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Purpose: To evaluate the usefulness of asenapine sublingual tablets for the treatment of delirium in patients with advanced cancer. Methods: We conducted a retrospective study using electronic medical records of patients with advanced cancer who were admitted to our hospital between October 1, 2019 and September 30, 2022 and who received asenapine sublingual tablets as treatment for delirium. The Agitation Distress Scale (ADS) was used to evaluate the degree of improvement of agitation symptoms caused by delirium. Results: Twenty patients were included in the analysis. The mean ADS(range) before treatment was 12 (4–17), and the mean ADS(range) after treatment was 7.9 (0–18), with the p-value <0.001. Conclusion: Asenapine sublingual tablets may be useful as an option for pharmacological treatment of delirium.
ABSTRACT
Delirium occurs in 30-40% of patients with terminal cancer, and 90% of patients are delirious immediately before death. Symptoms such as agitation and hallucination are often refractory to the standard pharmacological therapy. Also, the medication options for delirium in terminally ill patients are often limited due to a difficulty in swallowing or a lack of intravenous access. We herein report a case series of six patients with terminal cancer whose derilium symptoms were treated by asenapine sublingual tablets during the intervention period by the palliative care team. Asenapine was selected when other antipsychotics were ineffective or unavailable for agitation caused by delirium. All patients suffered dyspnea or choking sensations due to dysphagia or respiratory dysfunction. Sedative effect was observed among all patients without apparent adverse events. Sublingual asenapine could be an option for the management of restlessness due to terminal delirium when both oral and intravenous drug administration routes are not available.
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Introduction: We report a case of intractable nausea of a terminal malignant lymphoma patient with diabetes, which improved by sublingual administration of asenapine. Case: A 78-year-old man suffering from diffuse large B-cell lymphoma with diabetes presented intractable nausea and vomiting. Those symptoms were thought to be due to masses and nodules in the right frontal lobe and the cerebellum, and/or due to edema in the peripheral brain parenchyma. Because it was difficult to take medicines orally, we selected injections to control those symptoms. However, the combination of metoclopramide, haloperidol, and hydroxyzine injections failed to relieve nausea. Olanzapine is effective against nausea but is contraindicated for diabetic patients, so asenapine, one of the multi-acting receptor-targeted antipsychotics the same as olanzapine, was expected alternatively. The patient was administrated asenapine sublingually 5mg once a day before bedtime. This administration of asenapine remarkably improved his nausea. Discussion: Sublingual asenapine dose may be an effective therapeutic option for intractable nausea.
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Objective: One of the most important problems of schizophrenic patients is the impairment of cognitive functions. Methods: The aim of this study was to investigate the effects of haloperidol, asenapine and paliperidone on spatial learning and memory using the Morris water maze (MWM) and radial arm maze (RAM) tests; moreover the effects of haloperidol, asenapine, and paliperidone on MK-801 induced cognitive dysfunction were also evaluated in mice. Results: Both asenapine (0.05 mg/kg) and paliperidone reversed MK-801 induced increment in escape latency in 2nd, 3rd, and 4th acquisition sessions while haloperidol failed to reverse MK-801 induced this effect. Time spent in escape platform’s quadrant significantly decreased while the mean distance to platform significantly increased in MK-801 group in the probe trial of MWM test and administration of asenapine and paliperidone significantly reversed MK- 801 induced these effects while haloperidol had no effect. MK-801 significantly increased the speed of the animals in probe trial of the MWM test while both asenapine and paliperidone reversed this effect. In the RAM test, MK- 801 significantly increased the number of errors in the retention trial and haloperidol failed to reverse this effect. Both asenapine (0.075 mg/kg) and paliperidone reversed MK-801-induced increment in a number of errors and improved MK-801 induced prolongation in latency. Conclusions: The results of this study revealed that MK-801 exerted spatial memory impairment in MWM and RAM tests; haloperidol failed to improve MK-801 induced memory deterioration in mice. Moreover both asenapine and paliperidone improved MK-801 induced spatial learning and memory impairment in the MWM and RAM tests.
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Schizophrenic patients resistant to antipsychotics are diagnosed as having treatment-refractory schizophrenia, and they are treated with clozapine. However, clozapine is sometimes combined with electroconvulsive therapy (ECT) if clozapine monotherapy fails. In this report, a severe treatment-refractory schizophrenic patient who did not respond to clozapine even with ECT, but who recovered with asenapine monotherapy, is presented. Asenapine, considered a serotonin spectrum dopamine modulator, is a new atypical antipsychotic with unique pharmacological features that is used not only for schizophrenia, but also for bipolar disorder. The unique features of asenapine may be effective for some treatment-refractory schizophrenic patients.
