perospirone / Generic mfg. - LARVOL DELTA

Development of the novel formulations of perospirone for the treatment of schizophrenia. (PubMed, Drug Deliv Transl Res) - "These oral extended-release and controlled-release tablets promise to alleviate patients' medication discomfort and provide long-term sustained drug release. They would provide a platform with broad prospects for the clinical treatment of schizophrenia."

Journal • CNS Disorders • Cognitive Disorders • Psychiatry • Schizophrenia

Delirium due to Trousseau syndrome treated with memantine and perospirone: A case report. (PubMed, PCN Rep) - "Although haloperidol, risperidone, and chlorpromazine were used, severe insomnia persisted. We report the first case of Trousseau syndrome delirium treated by memantine used with perospirone. Although further studies are needed, memantine and perospirone might be candidates for the management of psychiatric symptoms associated with Trousseau syndrome."

Journal • CNS Disorders • Insomnia • Lung Cancer • Oncology • Psychiatry • Sleep Disorder • Solid Tumor

The effective perospirone augmentation with clonazepam for treatment-resistant burning mouth syndrome: A case report. (PubMed, Neuropsychopharmacol Rep) - "Further attempts to alleviate symptoms by combining aripiprazole with amitriptyline, aripiprazole with mirtazapine, or aripiprazole with clonazepam were limited; however, nearly all symptoms were relieved by a combination of perospirone 8.0 mg with clonazepam 1.5 mg. However, a regimen of perospirone 6.0 mg and clonazepam 1.5 mg relieved the crumb-like sensation and pain and culminated in a stabilized condition. The reported cases suggested that multiple approaches targeting the dopaminergic circuit in basal ganglia involving the serotoninergic and GABA systems, through the administration of perospirone with clonazepam is an effective adjunctive treatment for the remaining uncomfortable sensations in patients with BMS."

Biomarker • Clinical • Clinical guideline • Journal • Observational data • P1 data • P2 data • Retrospective data • Review • Pain • Xerostomia

Therapeutic drug monitoring of perospirone: The lowest effective plasma concentration in patients with schizophrenia. (PubMed, Asian J Psychiatr) - "The findings suggest that therapeutic drug monitoring of perospirone and adjustments to achieve steady-state concentrations of ≥ 1.17 ng/mL can be beneficial for optimising treatment for patients with schizophrenia."

Journal • CNS Disorders • Psychiatry • Schizophrenia

Adverse effects of antipsychotics on sleep in patients with schizophrenia. Systematic review and meta-analysis. (PubMed, Front Psychiatry) - "Several of the included antipsychotics were associated with a significantly increased risk of somnolence; haloperidol (OR, 1.90; 95% CrI, 1.12-3.22), lurasidone (OR, 2.25; 95% CrI, 1.28-3.97) and ziprasidone (OR, 1.79; 95% CrI, 1.06-3.02) had the narrowest confidence intervals...The evidence shows that chlorpromazine, clozapine, flupentixol, perospirone, and amisulpride had favorable safety profiles. In contrast, ziprasidone, perphenazine, haloperidol, and risperidone were the least safe for sleep. https://www.crd.york.ac.uk/prospero/display_record.php?ID=CRD42017078052, identifier: PROSPERO 2017 CRD42017078052."

Adverse events • Clinical • Retrospective data • Review • Anesthesia • CNS Disorders • Insomnia • Psychiatry • Schizophrenia • Sleep Disorder

Exploration of interaction interface of TRKβ/BDNF through fingerprint analysis to disinter potential agonists. (PubMed, Mol Divers) - "The study revealed molecular interactions of Perospirone, Droperidol, Urapidil, and Clobenzorex with the crucial amino acids lining the active binding pocket of TRKβ...Clobenzorex displayed high stability in dynamics simulation and therefore this drug is recommended for further experimental evaluations to attain better mechanistic insights and predict its implications in correcting neuropathological aberrations. This study's focus on the interaction interface between TRKβ and BDNF, combined with the utilization of fingerprint analysis for drug repurposing, contributes to our understanding of neurotrophic signalling and holds potential for identifying new therapeutic options for neurological disorders."

Journal • CNS Disorders • Oncology • BDNF

Agonistic properties of a series of psychotropic drugs at 5-HT receptors in rat and human brain membranes determined by [S]GTPγS binding assay. (PubMed, Pharmacol Rep) - "Our previous studies have raised the concept of a psychoactive drug group with a common pharmacological mechanism of action, i.e., 5-HT receptor agonism, consisting of perospirone, aripiprazole, ziprasidone, clozapine, quetiapine, nemonapride, and trazodone. The present study demonstrates the data indicating that brexpiprazole and probably vortioxetine are included in this drug group. Lurasidone and asenapine are excluded from this group."

Journal • Preclinical

Safety and Effectiveness of Perospirone in Comparison to Risperidone for Treatment of Delirium in Patients with Advanced Cancer: A Multicenter Prospective Observational Study in Real-World Psycho-Oncology Settings. (PubMed, Acta Med Okayama) - "There were fewer episodes of somnolence as an adverse event in the perospirone group. Low-dose perospirone was thus found to be effective for the treatment of delirium in patients with advanced cancer and may be associated with fewer episodes of over-sedation as an adverse event."

