asenapine / Generic mfg. - LARVOL DELTA

Serotonin Syndrome Associated With High-dose Diphenhydramine Use Complicating Abdominoplasty and Mastopexy. (PubMed, Plast Reconstr Surg Glob Open) - "The patient was on multiple serotonergic medications, including duloxetine, asenapine, and trazodone, in addition to high-dose diphenhydramine. Postoperatively, she developed tachycardia, leukocytosis, respiratory distress, and elevated lactate, initially leading to concerns of sepsis; however, further evaluation revealed the likely diagnosis of serotonin syndrome, triggered by the combination of serotonergic agents and intraoperative fentanyl...The interaction between our patient's chronic diphenhydramine abuse and multiple other serotonergic medications likely precipitated this condition. Preoperative medication reconciliation, early recognition of triggers and signs, and prompt intervention are key to preventing adverse outcomes in serotonin syndrome."

Journal • Aesthetic Medicine • Cardiovascular • Critical care • Infectious Disease • Psychiatry • Septic Shock

Antipsychotic drug dosing and study discontinuation in schizophrenia: A systematic review and dose-response meta-analysis. (PubMed, Eur Neuropsychopharmacol) - "Dose discontinuation curves varied between the antipsychotics and included U-shaped, monotonic, and hyperbolic patterns. Future studies should consistently present disease-related and side-effect-related dropouts due to adverse events separately."

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

Unraveling the Molecular Architecture of Mosquito D1-Like Dopamine Receptors: Insights Into Ligand Binding and Structural Dynamics for Insecticide Development. (PubMed, Proteins) - "The binding energy of dopamine is observed to be ~2-3 kcal/mol higher than that of the antagonist molecules amitriptyline, asenapine, and flupenthixol in mosquito DARs. These antagonist molecules bind to EBP, which obstructs dopamine movement toward the active site, thereby inhibiting signal transduction. Our findings elucidate the molecular architecture of the binding pockets and the versatility of DARs in accommodating diverse ligands, providing a foundational framework for future drug and insecticide development."

Journal

Identification of the atypical antipsychotic Asenapine as a direct survivin inhibitor with anticancer properties and sensitizing effects to conventional therapies. (PubMed, Biomed Pharmacother) - "Therapy resistance in human cancers is a major limitation in Clinical Oncology. Finally, a synergistic anticancer effect was detected in vitro when combined with different conventional chemotherapies, and in vivo studies showed higher antitumor effects when combined with cisplatin. Altogether, our results identify AM as a specific direct binding inhibitor of survivin, showing anticancer properties in vitro and in vivo and sensitizing effects when combined with cisplatin, opening the possibility of repositioning this approved drug for cancer treatment."

Journal • Brain Cancer • CNS Disorders • Lung Cancer • Oncology • Solid Tumor • BIRC5

Unlocking the secrets of trace amine-associated receptor 1 agonists: new horizon in neuropsychiatric treatment. (PubMed, Front Psychiatry) - "Recent cryogenic electron microscopic (cryo-EM) structures of human and mouse TAAR1 (hTAAR1 and mTAAR1, respectively) in complex with agonists and G proteins have revealed detailed atomic insights into the binding pockets, binding interactions and binding modes of several agonists including endogenous trace amines (β-phenylethylamine, 3-Iodothyronamine), psychostimulants (amphetamine, methamphetamine), clinical compounds (ulotaront, ralmitaront) and repurposed drugs (fenoldopam). The in vitro screening of drug libraries has also led to the discovery of novel TAAR1 agonists (asenapine, guanabenz, guanfacine) which can be used in clinical trials or further developed to treat different neuropsychiatric conditions...In this review, we discuss the emergence of structure-based approaches in the discovery of novel TAAR1 agonists through drug repurposing strategies and structure-guided designs. Additionally, we discuss the functional selectivity of TAAR1 signalling, which..."

