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Brexpiprazole aripiprazole

Kristen Ward, Leslie Citrome
The purpose of this review is to describe the available data for brexpiprazole in the maintenance treatment of schizophrenia. This objective was completed by searching the databases PubMed, Embase, and to identify relevant study results presented as papers or abstracts. In summary, brexpiprazole is a new agent in the D2 partial agonist class that has a unique receptor-binding profile, based in part on high affinity for serotonin 5HT1A and 5HT2A receptors, paired with lower intrinsic activity at dopamine D2 receptors...
2019: Neuropsychiatric Disease and Treatment
James E Frampton
Brexpiprazole (Rxulti® , Rexulti® ) is an oral atypical antipsychotic agent approved for the treatment of schizophrenia in the EU (in adult patients) and the USA, as well as in some other countries, including Japan. Like aripiprazole, it is a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at serotonin 5-HT2A receptors. However, brexpiprazole displays less intrinsic activity at D2 receptors and, coupled with actions at 5HT1A , 5HT2A and noradrenaline α1B receptors that are at least as potent as its action at D2 receptors, is predicted to demonstrate a lower propensity for activating adverse events and extrapyramidal symptoms than aripiprazole...
January 22, 2019: Drugs
Akshya Vasudev, Sumit Chaudhari, Rickinder Sethi, Rachel Fu, Rachel M Sandieson, Brent P Forester
Bipolar disorder prevalence rates vary in the older adult population (defined as age ≥ 65 years), ranging from 1% in community dwellers to as high as 8-10% in hospital inpatients. Although older agents, including lithium and valproic acid, offer significant antimanic efficacy, as supported by a recent randomized controlled trial (RCT), there is growing interest in using atypical antipsychotics to treat bipolar disorder in older adults. Newer atypical antipsychotics are of interest based on their tolerability and efficacy in the general adult bipolar population...
October 2018: Drugs & Aging
Massimo Carlo Mauri, Silvia Paletta, Chiara Di Pace, Alessandra Reggiori, Giovanna Cirnigliaro, Isabel Valli, Alfredo Carlo Altamura
Therapeutic drug monitoring studies have generally concentrated on controlling compliance and avoiding side effects by maintaining long-term exposure to minimally effective blood concentrations. The rationale for using therapeutic drug monitoring in relation to second-generation antipsychotics is still being discussed at least with regard to the real clinical utility, but there is evidence that it can improve efficacy, especially when patients do not respond or develop side effects using therapeutic doses. Furthermore, drug plasma concentration determinations can be of some utility in medico-legal problems...
June 19, 2018: Clinical Pharmacokinetics
Catherine Weiss, Emmanuelle Weiller, Ross A Baker, Ruth A Duffy, Keva K Gwin, Peter Zhang, Robert D McQuade
The aim of this analysis was to explore the effects of brexpiprazole and aripiprazole on body weight when used as monotherapy to treat schizophrenia and as adjunctive treatment to antidepressant treatment (ADT) for major depressive disorder (MDD) in short-term (4/6 weeks) and long-term (≤52 weeks) studies. Body weight data were obtained from the clinical studies of each drug (brexpiprazole and aripiprazole), in schizophrenia and adjunctive treatment of MDD. Data were pooled and analyzed to assess the mean change in body weight and to determine the incidence of a clinically relevant change in body weight from baseline (≥7% increase or decrease, at any time) in each treatment group...
September 2018: International Clinical Psychopharmacology
Arpamas Seetasith, Mallik Greene, Ann Hartry, Chakkarin Burudpakdee
AIMS: The study compared all-cause and major depressive disorder (MDD)-related healthcare resource use (HRU) and costs in patients with MDD treated with atypical antipsychotic (AAP) adjunctive therapy early or later in treatment. MATERIALS AND METHODS: Adults with MDD and antidepressant treatment (ADT) who newly initiated adjunctive aripiprazole, brexpiprazole, lurasidone, or quetiapine between October 1, 2014 and September 30, 2015 were identified in the IQVIA Real-World Data Adjudicated Claims database; the index date was the date of the first AAP claim...
