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https://www.readbyqxmd.com/read/28814871/exploring-the-long-term-safety-of-asenapine-in-adults-with-schizophrenia-in-a-double-blind-fixed-dose-extension-study
#1
Suresh Durgam, Ronald P Landbloom, Mary Mackle, Xiao Wu, Maju Mathews, Henry A Nasrallah
PURPOSE: The primary objective of this study was to assess long-term safety with sublingual asenapine 2.5 or 5 mg twice daily (BID) in patients with schizophrenia. PATIENTS AND METHODS: Actively treated patients on asenapine 2.5 mg BID, asenapine 5 mg BID, or olanzapine 15 mg once daily (QD) who completed a 6-week randomized, double-blind, placebo- and olanzapine-controlled study continued lead-in treatment in this 26-week, multicenter, double-blind, double-dummy, olanzapine-controlled Phase IIIB extension study; placebo patients were assigned to asenapine 2...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28803208/n-glucuronidation-catalyzed-by-ugt1a4-and-ugt2b10-in-human-liver-microsomes-assay-optimization-and-substrate-identification
#2
Danyi Lu, Qian Xie, Baojian Wu
N-glucuronidation is an important pathway for metabolism and disposition of tertiary amines in humans. This reaction is mainly catalyzed by the enzymes UGT1A4 and UGT2B10. However, the metabolic patterns of UGT1A4- and UGT2B10-mediated N-glucuronidation are not fully clear. In this study, we first optimized in vitro reaction conditions for N-glucuronidation by using specific substrates (i.e., trifluoperazine for UGT1A4, cotinine and amitriptyline for UGT2B10). Furthermore, we found that hepatic N-glucuronidation showed significant species differences...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28741044/efficacy-and-tolerability-of-asenapine-compared-with-olanzapine-in-borderline-personality-disorder-an-open-label-randomized-controlled-trial
#3
Paola Bozzatello, Paola Rocca, Maria Uscinska, Silvio Bellino
BACKGROUND: Asenapine is a new second-generation antipsychotic that is understudied in borderline personality disorder (BPD). Only one study investigating the use of the drug in this indication (an open-label pilot study) has been conducted to date. OBJECTIVE: The present open-label, randomized, controlled trial aimed to evaluate the efficacy and tolerability of asenapine in comparison with olanzapine, the most broadly studied antipsychotic in BPD. METHODS: A total of 51 outpatients aged between 18 and 50 years with a diagnosis of BPD based on Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5) criteria were assigned for 12 weeks to asenapine (5-10 mg/day) or olanzapine (5-10 mg/day)...
July 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28737445/preclinical-pharmacokinetics-and-biodistribution-studies-of-asenapine-maleate-using-novel-and-sensitive-rp-hplc-method
#4
Renuka S Managuli, Karthik Gourishetti, Rekha R Shenoy, Kunnatur B Koteshwara, Meka Sreenivasa Reddy, Srinivas Mutalik
AIM: Asenapine maleate (ASPM) is a newer antipsychotic drug available as a sublingual tablet in the market. EXPERIMENTAL: To investigate the pharmacokinetic and tissue distribution study of ASPM following oral administration in rats, reversed-phase HPLC method was developed and validated. RESULTS: ASPM was extracted from plasma and tissue matrix by liquid-liquid extraction technique and analyzed using mobile phase consisted of phosphate buffer pH 3...
July 24, 2017: Bioanalysis
https://www.readbyqxmd.com/read/28727644/cariprazine-specificity-profile-in-the-treatment-of-acute-schizophrenia-a-meta-analysis-and-meta-regression-of-randomized-controlled-trials
#5
Filippo Corponi, Alessandro Serretti, Stuart Montgomery, Chiara Fabbri
Cariprazine is a new dopamine D2 and D3 receptor partial agonist antipsychotic. Meta-analytic evidence of efficacy in acute schizophrenia and specific groups of patients is lacking. We carried out a meta-analysis in patients with acute schizophrenia to evaluate the efficacy of cariprazine over placebo and active comparators in overall symptoms, positive and negative symptoms and quality of life. Low and high (≥6 mg/day) doses were tested separately. The possible effect of clinical-demographic modulators was also tested...