Journal • Observational data • Real-world evidence • Anesthesia • CNS Disorders • Oncology

A novel and robust analytical method for the quantification of perospirone in human plasma using an LC-MS/MS system with self-internal standard calibration. (PubMed, Clin Biochem) - "This bioanalytical method can be used for the quantification of perospirone in human plasma by LC-MS/MS-Mate 9500 using perospirone itself as the SIS."

Journal

An Observational Study on Atypical Antipsychotics Long-term Treatment Patients With Schizophrenia (clinicaltrials.gov) - P=N/A; N=3000; Recruiting; Sponsor: Shanghai Mental Health Center; Trial completion date: May 2022 ➔ May 2033; Trial primary completion date: May 2021 ➔ May 2030

Clinical • Trial completion date • Trial primary completion date • CNS Disorders • Psychiatry • Schizophrenia

Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles. (PubMed, Biol Pharm Bull) - "Further, 11 antipsychotics (perphenazine, fluphenazine, prochlorperazine (phenothiazines), haloperidol, bromperidol, timiperone, spiperone (butyrophenones), pimozide (a diphenylbutylpiperidine), perospirone, blonanserin (serotonin-dopamine antagonists; SDAs), and asenapine (a MARTA)) significantly suppressed ACh-induced contraction; however, suppression occurred at concentrations substantially exceeding clinically achievable blood levels. The remaining nine antipsychotics (pipamperone (a butyrophenone), sulpiride, sultopride, tiapride, nemonapride (benzamides), risperidone, paliperidone (SDAs), aripiprazole, and brexpiprazole (dopamine partial agonists)) did not inhibit ACh-induced contractions at concentrations up to 10 M. These findings suggest that chlorpromazine, levomepromazine, zotepine, olanzapine, quetiapine, and clozapine should be avoided by elderly people with urinary disorders."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Psychiatry • Schizophrenia

Efficacy and safety of antipsychotic treatments for schizophrenia: A systematic review and network meta-analysis of randomized trials in Japan. (PubMed, J Psychiatr Res) - "Our results are similar to those of previous network meta-analysis involving various races and ethnicities."

Journal • Retrospective data • Review • CNS Disorders • Psychiatry • Schizophrenia

Livzon Pharmaceutical : ANNOUNCEMENT OF AUDITED RESULTS FOR THE YEAR ENDED 31 DECEMBER 2020 (Market Screener) - "...thirdly, professional and refined management were strengthened with continuous improvements in sales team of the psychiatric specialist, and the growth in Perospirone Hydrochloride Tablet...accelerated and doubled after admission to the National Reimbursement Drug List; fourthly, marketing with evidential support continued to expand, a total of 8 core guidelines for key products including the...Perospirone Hydrochloride Tablets...were adopted, and post-launching clinical research and economic research on drugs were progressing orderly, which drove further growth in the products....The sales income generated by key psychiatric products, Fluvoxamine Maleate Tablets and Perospirone Hydrochloride Tablets...amounted to RMB171.47 million and RMB107.19 million respectively, representing a year-on-year increase of 33.00% and 101.78% respectively."

Reimbursement • Sales • CNS Disorders • Schizophrenia

Efficacy and Safety of Peropirone Hydrochloride Tablets in the Treatment of Adolescent Bipolar Disorder Depression (clinicaltrials.gov) - P4; N=189; Recruiting; Sponsor: Shanghai Mental Health Center

New P4 trial • Bipolar Disorder • CNS Disorders • Depression • Mood Disorders • Psychiatry

[VIRTUAL] Camptocormia Secondary to Dopamine-Antagonist-Induced Dystonia of the Rectus Abdominis Muscles: A Case Report (CINP 2021) - "She was referred to our hospital at the age of 51 with mild-asymptomatic scoliosis which gradually developed after starting risperidone, and mild delusions and auditory hallucination with risperidone 2 mg/d, perospirone 12 mg/d, and sodium valproate 400 mg/d. Camptocormia resolved by reducing the dose of perospirone and adding quetiapine. This suggests that lowering the intensity of dopamine D2 receptor blockade of dopamine antagonist improved the dystonia of the rectus abdominis muscles and thereby camptocormia. Thus, in a case of camptocormia, abdominal physical examination and abdominal CT scan may be highly advisable considering the possibility of truncal dystonia."

Clinical • CNS Disorders • Dystonia • Epilepsy • Movement Disorders • Psychiatry • Schizophrenia • DRD2

Safety and related factors of treatment with long-term atypical antipsychotic in Chinese patients with schizophrenia: observational study. (PubMed, Gen Psychiatr) - "The atypical antipsychotics include quetiapine, olanzapine, risperidone, aripiprazole, ziprasidone, paliperidone, amisulpride, perospirone and clozapine. This is a large sample, non-interventional and long-term prospective clinical study designed to truly reflect the specific details of clinical practice, fully respect patients' needs, and understand patients' treatment intentions and actual treatment details. This research method details the aims, methods, study design, strengths and limitations of the study."

