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https://www.readbyqxmd.com/read/29237385/systemic-administrations-of-antipsychotic-asenapine-pre-or-postnatal-does-not-induce-anxiety-like-behaviors-in-mice
#1
Maria Silvia Oliveira, Thais Souza Barbosa de Souza, Daniela Miranda Farias, Rozimeri Fatima Coletti, Jorge Aparecido de Barros, Carolina Gomes Carrilho, Susana Elisa Moreno, Eric Murillo Murillo Rodriguez, Sergio Machado, Andre Barciela Veras
Asenapine is an atypical antipsychotic approved by US Food and Drug Administration in 2009 and by European Medicines Agency in 2010 for schizophrenia and bipolar disorder treatment. Currently, many studies have been developed in an attempt to clarify and minimize the risks related to the use of psychotropic during pre/postnatal period on patients with a history of mental disorders. To this finality, the purpose of the following work was to test on animal models the impact of being exposed to this medication during perinatal period upon anxiety and exploration/emotionality of female mice's descendants submitting them, in adulthood, to the Open Field and Elevated Plus Maze test...
December 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29219316/from-the-promiscuous-asenapine-to-potent-fluorescent-ligands-acting-at-a-series-of-aminergic-g-protein-coupled-receptors
#2
Candide Hounsou, Corinne Baehr, Vincent Gasparik, Doria Alili, Abderazak Belhocine, Thiéric Rodriguez, Elodie Dupuis, Thomas Roux, André Mann, Denis Heissler, Jean-Philippe Pin, Thierry Durroux, Dominique Bonnet, Marcel Hibert
Monoamine neurotransmitters such as serotonin, dopamine, histamine and noradrenaline have important and varied physiological functions and similar chemical structures. Representing important pharmaceutical drug targets, the corresponding G protein coupled receptors (termed aminergic GPCRs) belong to the class of cell membrane receptors and share many levels of similarity as well. Given their pharmacological and structural closeness, one could hypothesize the possibility to derivatize a ubiquitous ligand to afford rapidly fluorescent probes for a large set of GPCRs to be used for instance in FRET-based binding assays...
December 8, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29200857/reversal-of-olanzapine-induced-weight-gain-in-a-patient-with-schizophrenia-by-switching-to-asenapine-a-case-report
#3
Kosuke Okazaki, Kazuhiko Yamamuro, Toshifumi Kishimoto
Aims: Antipsychotics are effective for treating schizophrenia, but atypical antipsychotics can cause several adverse side effects including weight gain, hyperprolactinemia, and extrapyramidal symptoms. Moreover, weight gain increases the risk of metabolic diseases. Methods: We treated a case of olanzapine-induced weight gain in a 41-year-old man with schizophrenia by switching his medication from olanzapine to asenapine. Results: The weight gain improved after switching the medication, from 80...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29191711/analyzing-test-batteries-in-animal-models-of-psychopathology-with-multivariate-analysis-of-variance-manova-one-possible-approach-to-increase-external-validity
#4
Yelena Stukalin, Haim Einat
BACKGROUND: One concern regarding animal models of psychopathology is unclear external validity. One way to establish external validity is to examine measures representing separate facets of the pathology with a battery of tests in the same cohort of animals. Additionally, utilizing the same animals in a battery of tests can help to reduce the number of animals in research. However, issues had been raised regarding the analysis of data coming from batteries and the standard practice is to analyze each test separately...
November 27, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29189421/asenapine-in-the-management-of-impulsivity-and-aggressiveness-in-bipolar-disorder-and-comorbid-borderline-personality-disorder-an-open-label-uncontrolled-study
#5
Andrea Aguglia, Ludovico Mineo, Alessandro Rodolico, Maria S Signorelli, Eugenio Aguglia
Borderline personality disorder (BPD) often co-occurres with bipolar disorder (BD). Impulsivity and aggressiveness represent core shared features and their pharmacological management is mainly based on mood stabilizers and antipsychotics, although scarce evidence is available for this context of comorbidity. The aim of the present study was to evaluate the role of Asenapine as an adjunctive drug for reducing aggressiveness and impulsivity in a sample of Italian BD type I outpatients with or without a comorbid BPD...
November 17, 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29170943/asenapine-treatment-in-pediatric-patients-with-bipolar-i-disorder-or-schizophrenia-a-review
#6
REVIEW
Ekaterina Stepanova, Bradley Grant, Robert L Findling
Asenapine, administered as a twice-daily (BID) sublingual tablet, is approved in the US as monotherapy for the acute treatment of manic and mixed episodes of bipolar I disorder in children and adolescents aged 10-17 years based on the positive results of one 3-week, double-blind, placebo-controlled study; the recommended dose is 2.5-10 mg BID. Although asenapine has been studied in pediatric patients with schizophrenia, it is not approved for this indication. Asenapine is not approved for pediatric use in bipolar I disorder or schizophrenia in other major markets...