Journal • Review • Bipolar Disorder • CNS Disorders • Cognitive Disorders • Depression • Mental Retardation • Mood Disorders • Psychiatry • Schizophrenia

Pediatric Bipolar Disorder: Challenges in Diagnosis and Treatment. (PubMed, Paediatr Drugs) - "Converging evidence from disparate sites describe a developmentally distinct presentation of bipolar disorder in youth that is highly morbid, persistent and responds to treatment with the mood stabilizer medications used in the treatment of adult bipolar disorder, such as divalproex sodium and carbamazepine. Some are additionally approved for use in pediatric populations including, for manic or mixed states, risperidone, aripiprazole, and asenapine for those aged 10-17 years and also including lithium and olanzapine for ages 13-17 years. Quetiapine is approved as monotherapy or as adjunct to lithium or divalproex sodium for manic states in those aged 10-17 years...While an array of mood-stabilizing medications is available for treatment, such as second-generation antipsychotics, lithium, and anticonvulsants, these can be only partially effective and fraught with annoying and serious side effects. This article will review current practice in the diagnosis..."

Journal • Bipolar Disorder • CNS Disorders • Developmental Disorders • Mood Disorders • Pediatrics • Psychiatry

Exploring peptide dendrimers for intestinal lymphatic targeting: formulation and evaluation of peptide dendrimer conjugated liposomes for enhancing the oral bioavailability of Asenapine maleate. (PubMed, Sci Rep) - "Asenapine maleate (ASPM) is a second-generation atypical antipsychotic that is approved for treating acute schizophrenia and bipolar disorder in adults by the US FDA. The pharmacokinetic parameters of the developed liposomal formulation were evaluated using pharmacokinetic studies on Sprague- Dawley (SD) rats. The psychostimulant-induced hyperactivity model was used to evaluate the pharmacodynamic performance of the developed formulations by measuring the reversal of hyperlocomotor activity induced by levodopa-carbidopa."

Journal • Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry • Schizophrenia • PD-1

A phase II study of ME2136 (Asenapine Maleate) plus standard antiemetic therapy for patients, including diabetic patients, receiving cisplatin-based chemotherapy. (PubMed, Invest New Drugs) - "Olanzapine combined with the neurokinin-1 receptor antagonist, palonosetron and dexamethasone is the standard treatment for chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). This study was registered with the Japan Registry of Clinical Trials (jRCT2041200071) on 10 December 2020. Clinical trial registration: This study was registered with the Japan Registry of Clinical Trials (jRCT2041200071) on 10 December 2020."

Journal • P2 data • Chemotherapy-Induced Nausea and Vomiting • CNS Disorders • Diabetes • Metabolic Disorders • Oncology • Solid Tumor

A disproportionality analysis of antipsychotic-induced hyperprolactinemia based on FDA adverse event reporting system. (PubMed, Int J Clin Pharmacol Ther) - "Risperidone had the greatest risk of increasing prolactin, whereas clozapine had the lowest. Antipsychotic-induced hyperprolactinemia was more common in women and middle-aged patients. Clozapine had the shortest onset time in raising prolactin, whereas cariprazine had the longest."

Adverse events • Journal • CNS Disorders

Acute Pharmacologic approach to DSM-V Manic Episodes with Mixed Features in Bipolar Disorder: A review (ECNP 2024) - "Evidence suggests the use of Asenapine, Cariprazine and Aripiprazole as well as Divalproex in the management of DSM-V Manic Episodes with MF. Other recommendations are Olanzapine, Olanzapine/divalproex and Ziprasidone. Risperidone and FGAs are not recommended."

Review • Bipolar Disorder • CNS Disorders • Depression • Major Depressive Disorder • Mood Disorders • Psychiatry