September 2018: Journal of Medical Economics
Wilbert S Aronow, Tatyana A Shamliyan
Background: Drug-induced QT prolongation is associated with higher risk of cardiac arrhythmias and cardiovascular mortality. We investigated the effects of atypical antipsychotic drugs on QT interval in children and adults with mental disorders. Methods: We conducted random-effects direct frequentist meta-analyses of aggregate data from randomized controlled trials (RCT) and appraised the quality of evidence using the Grading of Recommendations Assessment, Development and Evaluation (GRADE) methodology...
April 2018: Annals of Translational Medicine
Eva Češková
Despite of tremendous development in CNS research, current treatment is suboptimal especially in severe mental disorders. In medicine, there are two main methods of improving the healthcare provided: seeking new treatment procedures and perfecting (optimizing) the existing ones. Optimization of treatment includes not only practical tools such as therapeutic drug monitoring, but also implementation of general trends into the clinical practice. New pharmacological options include drugs aimed at other than monoaminergic systems and old drugs used before the psychopharmacological era...
2018: Casopís Lékar̆ů C̆eských
Thiago C Genaro-Mattos, Keri A Tallman, Luke B Allen, Allison Anderson, Karoly Mirnics, Zeljka Korade, Ned A Porter
While antipsychotic medications provide important relief from debilitating psychotic symptoms, they also have significant adverse side effects, which might have relevant impact on human health. Several research studies, including ours, have shown that commonly used antipsychotics such as haloperidol and aripiprazole affect cholesterol biosynthesis at the conversion of 7-dehydrocholesterol (7-DHC) to cholesterol. This transformation is promoted by the enzyme DHCR7 and its inhibition causes increases in plasma and tissue levels of 7-DHC...
June 15, 2018: Toxicology and Applied Pharmacology
Eva Ceskova, Petr Silhan
In spite of tremendous development in central nervous system research, current treatment is suboptimal, especially in severe mental disorders. In medicine, there are two main methods of improving the health care provided: seeking new treatment procedures and perfecting (optimizing) the existing ones. Optimization of treatment includes not only practical tools such as therapeutic drug monitoring but also implementation of general trends in the clinical practice. New pharmacological options include new more sophisticated forms of monoaminergic drugs, old drugs rediscovered on the base of a better understanding of pathophysiology of mental illnesses, and drugs aimed at new treatment targets...
2018: Neuropsychiatric Disease and Treatment
Bruno Romeo, Lisa Blecha, Katia Locatelli, Amine Benyamina, Catherine Martelli
The objective of this meta-analysis is to assess the efficacy and safety of partial and complete dopamine agonists in the treatment of acute mood disorder episodes. Randomized, double-blind and placebo-controlled trials of dopamine agonists in the treatment of acute mood disorder episodes were identified in the MEDLINE and PsycINFO databases and included in the meta-analysis. In monotherapy of mania, improved remission rates were found for cariprazine (odds ratio (OR): 2.08, P < 0.01) and for high-dose aripiprazole (OR: 3...
April 2018: Journal of Psychopharmacology
Traci Aladeen, Erica Westphal, Yena Lee, Carola Rong, Michelle Rainka, Horacio Capote, Roger S McIntyre
PURPOSE: We sought to characterize the clinical experience of outpatients treated with brexpiprazole after achieving suboptimal outcomes with aripiprazole or bupropion as determined by the treating psychiatric provider. DESIGN AND METHODS: Case series; inefficacy, intolerability, or other unsatisfactory outcome to previous trial with aripiprazole or bupropion. FINDINGS: The majority of individuals in our sample exhibited tolerability of brexpiprazole...
October 2018: Perspectives in Psychiatric Care
Emmanuelle Weiller, Catherine Weiss, Christopher P Watling, Christopher Edge, Mary Hobart, Hans Eriksson, Maurizio Fava
Objective: Patients with major depressive disorder (MDD) with inadequate response to antidepressant treatment (ADT) may suffer a prolonged loss of functioning. This review aimed to determine if self-rated functional measures are informative in randomized placebo-controlled studies of adjunctive therapy in patients with MDD and inadequate response to ADT. Methods: This was a systematic literature review of articles in any language from the MEDLINE database published between January 1990 and March 2017...