Subject(s)
Humans , Antipsychotic Agents , Bipolar Disorder , Clozapine , Dopamine , Electroconvulsive Therapy , Recurrence , Schizophrenia , Serotonin , SuicideABSTRACT
A highly selective and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay has been described for the determination of asenapine (ASE) in presence of its inactive metabolites N-desmethyl asenapine (DMA) and asenapine-N-glucuronide (ASG). ASE, and ASE 13C-d3, used as in-ternal standard (IS), were extracted from 300 μL human plasma by a simple and precise liquid-liquid extraction procedure using methyl tert-butyl ether. Baseline separation of ASE from its inactive meta-bolites was achieved on Chromolith Performance RP8e(100 mm × 4.6 mm) column using acetonitrile-5.0 mM ammonium acetate-10% formic acid (90:10:0.1, v/v/v) within 4.5 min. Quantitation of ASE was done on a triple quadrupole mass spectrometer equipped with electrospray ionization in the positive mode. The protonated precursor to product ion transitions monitored for ASE and ASE 13C-d3 were m/z 286.1 → 166.0 and m/z 290.0 → 166.1, respectively. The limit of detection (LOD) and limit of quantitation (LOQ) of the method were 0.0025 ng/mL and 0.050 ng/mL respectively in a linear con-centration range of 0.050–20.0 ng/mL for ASE. The intra-batch and inter-batch precision (% CV) and mean relative recovery across quality control levels were ≤5.8% and 87.3%, respectively. Matrix effect, eval-uated as IS-normalized matrix factor, ranged from 1.03 to 1.05. The stability of ASE under different storage conditions was ascertained in presence of the metabolites. The developed method is much simpler, matrix free, rapid and economical compared to the existing methods. The method was suc-cessfully used for a bioequivalence study of asenapine in healthy Indian subjects for the first time.
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Combination of asenapine with valproic acid received regulatory approval for acute treatment of schizophrenia and maniac episodes of bipolar disorders. A simple LC-MS/MS method was developed and validated for simultaneous quantification of asenapine and valproic acid in human plasma. Internal standards were added to 300μL of plasma sample prior to liquid-liquid extraction using methyl tertiary butyl ether (MTBE). Chromatographic separation was achieved on Phenomenex C18 column (50 mm ? 4.6 mm, 5μm) in isocratic mode at 40 1C. The mobile phase used was 10 mM ammonium formate-acetonitrile (5:95, v/v) at a constant flow rate of 0.8 mL/min monitored on triple quadrupole mass spectrometer, operating in the multiple reaction monitoring (MRM) mode. The injection volume used for LC-MS/MS analysis was 15μL and the run time was 2.5 min. These low run time and small injection volume suggest the high efficiency of the proposed method. The method was validated over the concentration range of 0.1-10.02 ng/mL and 10-20,000 ng/mL for asenapine and valproic acid respectively. The method recoveries of asenapine (81.33%), valproic acid (81.70%), gliclazide (78.45%) and benzoic acid (79.73) from spiked plasma samples were consistent and reproducible. The application of this method was demonstrated by a pharmacokinetic study in 8 healthy male volunteers with 5 mg asenapine and 250 mg valproic acid administration.
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Asenapine is used in the treatment of schizophrenia disease.Asenapine mainly control the psychotic symptoms’ mainly antagonist to various receptors like, serotonin (5-HT1A, 5- HT1B,5-HT2A,5-HT2B,),histamine, and dopamine(D1,D2,D3,D4) receptors. It is also lower affinity towards muscaranic and acetylcholine receptors. In the present study, simple titrimetric method was developed. Respective quantities of Asenapine were taken in aqueous methanol titrated against 0.1N sodium hydroxide acid and 0.1N potassium hydroxide acid using phenolphthalein as an indicators for neutralization titration. This method were found to be sensitive and inexpensive, do not require any sample processing steps and can be utilized for estimation of asenapine in bulk and formulations.
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CONTEXTO: Os antipsicóticos de segunda geração representam o grande avanço na terapêutica da esquizofrenia das últimas décadas, porém nos últimos anos foram sintetizados novos antipsicóticos que estão abrindo maiores perspectivas no campo do tratamento da esquizofrenia. Alguns desses medicamentos já foram lançados, enquanto outros estão em fase de testes. OBJETIVO: Apresentar uma síntese do conhecimento dos novos antipsicóticos de segunda geração. MÉTODOS: Busca por meio do PubMed e literatura específica fornecida pelos fabricantes dos medicamentos. RESULTADOS E CONCLUSÕES: São apresentadas as principais características farmacológicas, de eficácia, segurança e tolerabilidade dos seguintes antipsicóticos: Asenapina, ACP-103, Bifeprunox, Paliperidona, Risperidona de Ação Prolongada e Sertindol.
BACKGROUND: The second generation antipsychotics represent the great achievement in the treatment of schizophrenia of the last decades. However in the last years some new antipsychotics were synthesized and such new compounds may represent great perspectives for the field of the treatment of schizophrenia. Some of these compounds are in use while others are still on evaluation through clinical trials. OBJECTIVE: Summarize the current knowledge of new antipsychotics. METHODS: PubMed search as well literature provided by the manufactures. RESULTS AND CONCLUSIONS: We present the main pharmacological characteristics as well as profiles of efficacy, security and tolerability of the following compounds: Asenapine, ACP-103, Bifeprunox, Paliperidone, Long Acting Injectable Risperidone and Sertindole.