chlorprothixene / Generic mfg. - LARVOL DELTA

Survey of the Notonectidae (Insecta, Hemiptera, Heteroptera, Nepomorpha) from northeastern Brazil. (PubMed, Zookeys) - "Nearly 1400 specimens of the following 18 species, four genera, and two subfamilies have been collected: Buenoaamnigenus (White, 1879), B.femoralis (Fieber, 1851), B.fuscipennis (Berg, 1879), B.koina Nieser & Pelli, 1994, B.konta Nieser & Pelli, 1994, B.mutabilis Truxal, 1953, B.pallipes (Fabricius, 1803), B.platycnemis (Fieber, 1851), B.pseudomutabilis Barbosa, Ribeiro & Nessimian, 2010, B.salutis Kirkaldy, 1904, B.tarsalis Truxal, 1953, B.unguis Truxal, 1953 (Anisopinae); Enitharoidesbrasiliensis (Spinola, 1837), E.tricomerus Barbosa, Ribeiro & Nessimian, 2017, Martaregabentoi Truxal, 1949, M.brasiliensis Truxal, 1949, M.membranacea White, 1879, and Notonectadisturbata Hungerford, 1926 (Notonectinae). Altogether, they represent 30 new records from the states of Alagoas, Bahia, Ceará, Pernambuco, Piauí, and Sergipe, and seven new records from northeastern Brazil, increasing the number of species recorded from the region from 11 to 18. A key to..."

Journal

Sexual dysfunctions associated with antipsychotic drug intake: a retrospective analysis of the FDA adverse events reporting system (FAERS). (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "FAERS was queried for sexual dysfunction adverse events (encoded by 35 different MedDRA preferred terms) secondary to amisulpride, aripiprazole, chlorprothixene, clozapine, haloperidol, loxapine, olanzapine, pipamperone, quetiapine, risperidone, and ziprasidone from 2000 to 2023. The pathogenesis of SD does not appear to be limited to specific pathomechanisms and therefore not to specific substances. The differing report distributions by sex and the impact of polypharmacy on the symptoms warrant further investigations."

Adverse events • Journal • Retrospective data • CNS Disorders • Sexual Disorders

Personalized character of toxic effects through mass nonlethal poisoning by phenazepam and other psychoactive substances (PubMed, Sud Med Ekspert) - "Other psychoactive substances (baclofen, pregabalin, chlorprothixene, chlorpromazine, phenibut, tramadol, diazepam), narcotic substances and ethanol were also found in the sufferers. The phenazepam concentration in the blood was in the range of 109.75-786.50 ng/ml, in the urine - 8.97-101.28 ng/ml. The pharmacokinetic and toxicokinetic characteristics of toxicants as well as additional factors characterizing the phenotype of the sufferer in addition to drug's content in the biological material must be taken into account to determine the toxicity level of phenazepam against the background of combined action with other psychoactive substances."

Journal

Global occurrence and aquatic hazards of antipsychotics in sewage influents, effluent discharges and surface waters. (PubMed, Environ Pollut) - "In wastewater effluent discharges and surface waters, sulpiride was the most detected antipsychotic; however, percent exceedances of the THV were minimal (0.6%) for this medication. In contrast, we observed elevated aquatic hazards for chlorpromazine (30.5%), aripiprazole (37.5%), and perphenazine (68.7%) in effluent discharges, and for chlorprothixene (35.4%) and flupentixol (98.8%) in surface waters. Elevated aquatic hazards for relatively understudied antipsychotics were identified, which highlight important data gaps for future environmental chemistry and toxicology research."

Journal • Review • CNS Disorders • Psychiatry

Identification of Potential Treatments for Acute Lymphoblastic Leukemia through Integrated Genomic Network Analysis. (PubMed, Pharmaceuticals (Basel)) - "Based on potentially druggable genes that we identified, palbociclib, sirolimus, and tacrolimus were under clinical trial for ALL. Additionally, chlorprothixene, sirolimus, dihydroergocristine, papaverine, and tamoxifen are the top five drug repositioning candidates for ALL according to the CMap score with dasatinib as a comparator. In conclusion, this study determines the practicability and the potential of integrated genomic network analysis in driving drug discovery in ALL."

Journal • Acute Lymphocytic Leukemia • Hematological Malignancies • Leukemia • Oncology • T Acute Lymphoblastic Leukemia • ARID5B

Association of In Utero Antipsychotic Medication Exposure With Risk of Congenital Malformations in Nordic Countries and the US. (PubMed, JAMA Psychiatry) - "In this study, considering the evidence from primary and sensitivity analyses and inevitable statistical noise for very rare exposure-outcome combinations, in utero antipsychotic exposure generally was not meaningfully associated with an increased risk of malformations. The observed increased risks of oral clefts associated with olanzapine, gastroschisis, and other specific brain anomalies with atypical antipsychotics and cardiac malformations with chlorprothixene requires confirmation as evidence continues to accumulate."