2018: Neuropsychiatric Disease and Treatment
Judy Hope, David Castle, Nicholas A Keks
OBJECTIVES: Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole. CONCLUSIONS: Brexpiprazole and aripiprazole are both partial agonists at dopamine D2 , and serotonin 5-HT1A and antagonists at serotonin 5-HT2A and noradrenergic α1B receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation...
February 2018: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
Awais Aftab, Keming Gao
Brexpiprazole is the most recently approved second-generation antipsychotic, which is used as adjunctive therapy to antidepressants for treating major depressive disorder (MDD) with inadequate response. Brexpiprazole shares pharmacological similarities with other second-generation antipsychotics, especially aripiprazole. Area covered: This review provides a detailed overview of the pre-clinical studies of brexpiprazole, followed by a summary of its clinical studies, and a comparison with other antipsychotics in MDD...
October 2017: Expert Opinion on Drug Discovery
Nishant B Parikh, Diana M Robinson, Anita H Clayton
Brexpiprazole, a serotonin-dopamine activity modulator, is the second D2 partial agonist to come to market and has been approved for the treatment of schizophrenia and as an adjunctive treatment in major depressive disorder. With less intrinsic activity than aripiprazole at the D2 receptor and higher potency at 5-HT2A , 5-HT1A , and α1B receptors, the pharmacological properties of brexpiprazole suggest a more tolerable side effect profile with regard to akathisia, extrapyramidal dysfunction, and sedation. While no head-to-head data are currently available, double-blind placebo-controlled studies show favorable results, with the number needed to treat (NNT) vs placebo of 6-15 for response in acute schizophrenia treatment and 4 for maintenance...
2017: Therapeutics and Clinical Risk Management
Kinjal Patel, Petal S Abdool, Tarek K Rajji, Benoit H Mulsant
Evidence on the pharmacotherapy of late-life major depressive disorder (LLD) is scant. Most of the recommendations in existing clinical guidelines are based on expert opinions, extrapolations from data obtained in younger patients, or theoretical considerations. Areas covered: This article summarizes the recommendations from existing clinical guidelines and recent reviews on the treatment of LLD. Next, it discusses the potential role of newer antidepressants - vilazodone, levomilnacipran, and vortioxetine - based on a systematic search of the literature published during the past five years...
April 2017: Expert Opinion on Pharmacotherapy
Joshua S Frankel, Thomas L Schwartz
BACKGROUND: Brexpiprazole and cariprazine are the latest US Food and Drug Administration approved atypical antipsychotics available in the United States. Both function as partial agonists of the dopamine-2 receptor (D2 R), a mechanism of action shared with aripiprazole. However, all three differ in their affinities for the D2 R as well as for serotonin receptors (5-HTRs). This paper seeks to delineate these pharmacodynamic and clinical differences amongst the three dopamine partial agonist atypical antipsychotic drugs...
January 2017: Therapeutic Advances in Psychopharmacology
Cedric Mombereau, Jørn Arnt, Arne Mørk
Previous studies have shown that partial and full 5-HT1A receptor agonists reduce antipsychotic-induced catalepsy. Consequently, some antipsychotics combining balanced efficacy between dopamine (DA) D2 antagonism or partial agonism and 5-HT1A receptor agonism have a low propensity to induce extrapyramidal side effects (EPS), as reflected by low cataleptogenic activity in rodents. In the present experiments, we attempted to explore the importance of pre- and postsynaptic 5-HT1A agonistic properties of brexpiprazole and aripiprazole in the context of neurological side-effect liabilities...
February 2017: Pharmacology, Biochemistry, and Behavior
Leslie Citrome
There are several new and emerging medication interventions for both the acute and maintenance treatment phases of schizophrenia. Recently approved are 2 new dopamine receptor partial agonists, brexpiprazole and cariprazine, as well as 2 new long-acting injectable antipsychotic formulations, aripiprazole lauroxil and 3-month paliperidone palmitate. Although differences in efficacy compared to other available choices are not expected, the new oral options offer different tolerability profiles that may be attractive for individual patients who have had difficulties with older medications...
December 2016: CNS Spectrums
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