Buronil (melperone) / Lundbeck - LARVOL DELTA

Sex differences of fall-risk-increasing drugs in the middle-aged and elderly: a descriptive, cross-sectional study of FDA adverse event reporting system. (PubMed, Sci Rep) - "For males, the top 3 signals with the highest ROR were fluprednidene acetate, potassium hydroxide, ketazolam (ROR: 216.86, 108.43, 108.43), while the top 3 signals with the highest IC025 were clomethiazole, piribedil, melperone (IC025: 3.31, 3.24, 2.99). We offered a series of FRIDs and suggested their sex differences in falls through the FAERS. In the future, it is essential to balance the inclusion of women and men, and analyse sex-stratified for FRIDs."

Adverse events • Journal • Observational data • Retrospective data • Cardiovascular • Musculoskeletal Diseases

Second-generation antipsychotics for Parkinson's disease psychosis: A systematic review and network meta-analysis. (PubMed, Gen Hosp Psychiatry) - "For patients with PDP, clozapine may substantially reduce psychotic symptoms with minimal abnormal movement, high acceptability, and moderate overall tolerability. Pimavanserin, not quetiapine, could be an alternative."

Journal • Retrospective data • Review • CNS Disorders • Movement Disorders • Parkinson's Disease • Psychiatry

Morphine concentrations in fatalities after palliative treatment of acute burn injury. (PubMed, Int J Legal Med) - "Besides morphine, propofol, fentanyl, sufentanil, midazolam, diazepam, lorazepam, cefazolin, and rocuronium were detected in femoral blood...Further evidence of therapeutic concentrations of quetiapine, duloxetine, and melperone could be matched to preexisting medication of the individuals...However, this prediction is not sufficient to explain the high morphine concentrations in femoral blood measured here. It can be assumed that burn shock in particular leads to altered pharmacokinetics, namely decreased distribution of morphine."

Journal • Palliative care • Thermal Injury

Sustainable Electrochemical Benzylic C-H Oxidation Using MeOH as an Oxygen Source. (PubMed, ChemSusChem) - "Mechanistic investigations by control experiments, radical scavenging experiments, electron paramagnetic resonance (EPR), kinetic studies, cyclic voltammetry (CV), and in-situ Fourier transform infrared (FTIR) spectroscopy support a pathway involving the formation and transformation of benzyl methyl ether via hydrogen atom transfer (HAT) and single-electron transfer (SET). The practical application of our strategy is highlighted by the successful synthesis of five pharmaceuticals, namely lenperone, melperone, diphenhydramine, cinnarizine, and flunarizine."

Journal

Iron-catalyzed β-hydroxymethylative carbonylation of styrene under photo-irradiation. (PubMed, Chem Commun (Camb)) - "Particularly, several drug-like molecules, such as melperone analogue, lenperone analogue, and haloperidol analogue, are synthesized. In addition, this method is also applicable to the synthesis of natural product (R)-atomoxetine."

Journal

Solvent-promoted photochemical carbonylation of benzylic C-H bonds under iron catalysis. (PubMed, Org Biomol Chem) - "It is shown that the reaction proceeds via a four-electron-transfer pathway, and a benzylic cation seems to be the crucial reactive species. The method is applied for the synthesis of pomalyst, haloperidol, melperone, and lenperone."

Journal

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

"#CardioTwitter for #hematology: Drug-induced long-QT by... Tacrolimus Pentamidin Foscarnet Grani/Ondansetron MCP Olanzapin Melperon Clemastin Diphenhydramin Amiodaron Azithro/Clarithro/Erythromycin Chinolones Cotrimoxazol Clindamycin Azoles #IDtwitter #MedTwitter #ESCCongress" (@NicoGagelmann)

Cardiovascular • Hematological Disorders

CHRONIC INSOMNIA SECONDARY TO SEVERE NOCTURNAL VISUAL HALLUCINATIONS IN CHARLES BONNET SYNDROME; A CHALLENGING CASE TO MANAGE (SLEEP 2022) - "His insomnia was then treated with once nightly temazepam, in addition to as needed diazepam. Treatment of Charles Bonnet syndrome is multifactorial and includes maintaining optimal eye care, stimulating senses, psychosocial therapy, and pharmacotherapy. Insomnia from release hallucinations remains difficult to manage, though GABA-A receptor agonists have shown some relief. Case reports of atypical antipsychotics and antidepressants, including melperone and agomelatine respectively, have demonstrated ability to improve release hallucinations."