Clinical • Journal • Observational data • CNS Disorders • Depression • Psychiatry • Schizophrenia

Neuroprotective effects of the second generation antipsychotics. (PubMed, Schizophr Res) - "A review of the literature suggests that in addition to their antipsychotic efficacy and low motoric side effects, SGAs exert measurable neuroprotective effects mediated via multiple molecular mechanisms and often in a dose-dependent manner. The neuroprotective effects of SGAs range from preventative to restorative and may play a salutary role in ameliorating the neurodegenerative effects of psychosis."

Journal • Review • CNS Disorders • Immunology • Psychiatry • Solid Tumor

Dissociation in Pharmacokinetic Attenuation Between Central Dopamine D2 Receptor Occupancy and Peripheral Blood Concentration of Antipsychotics: A Systematic Review. (PubMed, J Clin Psychiatry) - "The findings indicate pharmacokinetic attenuation of antipsychotics was generally slower at the central versus the peripheral level and pose a critical challenge to the current dosing strategy that primarily relies on peripheral pharmacokinetics of antipsychotics."

Journal • PK/PD data • Review • CNS Disorders • Schizophrenia

Antihyperalgesic effects of intrathecal perospirone in a rat model of neuropathic pain. (PubMed, Pharmacol Biochem Behav) - "WAY-100635 reversed the antihyperalgesic action of perospirone significantly, but neither DOI nor sumanirole exhibited such an effect. We conclude that perospirone attenuates mechanical and cold hyperalgesia principally via 5-HT receptor activation in the spinal cord, and the agent is a promising novel candidate for neuropathic pain relief."

Journal • Preclinical • CNS Disorders • Neuralgia • Pain

Efficacy and Tolerability of Dopamine D2 Receptor Partial Agonists Versus D2 Receptor Antagonists in Early Psychosis: A Systematic Review and Meta-Analysis (SOBP 2020) - "Aripiprazole was the only identified D2R partial agonist and was compared with risperidone, quetiapine, olanzapine, ziprasidone, paliperidone, perospirone, and haloperidol. Aripiprazole’s efficacy did not differ substantially from D2R antagonists in early psychosis, whereas it was more favorable regarding antidepressant effects and some side-effect profiles. Funding Source Unfunded Funding Source: Unfunded"

Retrospective data • Review • CNS Disorders • Psychiatry • Schizophrenia

Life-Threatening Serotonin Syndrome Precipitated by Discontinuation of Serotonin-Dopamine Antagonist in the Presence of Serotonergic Agents: A Case Report. (PubMed, Clin Neuropharmacol) - "Discontinuation of antipsychotics that are 5-HT2 receptor antagonists may lead to serotonin syndrome in patients who take serotonergic agents. As extrapyramidal symptoms and serotonin toxicity share some clinical features, detailed drug history and physical examination are necessary for successful treatment."

Clinical • Journal

Experimental analysis of the onset mechanism of TdP reported in an LQT3 patient during pharmacological treatment with serotonin-dopamine antagonists against insomnia and nocturnal delirium. (PubMed, Heart Vessels) - "These results indicate that perospirone and blonanserin may cause the hypotension-induced, reflex-mediated increase of sympathetic tone, leading to the increase of inward Ca current in the heart except that the high dose of perospirone reversed them. Thus, blonanserin may have more potential to produce intracellular Ca overload triggering early afterdepolarization than perospirone, which might explain the onset of TdP in the LQT3 patient."

Clinical • Journal

Efficacy and Tolerability of Atypical Antipsychotics in the Treatment of Delirium: A Systematic Review of the Literature. (PubMed, Psychosomatics) - "Although the current evidence of the efficacy and tolerability of AAPs in the treatment of delirium is limited and the heterogeneity of the data precluded a meta-analysis, olanzapine and quetiapine seem to be adequate alternatives to haloperidol, especially in patients who are vulnerable for extrapyramidal symptoms, who require sedation or who have a history of haloperidol intolerance. Evidently, larger-scale RCTs are urgently required."

Clinical • Journal • Review

Neuroprotective Effects of the Second Generation Antipsychotics (APA 2019) - "...All studies included at least one SGA (aripiprazole, clozapine, lurasidone, olanzapine, paliperidone, perospirone, quetiapine, risperidone, and/or ziprasidone). A few also included FGAs as a comparator (predominantly haloperidol)... A review of the literature suggests that in addition to their antipsychotic efficacy and low motoric side effects, SGAs exert measurable neuroprotective effects mediated via multiple molecular mechanisms and often in a dosedependent manner. The neuroprotective effects of SGAs range from preventative to restorative and may play a salutary role in ameliorating the neurodegenerative effects of psychosis."

New long-chain derivatives of 1-(1,2-benzisothiazol-3-yl)piperazine with high affinity for selected serotonin receptors (ACS-Sp 2019) - "To this group belong Lurasidone[4], Perospirone[5] and Ziprasidone[6]. In addition, a new ecological, microwave assisted method of synthesis for the described compounds was developed. The obtained compounds were characterized by high affinity for mentioned receptors, which makes it possible to use them as potential drugs."