Journal • Cardiovascular • CNS Disorders • Gastrointestinal Disorder • Mental Retardation • Psychiatry • Rare Diseases • Ventriculomegaly

Comparative Effectiveness of Medications in Bipolar Disorder in Real-World Settings Based on 60,045 Patients (ACNP 2022) - "The medications associated with lower risk of psychiatric hospitalizations were olanzapine LAI (aHR 0.54, 95% CI 0.37-0.80), haloperidol LAI (aHR 0.62, 95% CI 0.47-0.81), zuclopenthixol LAI (aHR 0.66, 95% CI 0.52-0.85), lithium (aHR 0.74, 95% CI 0.71-0.76), clozapine (aHR 0.75, 95% CI 0.64 – 0.87), carbamazepine (aHR 0.81, 95% CI 0.75-0.87), levomepromazine (aHR 0.88, 95% CI 0.83-0.93), lamotrigine (aHR 0.88, 95% CI 0.85-0.92), valproic acid (aHR 0.89, 95% CI 0.87-0.92), pregabalin (aHR 0.92, 95% CI 0.86-0.98) and chlorprothixene (aHR 0.93, 95% CI 0.86-0.99)...Of the studied medications, only lithium (aHR 0.77, 95% CI 0.74-0.81) and carbamazepine (aHR 0.91, 95% CI 0.85-0.97) were associated with significantly reduced risk of non-psychiatric hospitalizations, whereas risperidone (aHR 1.07, 95% CI 1.02-1.13), olanzapine (aHR 1.10, 95% CI 1.05-1.15), quetiapine (aHR 1.10, 95% CI 1.07-1.13), haloperidol (aHR 1.12, 95% CI 1.03-1.22), melperone (aHR 1.19, 95% CI 1.03-1.35),..."

Clinical • HEOR • Real-world evidence • Alzheimer's Disease • Bipolar Disorder • CNS Disorders • Dementia • Mental Retardation • Mood Disorders • Psychiatry • Schizophrenia

Machine Learning Enabled Structure-Based Drug Repurposing Approach to Identify Potential CYP1B1 Inhibitors. (PubMed, ACS Omega) - "In particular, some commonly used anticancer medicines, including docetaxel, tamoxifen, imatinib, cisplatin, and paclitaxel, are inactivated by CYP1B1. From the in vitro analysis, it was observed that chlorprothixene, nadifloxacin, and ticagrelor showed promising inhibitory activity toward CYP1B1 in the IC range of 0.07-3.00 μM. These new chemical scaffolds can be explored as adjuvant therapies to address CYP1B1-mediated drug-resistance problems."

Journal • Oncology • CYP1B1

Comparative effectiveness of mood stabilizers and antipsychotics in the prevention of hospitalization after lithium discontinuation in bipolar disorder. (PubMed, Eur Neuropsychopharmacol) - "Of antipsychotic monotherapies, the use of long-acting injectable (LAI) antipsychotics (HR = 0.48, 95% CI = 0.26 - 0.88) and chlorprothixene (HR = 0.62, 95% CI = 0.44 - 0.88) were associated with lower risk and the use of quetiapine (HR = 1.26, 95% CI = 1.07 - 1.48) and oral olanzapine (HR = 1.23, 95% CI = 1.01 - 1.49) with higher risk of psychiatric hospitalizations than nonuse of antipsychotics...The results suggest that antipsychotic LAIs are especially effective in the prevention of psychiatric hospitalizations after lithium discontinuation. The need to alter used medications may be the lowest when lithium is restarted."

HEOR • Journal • Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry

Use of chlorprothixene and the risk of diabetes and major adverse cardiovascular events: a nation-wide cohort study. (PubMed, Basic Clin Pharmacol Toxicol) - "Cumulative dose of chlorprothixene ≥6000mg was associated with increased risk of diabetes (OR:1.15-1.63;test for trend:p<0.001), whereas cumulative dose of chlorprothixene ≥1500mg was associated with increased risk of MACE (OR:1.10-1.85;test for trend:p<0.001). In conclusion, low-dose chlorprothixene use is associated with increased risk of cardiometabolic adverse events compared to low-dose quetiapine use."

Adverse events • Journal • Cardiovascular • CNS Disorders • Diabetes • Metabolic Disorders • Myocardial Infarction

Development, validation, and application of a simple UPLC-MS/MS method for simultaneous quantification of five traditional antipsychotics in human plasma. (PubMed, Biomed Chromatogr) - "A UPLC-MS/MS method was developed to determine the levels of five traditional antipsychotics (chlorprothixene, perphenazine, fluphenazine, thioridazine, and promethazine) in human plasma with carbamazepine as the internal standard (IS). The recoveries of five drugs are in the range of 70-109%. The results of methodology verification indicate that this method is simple, economical, and sensitive, and suitable for the simultaneous quantification of five traditional antipsychotics in human plasma."