Clinical • CNS Disorders • Insomnia • Migraine • Psychiatry • Sleep Disorder

Interpretation of melperone intoxication: post-mortem concentration distribution and interpretation of intoxication data. (PubMed, Drug Metab Pers Ther) - "The lethal reference concentration of melperone in femoral blood of 17.1 mg/L pointed out in different reference lists should be used with caution. Instead, a lower lethal melperone concentration should be considered. The post-mortem concentration distribution of the drug presented could be helpful in the interpretation of cases where no blood samples are available."

Journal

The Dopaminergic Neuronal System Regulates the Inflammatory Status of Mouse Lacrimal Glands in Dry Eye Disease. (PubMed, Invest Ophthalmol Vis Sci) - "Using flow cytometry and ELISA, immune cell infiltration and inflammatory cytokine expression were determined in DE-induced LGs with or without DR blockers, SCH-23390 (DR1i), or melperone (DR2i). Upregulation of DR1 and DR2 was observed in DE-induced mouse LGs. As the inflammatory conditions are aggravated by the inhibition of DRs, especially DR2, their activity may be an important factor preserving ocular surface homeostasis."

Journal • Preclinical • Corneal Abrasion • Dry Eye Disease • Immunology • Inflammation • Ocular Inflammation • Ophthalmology • CD19 • IFNG • IL17A • TNFA

Interpretation of melperone intoxication: post-mortem concentration distribution and interpretation of intoxication data. (PubMed, Drug Metab Pers Ther) - "The lethal reference concentration of melperone in femoral blood of 17.1 mg/L pointed out in different reference lists should be used with caution. Instead, a lower lethal melperone concentration should be considered. The post-mortem concentration distribution of the drug presented could be helpful in the interpretation of cases where no blood samples are available."

Journal

Pharmacodynamic Drug-Drug interactions of QT-prolonging drugs in hospitalized psychiatric patients. (PubMed, J Neural Transm (Vienna)) - "Most frequently prescribed psychotropic high-risk drugs (n = 48,995) were the antipsychotics pipamperone (n = 6202), quetiapine (n = 5718), prothipendyl (n = 4298), and risperidone (n = 4265). The replacement of high-risk drugs such as tricyclic antidepressants, levomepromazine, melperone, and promethazine with more tolerable drugs could avoid 11% of QT-prolonging drugs and increase the tolerability of psychopharmacological treatment. More than 80% of psychiatric patients receive at least one QT-prolonging drug during their hospital stay, and almost 50% of these drugs are combined in clinical practice. For the prevention of cardiac ADRs, the physician should evaluate the risk for QT prolongation for each drug and patient-specific risk factors before prescribing these drugs or drug combinations."

Clinical • Journal • PK/PD data • CNS Disorders • Psychiatry

Identification and Quantification of Antipsychotics in Blood Samples by LC-MS-MS: Case Reports and Data from Three Years of Routine Analysis. (PubMed, J Anal Toxicol) - "A quantitative liquid chromatography-tandem mass spectrometry (LC-MS-MS) assay was developed for the simultaneous determination of 16 AP (amisulpride, aripiprazole, chlorpromazine, clozapine, cyamemazine, fluphenazine, haloperidol, levomepromazine, melperone, olanzapine, paliperidone, promethazine, quetiapine, risperidone, sulpiride, ziprasidone) in blood samples of postmortem cases. Our results point that antipsychotics are an increasingly prevalent class of drugs. Antipsychotic drugs must be measured not only in toxic concentrations but also in therapeutic levels in postmortem cases therefore, the importance of a sensitive method to cover the low therapeutic range in which AP are usually present."