Antipsychotic-induced prolactin variation: a systematic review and dose-response meta-analysis (ECNP 2024) - "Our dose-response curves depicted that the evolvement of prolactin in aripiprazole, cariprazine, and lumateperone had a negative relationship with the taken doses (the lowest point was -6.37ng/mL at 14.7mg/d, -3.40ng/mL at 8.7mg/d, -3.6ng/mL at 120mg/d, respectively). Quetiapine carried negligible risks for prolactin growth across examined doses (prolactin change between -0.87 to 1.55ng/mL within 1144mg/d). While most of the other antipsychotics had their risks of prolactin rise with increasing doses and then continued to step-up(the maximum point was asenapine 10.44ng/mL at 20mg/d, iloperidone 10.18ng/mL at 24mg/d, lurasidone 17.91ng/mL at 240mg/d, olanzapine 14.97ng/mL at 40mg/d, risperidone 159.92ng/mL at 12mg/d), plateaued(the maximum point was paliperidone 50.97ng/mL at 12mg/d, ziprasidone 8.07ng/mL at 200mg/d) or even declined(the maximum point for brexpiprazole was 2.11ng/mL at 1.7mg/d, haloperidol was 22.56ng/mL at 8.6mg/d)...However, the extent of prolactin..."

Retrospective data • Review • CNS Disorders • Psychiatry • Schizophrenia

Real-World Effectiveness, Economic, and Humanistic Outcomes of Selected Oral Antipsychotics in Patients with Schizophrenia: A Systematic Review Evaluating Global Evidence. (PubMed, Clinicoecon Outcomes Res) - "Our systematic review aimed to synthesize literature describing real-world effectiveness, economic, and humanistic outcomes of OATs (asenapine, brexpiprazole, cariprazine, iloperidone, lumateperone, lurasidone, olanzapine/samidorphan, paliperidone, and quetiapine) for successful management of the disease. Medication non-adherence and treatment discontinuation were predominant factors contributing to the economic burden of schizophrenia. Our research showcased a significant knowledge gap across OATs spanning the humanistic and behavioral outcomes and medication adherence and switching, suggesting a need for robust evidence generation to help clinicians and payers make informed decisions regarding treatment opportunities and cost-effective strategies for patients with schizophrenia."

Journal • Real-world • Real-world effectiveness • Real-world evidence • Review • CNS Disorders • Psychiatry • Schizophrenia

Characteristics of eye disorders induced by atypical antipsychotics: a real-world study from 2016 to 2022 based on Food and Drug Administration Adverse Event Reporting System. (PubMed, Front Psychiatry) - "Common atypical antipsychotics include risperidone, paliperidone, olanzapine, lurasidone, quetiapine, clozapine, aripiprazole, ziprasidone, asenapine, brexpiprazole, and cariprazine. In terms of the types of adverse events, our study found that aripiprazole was associated with 28 types of ocular adverse events, followed by quetiapine. Clozapine was only associated with two types of ocular adverse events."

Adverse events • Journal • Real-world • Real-world evidence • Cataract • CNS Disorders • Ophthalmology

Safety assessment of asenapine in the FAERS database: real adverse event analysis and discussion on neurological and psychiatric side effects. (PubMed, BMC Pharmacol Toxicol) - "Asenapine carries the risk of various adverse reactions alongside its therapeutic effects. In clinical practice, physicians should closely monitor the occurrence of neurological disorders, psychiatric disorders, and gastrointestinal system disorders."

Adverse events • Journal • Bipolar Disorder • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Mental Retardation • Mood Disorders • Psychiatry • Schizophrenia

Systematic Review and Network Meta-Analysis: Efficacy and Safety of Antipsychotics vs Antiepileptics or Lithium for Acute Mania in Children and Adolescents. (PubMed, J Am Acad Child Adolesc Psychiatry) - "SGAs are more efficacious than placebo and MSs in treating acute mania symptoms, however, their use must be carefully weighed against important side effects."

Journal • Retrospective data • Review • Anesthesia • Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry

Predictors of continuation for asenapine from real-world data in patients with schizophrenia. (PubMed, Ann Gen Psychiatry) - "Our findings shed light on distinct patient-related predictors of asenapine continuation, deviating from those observed with other antipsychotic medications. This underscores the necessity of recognizing that predictive factors for antipsychotic medication continuation vary across different agents. Moving forward, elucidating these predictive factors for various antipsychotic medications holds paramount importance in schizophrenia treatment, facilitating the delivery of tailored therapeutic interventions for individual patients."

