asenapine / Generic mfg. - LARVOL DELTA

Grading the Evidence- Bipolar Disorder and Schizophrenia (AACAP 2025) - "FDA approval will also be part of the metric in helping to determine recommendations. Multiple studies are available that are funded by the NIH and FDA for psychosis (primarily schizophrenia) that show high levels of evidence, ie, grades 1A and 1B for benefit with tolerable side effects including newer medications such as lurasidone. Other medications have good efficacy but higher side-effect burdens such as clozapine. Finally, some medications have inadequate separation from placebo and are not approved, such as ziprasidone and asenapine... The field of psychopharmacology for bipolar and psychotic disorders has a number of completed controlled trials that contribute to the evidence base. Clinicians can use the GRADE system to recommend medications based on the balance of efficacy vs adverse event burden to obtain symptom control.BRD, PSY, PTA"

Bipolar Disorder • CNS Disorders • Depression • Mood Disorders • Pediatrics • Psychiatry • Schizophrenia

Bipolar disorder in children, adolescents and young adults. Part 2. Therapeutic management. Recommendations under the patronage of the Executive Board of the Polish Psychiatric Association, National Consultants in the field of Psychiatry and National Consultants in Child and Adolescent Psychiatry. (PubMed, Psychiatr Pol) - "Lithium, aripiprazole, quetiapine, risperidone, olanzapine, asenapine, ziprasidone are recommended for the treatment of mania and mixed states. For the treatment of depressive episodes in bipolar disorder in children and adolescents, experts recommend lurasidone as monotherapy or olanzapine + fluoxetine as combination therapy. Although long-term treatment is a key aspect of bipolar disorder management in children and adolescents, consistent efficacy data are still lacking. Safety data indicate that the most commonly reported adverse reactions in children and adolescents treated with mood stabilizers are gastrointestinal and neurological adverse reactions, while the use of antipsychotics is mainly associated with weight gain and sedation."

Clinical guideline • Journal • Review • Anesthesia • Bipolar Disorder • CNS Disorders • Depression • Mood Disorders • Psychiatry

Analysis of acute pancreatitis caused by multi-acting receptor-targeted antipsychotics using the Japanese claims database. (PubMed, J Affect Disord) - "These results highlight the need for careful monitoring of pancreatitis in patients receiving long-term MARTA therapy. In individuals with risk factors such as obesity, diabetes, or dyslipidemia, the use of MARTA should be considered cautiously. Early detection and appropriate management are essential to reduce the risk of serious outcomes."

Journal • CNS Disorders • Diabetes • Dyslipidemia • Genetic Disorders • Metabolic Disorders • Obesity • Pancreatitis

Glucose dysregulation signals in weight-neutral atypical antipsychotics: A pharmacovigilance-pharmacodynamic evaluation of FAERS data. (PubMed, J Affect Disord) - "Weight-neutral drugs such as ziprasidone, asenapine, lurasidone, and aripiprazole may be associated with glucose dysregulation, underscoring the need for vigilance when switching antipsychotics. This phenomenon might be attributable to their antagonistic effects on 5-HT2C receptors. However, given the exploratory nature of this study, these findings warrant further validation."

Adverse events • Journal • PK/PD data • CNS Disorders

Cults, trauma, and bipolarity: Clinical perspectives through a real case (ECNP 2025) - "The treatment plan involved discontinuing sertraline and starting asenapine 5 mg, which was poorly tolerated. It was then switched to quetiapine, increasing up to 200 mg, leading to normalization of circadian rhythms and progressive resolution of the manic episode...Findings suggest that PTSD exacerbates the outcome of bipolar disorder, as bipolar patients with PTSD are less likely to recover, experience more rapid cycling, have an increased risk of suicide attempts, and suffer from a poorer quality of life [3]. Given the limited literature on the relationship between PTSD and bipolar disorder, and the high comorbidity of both, further research is needed to establish treatment strategies tailored to these patients."

Clinical • Bipolar Disorder • CNS Disorders • Insomnia • Mood Disorders • Post-traumatic Stress Disorder • Psychiatry • Sleep Disorder • Substance Abuse

Modelling-filtered drug repurposing and first-in-protein SPR validation of histone deacetylase 4 inhibitors for Ataxia-telangiectasia. (PubMed, Biomed Pharmacother) - "Competitive assay with tasquinimod, a known HDAC4 modulator, revealed that asenapine exhibits higher affinity supporting its candidacy for further pharmacological development. These findings underscore the utility of combining repositioning pipelines with real-time affinity quantification to accelerate the discovery of selective HDAC4-targeted therapeutics for Ataxia-Telangiectasia."