Journal • CNS Disorders

Drug Repurposing Screen for Compounds Inhibiting the Cytopathic Effect of SARS-CoV-2. (PubMed, Front Pharmacol) - "Chlorprothixene, methotrimeprazine, and piperacetazine were the three most potent FDA-approved drugs with anti-SARS-CoV-2 activities. These three compounds have not been previously reported to have anti-SARS-CoV-2 activities, although their antiviral activities against SARS-CoV and Ebola virus have been reported. These results demonstrate that this comprehensive data set is a useful resource for drug repurposing efforts, including design of new drug combinations for clinical trials for SARS-CoV-2."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Repurposing of Antipsychotic Trifluoperazine for Treating Brain Metastasis, Lung Metastasis and Bone Metastasis of Melanoma by Disrupting Autophagy Flux. (PubMed, Pharmacol Res) - "Moreover, the colocalization of LC3 with lysosomal-associated membrane protein 1 (LAMP1), a lysosome marker, was also suppressed after TFP treatment, suggesting that TFP might block the fusion of autophagosomes with lysosomes, which led to autophagosome accumulation. Taken together, our data highlight the potential of repurposing TFP as a new adjuvant drug for treating melanoma patients with brain, lung, and bone metastases."

IO Biomarker • Journal • CNS Disorders • Lung Cancer • Melanoma • Oncology • Psychiatry • Schizophrenia • Solid Tumor

Electromembrane extraction of chlorprothixene, haloperidol and risperidone from whole blood and urine. (PubMed, J Chromatogr A) - "The limit of detection (LOD) and accuracy for all the targets ranged from 0.2-0.6 ng mL and 102%-110%, respectively, and the repeatability at low (1 ng mL), medium (10 ng mL) and high (200 ng mL) concentration was ≤ 12% (RSD). Finally, the validated approach was successfully used to determine chlorprothixene, risperidone and haloperidol in whole blood and urine from rats, which were treated with chlorprothixene, risperidone and haloperidol at low therapeutic dose, respectively."

Journal • CNS Disorders

Trends in utilization and dosing of antipsychotic drugs in Scandinavia: comparison of 2006 and 2016. (PubMed, Br J Clin Pharmacol) - "There is an increased prevalence of antipsychotic prescriptions that coincides with low and/or decreasing mean doses of the majority of commonly used antipsychotics in Scandinavia. Of all antipsychotics, this development was most pronounced for quetiapine. Reasons for and consequences of increased antipsychotic use that lasts shorter periods of time requires further study."

Journal • CNS Disorders

Development of a method of hollow fiber-based solid-phase microextraction followed by ultra performance liquid chromatography-tandem mass spectrometry for determination of five antipsychotics in human whole blood and urine. (PubMed, J Chromatogr A) - "Under the optimum experimental conditions, this method allowed for determination of five antipsychotics in human whole blood with excellent limits of quantification (LOQs) (25.0, 12.5, 25.0, 25.0 and 12.5 pg mL for perphenazine, chlorpromazine, chlorprothixene, promethazine and trifluoperazine, respectively). The proposed method was compared with other methods from the literature and the results demonstrate that it is a simple, sensitive, efficient and green technique. It is suitable for analyzing trace target analytes in complex matrices such as biological samples and can provide a reliable tool for drug monitoring especially in forensic analysis and case of drug abuse."

Journal • CNS Disorders

Different number of contraindications between summaries of product characteristics (SmPC) of drugs with the same active ingredients - an analysis of data from SmPCs of neuropsychiatric drugs (PubMed, Fortschr Neurol Psychiatr) - "In numerous (neuro-)psychopharmacologic substances differences exists between the SmPCs of the associated same-substance medications regarding the number of CIs. Due to the outstanding evaluation of content aspects of these differences and legal evaluation the relevance of this result for clinical practice is not yet clear."

Journal • CNS Disorders • Dementia • Psychiatry

[VIRTUAL] Trends in prevalence and mean doses of commonly used antipsychotic drugs in Scandinavia: A multi-national drug utilization study (EPA 2020) - "In 2006, chlorprothixene and levomepromazine were the most commonly used antipsychotics...Mean doses of quetiapine decreased markedly during the 11-year study period (0.46 to 0.28 DDD/user/day), while mean doses for clozapine and olanzapine remained high (0.90-1.07 resp... We found an increasing prevalence of antipsychotic prescriptions that coincides with low and/or decreasing mean doses of the majority of commonly used antipsychotics in Scandinavia. Of all antipsychotics, this development was most pronounced for quetiapine. Reasons for and consequences of increased antipsychotic use that lasts shorter periods of time requires further study."

Hair analysis of antidepressants and antipsychotics - overview of quantitative data. (PubMed, Drug Test Anal) - "On the other hand, clozapine, haloperidol, amitriptyline, nortriptyline, risperidone and its metabolite, methylphenidate, citalopram, chlorpromazine, chlorprothixene and quetiapine had a well-founded database as these substances were investigated in controlled dose studies with higher case numbers. A harmonization on the investigated hair lengths as well as on the extraction protocol would be of favor to achieve better comparability. Although hair analysis research focused mainly on drugs abuse, contribution of more data on antidepressants and antipsychotics would help to gain better knowledge and assistance for other forensic investigators."

Journal • Review