New approaches for the management of bipolar disorder: role of sublingual asenapine in the treatment of mania

Warren, Calvert; Dubovsky, Steven

doi:10.2147/ndt.s16078

Cited by 2 publications

(2 citation statements)

References 59 publications

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“…It shows high affinity to serotonin receptors (5-HT1a, 5-HT1b, 5-HT2a, 5-HT2b, 5-HT2c, 5-HT5, 5-HT6, and 5-HT7), dopamine receptors (D1, D2, D3, and D4), alpha 1 and 2 receptors, histamine (H1) receptors and moderate affinity to histamine (H2) receptors. Unlike other antipsychotic agents, ASE has no appreciable affinity towards muscarinic receptors [1] , [4] . ASE is unique among other atypical antipsychotics like risperidone, olanzapine and aripiprazole, in its mode of administration.…”

Section: Introductionmentioning

confidence: 96%

“…Pharmacologically, ASE is a dibenzo-oxepino pyrrole drug with a tetracyclic structure. It is the ninth atypical antipsychotic agent that received regulatory approval in August 2009 from the US Food and Drug Administration (FDA) to schizophrenia and bipolar I disorder in adults [4] . It shows high affinity to serotonin receptors (5-HT1a, 5-HT1b, 5-HT2a, 5-HT2b, 5-HT2c, 5-HT5, 5-HT6, and 5-HT7), dopamine receptors (D1, D2, D3, and D4), alpha 1 and 2 receptors, histamine (H1) receptors and moderate affinity to histamine (H2) receptors.…”

Section: Introductionmentioning

confidence: 99%

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Determination of asenapine in presence of its inactive metabolites in human plasma by LC-MS/MS

Patel

Sanyal

Sharma

et al. 2018

Journal of Pharmaceutical Analysis

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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 internal 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 metabolites 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 concentration 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, evaluated 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 successfully used for a bioequivalence study of asenapine in healthy Indian subjects for the first time.

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Section: Introductionmentioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

Determination of asenapine in presence of its inactive metabolites in human plasma by LC-MS/MS

Patel

Sanyal

Sharma

et al. 2018

Journal of Pharmaceutical Analysis

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Does the efficacy of asenapine in bipolar disorder increase in the presence of comorbidity with a substance use disorder? A naturalistic study

Filippis

Cuomo²,

Kotzalidis

et al. 2016

Therapeutic Advances in Psychopharmacology

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Background: Asenapine is a second-generation antipsychotic approved in Europe for treating moderate-to-severe manic episodes in adults affected by type I bipolar disorder (BD-I). We aimed to compare its efficacy in psychiatric inpatients with BD-I, with or without substance use disorder (SUD). Methods: We administered flexible asenapine doses ranging from 5-20 mg/day to 119 voluntarily hospitalized patients with Diagnostic and Statistical Manual of Mental Disorders, 4th Edition, Text Revision (DSM-IV-TR) BD-I diagnosis, with or without SUD. Patients were assessed with clinician-rated questionnaires [i.e. Brief Psychiatric Rating Scale (BPRS), Young Mania Rating Scale (YMRS), Hamilton Depression Rating Scale (HDRS), Hamilton Anxiety Rating Scale (HARS), and Global Assessment of Functioning (GAF)]. Assessments were carried out at baseline (T0, prior to treatment), and 3 (T1), 7 (T2), 15 (T3), and 30 days (T4) after starting treatment for all clinical scales and at T0 and T4 for the GAF. Results: Patients improved on all scales (p < 0.001) across all timepoints, as shown both by paired-sample comparisons and by applying a repeated-measures, generalized linear model (GLM). Patients without comorbid SUD showed greater reductions in BPRS scores at T2 and T3, greater reduction in YMRS scores at T3, and lower HARS scores at all timepoints. HDRS scores did not differ between the two groups at any timepoint. However, the reduction in HARS scores in the comorbid group was stronger than in the BD-I only group, albeit not significantly. Side effects were few and mild-to-moderate. Conclusions: The open-label design and the relatively short observation period may expose to both type I and type II statistical errors (false positive and false negatives). Asenapine showed effectiveness and safety in hospitalized BD-I patients. Its effect was stronger in patients without comorbid SUD.

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New approaches for the management of bipolar disorder: role of sublingual asenapine in the treatment of mania

Cited by 2 publications

References 59 publications

Determination of asenapine in presence of its inactive metabolites in human plasma by LC-MS/MS

Determination of asenapine in presence of its inactive metabolites in human plasma by LC-MS/MS

Does the efficacy of asenapine in bipolar disorder increase in the presence of comorbidity with a substance use disorder? A naturalistic study

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