November 23, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/29165075/preferential-formulation-of-second-generation-antipsychotic-asenapine-as-inclusion-complex-with-sulphobutylether-%C3%AE-cd-captisol-in-vitro-and-in-vivo-evaluation
#7
Amelia Makarand Avachat, Juilee A Kulkarni, Charul M Avachat, Rohan Pradhan, Tushar S Suryawanshi, E M Khan, Elvis A F Martis, Evans C Coutinho, Subhash Padhye
Asenapine is an anti-psychotic agent approved by the US-FDA for treatment of acute schizophrenia and manic or bipolar I disorder in adults. It is poorly absorbed when administered orally, hence exhibits poor oral bioavailability, which limits its use in clinical practice. Consequently, enhancement in its solubility through complexation with three different cyclodextrins, viz. βCD (β cyclodextrin), HPβCD (Hydroxypropyl β cyclodextrin) and sulphobutylether-βCD (Captisol®) was attempted and compared. Kneading method was used for preparation of inclusion complexes which were characterized by FTIR, DSC, and XRD methods...
November 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/29126941/glycol-chitosan-functionalized-asenapine-nanostructured-lipid-carriers-for-targeted-brain-delivery-pharmacokinetic-and-teratogenic-assessment
#8
Sanjay Kumar Singh, Mahendra Kumar Hidau, Shrikant Gautam, Kiran Gupta, Krishna Pal Singh, Shio Kumar Singh, Sanjay Singh
Blood brain barrier (BBB) is a complex, tight barrier between endothelial cells of cerebral blood vessels. It acts as a physical barrier and provides access to only those moieties which are necessary for proper brain functioning. However, this selective prudence also acts as a hindrance in therapeutic targeting of brain necessitating pharmaceutical intervention. Intranasal drug delivery is one such approach which we have exploited here for targeted brain delivery of asenapine via glycol chitosan coated nanostructured lipid carrier (GC-ANLC)...
November 7, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29105003/anxiety-irritability-and-agitation-as-indicators-of-bipolar-mania-with-depressive-symptoms-a-post-hoc-analysis-of-two-clinical-trials
#9
Trisha Suppes, Jonas Eberhard, Ole Lemming, Allan H Young, Roger S McIntyre
BACKGROUND: Symptoms of anxiety, irritability, and agitation (AIA) are prevalent among patients with bipolar I disorder (BD-I) mania with depressive symptoms, and could potentially be used to aid physicians in the identification of this more severe form of BD-I. Using data from two clinical trials, the aims of this post hoc analysis were to describe the phenomenology of bipolar mania in terms of AIA and depressive symptoms, and to evaluate the influence of these symptoms on the likelihood of remission during treatment...
November 6, 2017: International Journal of Bipolar Disorders
https://www.readbyqxmd.com/read/29067671/a-review-of-asenapine-in-the-treatment-of-bipolar-disorder
#10
REVIEW
Eduard Vieta, José Manuel Montes
Bipolar disorder places a significant burden on the affected individuals, their family, healthcare systems and the overall economy. More treatment options are needed, especially those with better efficacy and tolerability. Asenapine is a second-generation antipsychotic approved in Europe (brand name Sycrest(®)) for the treatment of moderate-to-severe manic episodes associated with bipolar I disorder in adults, and in the US (brand name Saphris(®)) for the treatment of manic or mixed episodes of bipolar I disorder in adults and children aged 10-17 years...
October 24, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29040152/acute-laryngeal-dystonia-associated-with-asenapine-use-a-case-report
#11
Nathaniel Collins, Jeffrey Sager
No abstract text is available yet for this article.
October 16, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28992737/asenapine-iloperidone-and-lurasidone-exposures-in-young-children-reported-to-u-s-poison-centers
#12
Gina Stassinos, Wendy Klein-Schwartz
CONTEXT: Asenapine, iloperidone and lurasidone are relatively new atypical antipsychotics. There is limited information on toxicity on pediatric exposures to these drugs. The objective of this study was to compare toxicity associated with asenapine, iloperidone and lurasidone exposures in young children. METHODS: A retrospective study of U.S. National Poison Data System from 2010 to 2015 of single substance exposures to asenapine, iloperidone or lurasidone in children <6 years of age that were followed to known outcome was performed...
October 10, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28946761/randomized-double-blind-placebo-controlled-trial-of-asenapine-maintenance-therapy-in-adults-with-an-acute-manic-or-mixed-episode-associated-with-bipolar-i-disorder
#13
Armin Szegedi, Suresh Durgam, Mary Mackle, Sung Yun Yu, Xiao Wu, Maju Mathews, Ronald P Landbloom
OBJECTIVE: The authors determined the efficacy and safety of asenapine in preventing recurrence of any mood episode in adults with bipolar I disorder. METHOD: Adults with an acute manic or mixed episode per DSM-IV-TR criteria were enrolled in this randomized, placebo-controlled trial consisting of an initial 12- to 16-week open-label period and a 26-week double-blind randomized withdrawal period. The target asenapine dosage was 10 mg b.i.d. in the open-label period but could be titrated down to 5 mg b...
September 26, 2017: American Journal of Psychiatry
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
#14
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
#15
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
#16
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)...
September 2017: CNS Drugs
https://www.readbyqxmd.com/read/28737445/preclinical-pharmacokinetics-and-biodistribution-studies-of-asenapine-maleate-using-novel-and-sensitive-rp-hplc-method
#17
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
#18
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...
November 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
#19
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
#20
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
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