July 19, 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28721057/safety-tolerability-and-risks-associated-with-first-and-second-generation-antipsychotics-a-state-of-the-art-clinical-review
#6
REVIEW
Marco Solmi, Andrea Murru, Isabella Pacchiarotti, Juan Undurraga, Nicola Veronese, Michele Fornaro, Brendon Stubbs, Francesco Monaco, Eduard Vieta, Mary V Seeman, Christoph U Correll, André F Carvalho
Since the discovery of chlorpromazine (CPZ) in 1952, first-generation antipsychotics (FGAs) have revolutionized psychiatric care in terms of facilitating discharge from hospital and enabling large numbers of patients with severe mental illness (SMI) to be treated in the community. Second-generation antipsychotics (SGAs) ushered in a progressive shift from the paternalistic management of SMI symptoms to a patient-centered approach, which emphasized targets important to patients - psychosocial functioning, quality of life, and recovery...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28609288/eff-ect-of-a-single-asenapine-treatment-on-fos-expression-in-the-brain-catecholamine-synthesizing-neurons-impact-of-a-chronic-mild-stress-preconditioning
#7
J Osacka, L Horvathova, Z Majercikova, Alexander Kiss
OBJECTIVE: Fos protein expression in catecholamine-synthesizing neurons of the substantia nigra (SN) pars compacta (SNC, A8), pars reticulata (SNR, A9), and pars lateralis (SNL), the ventral tegmental area (VTA, A10), the locus coeruleus (LC, A6) and subcoeruleus (sLC), the ventrolateral pons (PON-A5), the nucleus of the solitary tract (NTS-A2), the area postrema (AP), and the ventrolateral medulla (VLM-A1) was quantitatively evaluated aft er a single administration of asenapine (ASE) (designated for schizophrenia treatment) in male Wistar rats preconditioned with a chronic unpredictable variable mild stress (CMS) for 21 days...
April 25, 2017: Endocrine Regulations
https://www.readbyqxmd.com/read/28559635/asenapine-for-the-control-of-physical-aggression-a-prospective-naturalist-pilot-study
#8
Jin Shi Amon, Sarah B Johnson, Rif S El-Mallakh
It has been previously purported that higher relative affinity to the dopamine D4 receptor compared to D2 (i.e., D4/D2 affinity ratio > 1) may underlie unique antiaggression potency. Asenapine is a newer antipsychotic that also has D4/D2 affinity ratio > 1. It has demonstrated efficacy in reducing acute agitation in a placebo-controlled study. We performed a prospective naturalistic, pilot, proof of concept study on an inpatient psychiatric unit. Among patients with aggression at time of admission (≥ 12 on Refined Aggression Questionnaire [RAQ], or ≥ 2 on Modified Overt Aggression Scale [MOAS]), asenapine treatment was associated with a significant reduction in total aggression as measured by the MOAS (-14...
January 26, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/28462607/have-antipsychotics-a-different-speed-of-action-in-the-acute-treatment-of-mania-a-single-blind-comparative-study
#9
Massimiliano Buoli, Cecilia Maria Esposito, Marco Godio, Alice Caldiroli, Marta Serati, A Carlo Altamura
Available antipsychotics show different efficacy on manic symptoms of bipolar patients, but few studies have investigated the speed of action of the various compounds. For this reason, purpose of the present paper was to compare antipsychotic mono-therapies in terms of speed of action in a sample of manic bipolar patients. In total, 155 bipolar patients, treated with antipsychotic mono-therapy and followed-up in Inpatient Psychiatry Clinic of University of Milan, were included in this single-blind comparative study...
April 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28417647/mixed-states-in-bipolar-disorder-changes-in-dsm-5-and-current-treatment-recommendations
#10
Felix Betzler, Laura Apollonia Stöver, Philipp Sterzer, Stephan Köhler
OBJECTIVE: Mixed states in affective disorders represent a particular challenge in clinical routine, characterized by a complicated course of treatment and a worse treatment response. METHODS: Clinical features of mixed states and the Diagnostic and Statistical Manual of Mental Disorders (DSM-5) criteria are presented and critical discussed. We then performed a systematic review using the terms 'bipolar', 'mixed' and 'randomized' to evaluate current treatment options...