Journal • Real-world • Real-world evidence • CNS Disorders • Psychiatry • Schizophrenia

Sublingual asenapine for agitation in malabsorptive states: three patient cases. (PubMed, Ther Adv Psychopharmacol) - "Clinicians should consider the use of SL asenapine for medically complex agitated patients where gastric absorption is questionable. There is an urgent need for guidelines on this matter, as well as more, alternative dosage forms for various medications that may help with agitation in this population."

Journal • Bipolar Disorder • CNS Disorders • Gastrointestinal Disorder • Mood Disorders • Psychiatry • Short Bowel Syndrome

Iloperidone (Fanapt) - a new indication for bipolar disorder. (PubMed, Med Lett Drugs Ther) - No abstract available

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

Structure-based virtual screening study for identification of potent insecticides against Anopheles gambiae to combat the malaria. (PubMed, J Vector Borne Dis) - "The screening demonstrated strong binding and interactions with active site residues of DOP2 for five compounds: Diclazuril, Kaempferol, Deracoxib, Clindamycin, and Diaveridine. These compounds exhibited higher binding affinity values compared to the control (Asenapine)...These compounds show promise as potential new insecticides targeting A. gambiae mosquito by inhibiting the DOP2 protein. However, additional experimental validation is required to optimize their efficacy as DOP2 inhibitors."

Journal • Infectious Disease • Malaria

Comparative physiological effects of antipsychotic drugs in children and young people: a network meta-analysis. (PubMed, Lancet Child Adolesc Health) - "Children and adolescents show varied but clinically significant physiological responses to individual antipsychotic drugs. Treatment guidelines for children and adolescents with a range of neuropsychiatric and neurodevelopmental conditions should be updated to reflect each antipsychotic drug's distinct profile for associated metabolic changes, alterations in prolactin, and haemodynamic alterations."

Clinical • Journal • Retrospective data • CNS Disorders • Psychiatry

The effect of new atypical antipsychotic drugs on the expression of transcription factors regulating cytochrome P450 enzymes in rat liver. (PubMed, Pharmacol Rep) - "Prolonged treatment with asenapine, iloperidone, or lurasidone affects the expression of transcription factors regulating the CYP drug-metabolizing enzymes. The changes in the expression of AhR, CAR, and PXR mostly correlate with alterations in the expression and activity of respective CYP enzymes found in our previous studies. Since these transcription factors are also engaged in the expression of phase II drug metabolism and drug transporters, changes in their expression may affect the metabolism of endogenous substrates and pharmacokinetics of concomitantly used drugs."

Journal • Preclinical • CNS Disorders • AHR • PPARG

An overview of the efficacy and safety of brexpiprazole for the treatment of schizophrenia in adolescents. (PubMed, Expert Rev Neurother) - "Two previous agents (asenapine and ziprasidone) approved for adult schizophrenia failed to separate from placebo in adolescent schizophrenia studies; this partially undermines the process of extrapolation. For brexpiprazole, the paucity of data in adolescents relegates it to second-line agent. More research on brexpiprazole is needed to delineate its relative role in the management of adolescent schizophrenia."

Journal • Review • CNS Disorders • Psychiatry • Schizophrenia

Fixed-dose Safety and Efficacy Study of Asenapine for the Treatment of Acute Manic or Mixed Episode in Bipolar 1 Disorder (P05691) (clinicaltrials.gov) - P3 | N=367 | Completed | Sponsor: Organon and Co | Phase classification: P3b ➔ P3

Phase classification • Bipolar Disorder • CNS Disorders • Psychiatry

Mining clinical data for novel medications to treat alcohol use disorder. (PubMed, J Subst Use Addict Treat) - "Most medications significantly associated with decreased alcohol consumption in our analysis were either contraindicated with alcohol or likely attributable to patients abstaining from alcohol due to severe illness. However, the large effect of asenapine is notable, and a worthwhile candidate for more careful analysis."

Clinical data • Journal • Addiction (Opioid and Alcohol) • Chronic Kidney Disease • CNS Disorders • Diabetes • Hepatitis C • Hepatology • Infectious Disease • Metabolic Disorders • Nephrology • Oncology • Renal Disease

Drugs for bipolar disorder. (PubMed, Med Lett Drugs Ther) - No abstract available

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