translation, we investigated the differentially expressed genes which might be targeted to revert to normal and ameliorate behavioral symptoms. Gene expression data was analyzed and used the connectivity map (CMap) to understand the changes in gene expression in FXS and predict the effective drug candidates. We analyzed the GSE7329 dataset that had 15 control and 8 FXS patients’ lymphoblastoid samples. Among 924 genes, 42 genes were selected as signatures for CMap analysis, and 24 associated drugs were found. Pirenperone was selected as a potential drug candidate for FXS for its possible antipsychotic effect. Treatment of pirenperone increased the expression level of Fmr1 gene. Moreover, pirenperone rescued the behavioral deficits in Fmr1 KO mice including hyperactivity, spatial memory, and impulsivity. These results suggest that pirenperone is a new drug candidate for FXS, which should be verified in future studies.

show abstract

Section: Discussionmentioning

confidence: 99%

Pirenperone relieves the symptoms of fragile X syndrome in Fmr1 knockout mice

Kim

Jeon

Gonzales

et al. 2022

Sci Rep

View full text Add to dashboard Cite

show abstract

“…Melperone is an antipsychotic of the butyrophenone class, with a similar structure to haloperidol, but with a profile of receptor action more akin to atypical antipsychotics [ 40 ]. It is often used in treatment-resistant cases of schizophrenia where clozapine is not suitable [ 41 ] and its half-life is 3–4 h. The patient's weekly activities consisted of leaving the house to food shop twice a week. He found the drug made him tired during the day, and he had put on large amounts of weight.…”

Section: Case Studiesmentioning

confidence: 99%

Gradually tapering off antipsychotics: lessons for practice from case studies and neurobiological principles

Horowitz,

Moncrieff

2024

Current Opinion in Psychiatry

View full text Add to dashboard Cite

Purpose of review There has been an increasing focus on deprescribing in psychiatry recently, particularly of antipsychotic medication, with recognition that not all patients with psychotic disorders require lifelong medication. We summarize some empirical and theoretical papers, and examine case studies to provide instruction on this topic. Recent findings Recent studies have found that slower tapering (over months or longer) of antipsychotics is associated with a lower relapse rate than quicker tapering (weeks). Case studies presented suggest that the process of reduction is associated with the precipitation or exacerbation of psychotic symptoms and that a slower process of reduction may minimize this effect. This may be because faster reductions cause greater disruption of homeostatic equilibria, provoking psychotic symptoms either as direct withdrawal symptoms or consequences of nonpsychotic withdrawal symptoms (e.g. insomnia) – although not all patients will experience withdrawal symptoms. This suggests that smaller dose reductions, especially at lower doses, made very gradually, may minimize the risk of psychotic symptoms. Summary Slower tapering of antipsychotics may provide time for adaptations made to the presence of the medications to resolve, thus reducing the disruption to homeostatic equilibrium caused by dose reduction, potentially reducing the risk of relapse. Exacerbation of psychotic symptoms on antipsychotic reduction may not represent evidence of the need for a higher dose of antipsychotic on a long-term basis but may indicate the need for more gradual reduction. Gradual reduction of antipsychotics, especially after long-term use in clinical practice is prudent.

show abstract

“…-Used postoperatively and in as antiemetic, with minimal toxicity [329,330]. -It also has antagonistic activity at 5HT 2A receptors [331].…”

Section: Domperidonementioning

confidence: 99%