April 18, 2017: International Journal of Psychiatry in Clinical Practice
https://www.readbyqxmd.com/read/28417559/asenapine-modulates-mood-related-behaviors-and-5-ht1a-7-receptors-mediated-neurotransmission
#11
Sarah Delcourte, Erika Abrial, Adeline Etiévant, Renaud Rovera, Jørn Arnt, Michael Didriksen, Nasser Haddjeri
AIM: Asenapine is a new atypical antipsychotic prescribed for the treatment of psychosis/bipolar disorders that presents higher affinity for serotonergic than dopaminergic receptors. The objective of this study was to investigate its antidepressant-like and antimanic-like properties on relevant animal models of depression and mania and to assess the acute and chronic effect of Asenapine on dorsal raphe nucleus (DRN) 5-HT cell firing activity. METHODS: We assessed the effects of Asenapine using in vivo electrophysiological and behavioral assays in rats...
June 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28255436/does-the-efficacy-of-asenapine-in-bipolar-disorder-increase-in-the-presence-of-comorbidity-with-a-substance-use-disorder-a-naturalistic-study
#12
Sergio De Filippis, Ilaria Cuomo, Georgios D Kotzalidis, Daniela Pucci, Pietro Zingaretti, Raffaella Porrari, Camilla Fini, Paola Motta, Matteo Caloro, Paolo Girardi
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...
February 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28235555/re-arrangements-of-gene-transcripts-at-glutamatergic-synapses-after-prolonged-treatments-with-antipsychotics-a-putative-link-with-synaptic-remodeling
#13
Elisabetta Filomena Buonaguro, Felice Iasevoli, Federica Marmo, Anna Eramo, Gianmarco Latte, Camilla Avagliano, Carmine Tomasetti, Andrea de Bartolomeis
OBJECTIVES: The postsynaptic density (PSD) represents a site of dopamine-glutamate integration. Despite multiple evidence of PSD involvement in antipsychotic-induced synaptic changes, there are no direct head-to-head comparisons of the effects at the PSD of antipsychotics with different receptor profile and at different doses after chronic administration. METHODS: Molecular imaging of gene expression was used to investigate whether chronic treatment with first and second generation antipsychotics (haloperidol, asenapine and olanzapine) may induce changes in the expression levels of PSD transcripts involved in schizophrenia pathophysiology, i...
February 22, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28219485/acute-antipsychotic-treatment-of-children-and-adolescents-with-schizophrenia-spectrum-disorders-a-systematic-review-and-network-meta-analysis
#14
REVIEW
Anne Katrine Pagsberg, Simon Tarp, Dorte Glintborg, Anne Dorte Stenstrøm, Anders Fink-Jensen, Christoph Ulrich Correll, Robin Christensen
OBJECTIVE: To determine the comparative efficacy and safety of antipsychotics for youth with early-onset schizophrenia using network meta-analytic methods combining direct and indirect trial data. METHOD: The authors systematically searched MEDLINE, the Cochrane Library, and clinicaltrials.gov and selected randomized controlled trials allocating youth with schizophrenia spectrum disorders to a (non-clozapine) antipsychotic versus placebo or another antipsychotic...
March 2017: Journal of the American Academy of Child and Adolescent Psychiatry
https://www.readbyqxmd.com/read/28141623/activating-and-sedating-adverse-effects-of-second-generation-antipsychotics-in-the-treatment-of-schizophrenia-and-major-depressive-disorder-absolute-risk-increase-and-number-needed-to-harm
#15
Leslie Citrome
PURPOSE/BACKGROUND: Activating and sedating adverse effects of antipsychotics can be obstacles to their use. METHODS/PROCEDURES: This study quantified the activating and sedating properties of first-line oral second-generation antipsychotics by examining the rates of adverse reactions as reported in product labeling for the indications of schizophrenia and adjunctive treatment of major depressive disorder. Additional data sources included regulatory documents, study synopses, and published study reports...