Journal • Ataxia • CNS Disorders • Immunology • Movement Disorders • Primary Immunodeficiency • HDAC4

Hyperosmolar Hyperglycemic Syndrome Induced by Lurasidone: A Rare and Serious Adverse Effect (ISBD 2025) - " Case Presentation: An 81-year-old male with bipolar disorder, maintained on asenapine without notable side effects, was hospitalized due to worsening depression and suicidal tendencies. Though lurasidone is considered metabolically safer, this rare case highlights the potential for severe hyperglycemia. This case is particularly notable due to its rarity. Antipsychotics may induce hyperglycemia via insulin resistance and β-cell damage."

Adverse events • Bipolar Disorder • CNS Disorders • Depression • Mood Disorders • Psychiatry • Schizophrenia

Asenapine for aggressive behaviours in psychiatric disorders: a systematic review of efficacy and real-world effectiveness. (PubMed, Int J Psychiatry Clin Pract) - "Three studies found no advantages over olanzapine. Asenapine may be a viable option for the treatment of psychomotor agitation and hostility, although more head-to-head trials are needed to clarify its efficacy relative to other antipsychotics. Since the evidence of efficacy in other aggressive domains and diagnoses is still limited, clinicians should primarily consider the tolerability profile to guide their prescription."

Journal • Real-world evidence • Review • Bipolar Disorder • CNS Disorders • Mental Retardation • Psychiatry • Psychomotor Agitation

Point of Care Apps for Facilitating Guideline Uptake by Clinicians (WFSBP 2025) - " The preference-based tool incorporates ten first-line interventions—aripiprazole, asenapine, cariprazine, divalproate, lamotrigine, lithium, lurasidone, paliperidone, quetiapine, and risperidone—and evaluates them against 17 safety outcomes... This point-of-care app provides a promising solution to the challenges of implementing evidence-based clinical guidelines in BD care. By incorporating patient preferences and utilizing multicriteria decision analysis, the tool enhances treatment adherence, fosters personalized care, and improves clinical outcomes. It offers a more accessible and tailored approach to BD management, benefiting both clinicians and patients in everyday practice."

Clinical • Bipolar Disorder • CNS Disorders • Insomnia • Mood Disorders • Psychiatry • Sleep Disorder

Antipsychotic-Related Prolactin Changes: A Systematic Review and Dose-Response Meta-analysis. (PubMed, CNS Drugs) - "The prolactin-increasing property varies among antipsychotics, is dose-related, and is greater in females. These findings in adults with acutely exacerbated schizophrenia can help clinicians titrate and adapt antipsychotic doses and consider patients' sex in treatment decisions. The protocol was registered in the International Prospective Register of Systematic Reviews (PROSPERO); registration no. CRD42020181467."

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

Weight change from incretin-based weight loss medications across categories of second-generation antipsychotics. (PubMed, Int J Obes (Lond)) - "Semaglutide and tirzepatide induce weight loss among those prescribed SGAs, with lower effectiveness in those prescribed higher AIWG SGAs."

Journal • CNS Disorders • Diabetes • Metabolic Disorders

Sexual dysfunctions related to use of antipsychotics: A protocol for a systematic review and meta-analysis. (PubMed, PLoS One) - "The antipsychotic medications of interest are amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, chlorpromazine, clopenthixol, clozapine, droperidol, flupenthixol, fluphenazine, haloperidol, iloperidone, levomepromazine, loxapine, lurasidone, molindone, olanzapine, paliperidone, penfluridol, perphenazine, perazine, pimozide, prochlorperazine, quetiapine, risperidone, sertindole, sulpiride, thiothixene, thioridazine, trifluoperazine, ziprasidone, zuclopenthixol and zotepine. The Cochrane Risk of Bias tool and RoB 2.0 will be used to assess the risk of bias in studies. We will evaluate the quality of the evidence contributing to network estimates for the primary outcomes using the GRADE framework, and key factors that may affect the observed effects will be analysed for consistency across studies."