Clinical • Journal • CNS Disorders • Psychiatry • Schizophrenia

Prevalence and sort of pharmacokinetic drug-drug interactions in hospitalized psychiatric patients. (PubMed, J Neural Transm (Vienna)) - "The most frequently prescribed CYP inhibitors were melperone (n = 2504, 28.1%) and duloxetine (n = 1324, 14.9%)...Carbamazepine was the most frequently prescribed CYP inducer (n = 733, 88.8%)...The frequency of CYP-mediated DDI is considerably high in the psychiatric setting. Physicians should be aware of the CYP inhibitory and inducing potential of psychotropic and internistic drugs (especially, melperone)."

Clinical • Journal • PK/PD data • CNS Disorders • Psychiatry

Lurasidone Improves Psychopathology and Cognition in Treatment-Resistant Schizophrenia. (PubMed, J Clin Psychopharmacol) - "In addition to clozapine, other atypical antipsychotic drugs pharmacologically similar to clozapine, for example, olanzapine, risperidone, and melperone, are also effective in a similar proportion of treatment-resistant schizophrenia (TRS) patients, ~40%. In addition, this study demonstrated that 80 mg/d lurasidone, an effective and tolerable dose for non-TRS patients, was also effective in TRS patients but required longer duration of treatment. Direct comparison of lurasidone with clozapine in TRS patients is indicated."

Journal • CNS Disorders • Schizophrenia

The Impact of Antipsychotic Drugs on Long-term Care, Nursing Home Admission and Death among Dementia Patients. (PubMed, J Gerontol A Biol Sci Med Sci) - "Cox proportional hazards models were estimated to explore whether the risk of these outcomes differed between patients receiving haloperidol, melperone, risperidone, or quetiapine. In our study, APDs appeared to accelerate adverse health outcomes in German dementia patients. Differentiating between the effect of antipsychotic drug use among dementia patients residing in private households and in nursing homes, we found that excess mortality for haloperidol and melperone users was higher in private settings."

Journal

ELECTROCONVULSIVOTHERAPY (ECT) IN AUTISM SPECTRUM DISORDER (ASD) (WPA 2019) - "Nowadays, ECT occurs every five weeks, while taking the oral medication (olanzapine, sodium valproate and diazepam). A 29 years-old male patient was diagnosed with ASD and focal epilepsy at the age of 2 years-old. He had history of aggression and self-injury behaviours since childhood. Besides sodium valproate and lamotrigine prescribed for epilepsy, risperidone, paliperidone, cloropromazine, levomepromazine, melperone, diazepam and clonidine were tried."

Altered orientation and aggressiveness in an 89-year-old woman (PubMed, Internist (Berl)) - "Inspection of the urine and laboratory findings pointed towards an acute exacerbation of acute intermittent porphyria as a possible cause of the delirium. After discontinuation of melperone with additional parenteral therapy with physiological fluids, the signs of delirium significantly improved."

Clinical • Journal

ELECTROCONVULSIVE THERAPY (ECT) FOR TREATMENT RESISTANT SCHIZOAFFECTIVE DISORDER. (EPA 2019) - "...Results :Since 2009, in the patient's case, the following psychotropic drugs have been used in sufficient dosage and in sufficient time: benperidol, melperone, risperidone, paliperidone, olanzapine, clozapine, amisulpride, ziprasidone, mirtazapine, doxepin, benzodiazepines...67 old patient with schizoaffective disorder has been received to psychiatric ward. Due to lack of response to pharmacotherapy treatment, electroconvulsive therapy was used. There were carried out, as required, a total of 8 treatments EKT- through bilateral stimulation starting with 20% to 80% of max."