April 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28138201/asenapine-for-the-control-of-physical-aggression-a-prospective-naturalist-pilot-study
#16
Jin Shi Amon, Sarah B Johnson, Rif S El-Mallakh
It has been previously purported that higher relative affinity to the dopamine D4 receptor compared to D2 (i.e., D4/D2 affinity ratio > 1) may underlie unique antiaggression potency. Asenapine is a newer antipsychotic that also has D4/D2 affinity ratio > 1. It has demonstrated efficacy in reducing acute agitation in a placebo-controlled study. We performed a prospective naturalistic, pilot, proof of concept study on an inpatient psychiatric unit. Among patients with aggression at time of admission (≥ 12 on Refined Aggression Questionnaire [RAQ], or ≥ 2 on Modified Overt Aggression Scale [MOAS]), asenapine treatment was associated with a significant reduction in total aggression as measured by the MOAS (-14...
January 26, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/28005435/is-there-a-weight-neutral-second-generation-antipsychotic-for-bipolar-disorder
#17
REVIEW
Fang Fang, Zuowei Wang, Renrong Wu, Joseph R Calabrese, Keming Gao
Antipsychotic-induced weight gain (WG) and metabolic abnormalities are major concerns. This review was untaken to answer if there is a weight-neutral second-generation antipsychotic for bipolar disorder (BPD). Areas covered: English-language literature in MEDLINE was searched with the keywords of antipsychotic/second-generation antipsychotic or generic/brand name of second-generation antipsychotic, and BPD/mania/depression or bipolar maintenance, and safety/tolerability or WG/weight increase, and randomized, placebo-controlled trial...
April 2017: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/28004626/treating-mixed-mania-hypomania-a-review-and-synthesis-of-the-evidence
#18
REVIEW
Minoru Takeshima
The DSM-5 incorporates a broad concept of mixed states and captured ≥3 nonoverlapping symptoms of the opposite polarity using a "with mixed features" specifier to be applied to manic/hypomanic and major depressive episodes. Pharmacotherapy of mixed states is challenging because of the necessity to treat both manic/hypomanic and depressive symptoms concurrently. High-potency antipsychotics used to treat manic symptoms and antidepressants can potentially deteriorate symptoms of the opposite polarity. This review aimed to provide a synthesis of the current evidence for pharmacotherapy of mixed states with an emphasis on mixed mania/hypomania...
April 2017: CNS Spectrums
https://www.readbyqxmd.com/read/27821210/asenapine-for-the-treatment-of-adults-with-an-acute-exacerbation-of-schizophrenia-results-from-a-randomized-double-blind-fixed-dose-placebo-controlled-trial-with-olanzapine-as-an-active-control
#19
Ronald Landbloom, Mary Mackle, Xiao Wu, Linda Kelly, Linda Snow-Adami, Roger S McIntyre, Maju Mathews, Carla Hundt
OBJECTIVE: Evaluate the efficacy and safety of asenapine 2.5 mg twice daily (bid; n=97) or 5 mg bid (n=113) versus placebo (n=101) in adults with acute exacerbation of schizophrenia. METHODS: Adults with Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, Text Revision (DSM-IV-TR) schizophrenia diagnosis were randomized to asenapine 2.5 mg bid, 5 mg bid, placebo, or olanzapine 15 mg once daily. The primary objective was to test superiority of asenapine versus placebo as measured by the change from baseline to day 42 in the Positive and Negative Syndrome Scale (PANSS) total score...
August 2017: CNS Spectrums
https://www.readbyqxmd.com/read/27756486/repeated-asenapine-treatment-does-not-participate-in-the-mild-stress-induced-fosb-%C3%AE-fosb-expression-in-the-rat-hypothalamic-paraventricular-nucleus-neurons
#20
Alexander Kiss, Zuzana Majercikova
Effect of repeated asenapine (ASE) treatment on FosB/ΔFosB expression was studied in the hypothalamic paraventricular nucleus (PVN) of male rats exposed to chronic mild stress (CMS) for 21days. Our intention was to find out whether repeated ASE treatment for 14days may: 1) induce FosB/ΔFosB expression in the PVN; 2) activate selected PVN neuronal phenotypes, synthesizing oxytocin (OXY), vasopressin (AVP), corticoliberin (CRH) or tyrosine hydroxylase (TH); and 3) interfere with the impact of CMS. Control, ASE, CMS, and CMS+ASE treated groups were used...
February 2017: Neuropeptides
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