Journal • Retrospective data • CNS Disorders • Sexual Disorders • PRL

In Vitro Oral Cavity Permeability Assessment to Enable Simulation of Drug Absorption. (PubMed, Pharmaceutics) - " Epithelial barrier properties were monitored using propranolol and Lucifer Yellow as prototypic transcellular and paracellular markers... Apparent permeability coefficients (Papp) calculated for these APIs in the sublingual HO-1-u-1 tissue model varied from Papp = 2.72 ± 0.06 × 10-5 cm/s for asenapine to Papp = 6.21 ± 2.60 × 10-5 cm/s for naloxone. In contrast, the buccal EpiOral™ tissue model demonstrated greater discrimination power in terms of permeation properties for the same APIs, with values ranging from Papp = 3.31 ± 0.83 × 10-7 cm/s for acyclovir to Papp = 2.56 ± 0.68 × 10-5 cm/s for sufentanil... Experimental permeation data collected for selected APIs in FDA-approved oral cavity products will serve as a training set to aid the development of predictive computational models for improving algorithms that describe drug absorption from the oral cavity. Following a robust in vitro-in vivo correlation analysis, it is expected..."

Journal • Preclinical

Strategies for Switching between Oral Postsynaptic Antidopaminergic Antipsychotics in Patients with Schizophrenia: A Systematic Review. (PubMed, CNS Drugs) - "Despite the importance and frequency of antipsychotic switching, few studies have specifically investigated outcomes of different switch strategies. General clinical preference appears to utilize gradual switching approaches to avoid potential rebound symptoms. Future research with current and emerging antipsychotics is needed, especially for switching between antipsychotics with different receptor profiles and for switches that are potentially vulnerable to rebound and withdrawal symptoms."

Journal • Review • CNS Disorders • Psychiatry • Schizophrenia

RAKGEORREC: Τhe Combination of Pharmacotherapy With RECOVERYTRSGR and RECOVERYTRSBDGR. (clinicaltrials.gov) - P4 | N=40 | Recruiting | Sponsor: Dr. Stavroula Rakitzi

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

Asenapine-induced severe dystonia in a patient with schizophrenia: medication error due to sound-alike drug. (PubMed, BMJ Case Rep) - "The misinterpretation of the sound-alike drugs Azapin (clozapine) and asenapine caused an acute dystonic reaction. First, it uncovers a medication error due to a sound-alike drug and emphasises the importance of paying attention to national guidelines since first-line treatment can differ between countries. These factors combined increase the risk of medication error with potentially fatal consequences."

Journal • CNS Disorders • Dystonia • Movement Disorders • Psychiatry • Schizophrenia

Unsupervised Graph Clustering Reveals a Clinical Taxonomy of Antipsychotics (APA 2025) - "Cluster 1 contained Aripiprazole, Brexpiprazole, Cariprazine, Lurasidone, Sertindole, and Ziprasidone, and was characterized by an excellent side-effect profile but also with the lowest efficacy. Cluster 2 contained Chlorpromazine, Haloperidol, Loxapine, Molindone, Perphenazine, and Thiothixene, and showed strong efficacy in positive symptoms, but also had a high-risk for EPS, QTc prolongation and seizures. Cluster 3 contained Clozapine, Iloperidone, Olanzapine, Quetiapine, Thioridazine, and Zotepine, and showed strong overall efficacy but carried the highest risk for sedation and metabolic side effects. Cluster 4 contained Amisulpride, Asenapine, Paliperidone, Risperidone, and Sulpride, and showed excellent positive and negative symptom efficacy but carried the highest risk of hyperprolactinemia. Cluster 5 contained Flupentixol, Fluphenazine, Pimozide, and Trifluoperazine and showed the lowest efficacy with a high risk of causing EPS. Conclusion Despite traditional..."

Clinical • Anesthesia • CNS Disorders • Epilepsy • Hypotension • Psychiatry • Schizophrenia

Ergotamine enhances circadian amplitude and diurnally mitigates nitroglycerin-induced mechanical hypersensitivity. (PubMed, J Headache Pain) - "Ergotamine has substantial circadian rhythm modification effects in both cellular and animal models. Ergotamine's circadian effects appear to be mediated through serotonin 1D and 2C receptors, providing a rationale for why sub-psychedelic doses of psilocybin (which induces psychedelic responses through the serotonin 2A receptor) might be effective. Ergotamine's peak effect on hindpaw thresholds at ZT4 suggests that ergotamine may be more effective at certain times of day."

Journal • CNS Disorders • Immunology • Migraine • Pain • ARNTL • BMAL1 • CLOCK • NR1D1 • PER2

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