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Carl Björkholm, Monica M Marcus, Åsa Konradsson-Geuken, Kent Jardemark, Torgny H Svensson
Brexpiprazole (Rexulti® ), a novel D2/3 receptor (R) partial agonist, was recently approved as monotherapy for schizophrenia, demonstrating effectiveness against both positive and negative symptoms, and also approved as add-on treatment to antidepressant drugs, inducing a potent antidepressant effect with a faster onset compared to an antidepressant given alone. Moreover, brexpiprazole has demonstrated pro-cognitive effects in preclinical studies. To explore whether the observed effects may be mediated via modulation of prefrontal glutamatergic transmission, we investigated the effect of brexpiprazole, alone and in combination with the SSRI escitalopram, on prefrontal glutamatergic transmission using in vitro electrophysiological intracellular recordings of deep layer pyramidal cells of the rat medial prefrontal cortex (mPFC)...
April 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Shannon Eaves, Jose A Rey
Brexpiprazole (Rexulti): a new monotherapy for schizophrenia and adjunctive therapy for major depressive disorder.
July 2016: P & T: a Peer-reviewed Journal for Formulary Management
Karly P Garnock-Jones
Oral brexpiprazole (Rexulti(®)) is a partial dopamine D2 agonist, which also has activity at several other receptors. This article reviews the pharmacological properties of brexpiprazole and its clinical efficacy and tolerability in patients with schizophrenia; its use in patients with major depressive disorder is beyond the scope of this review. Brexpiprazole 2-4 mg/day was generally effective in short-term, phase III studies at improving Positive and Negative Symptom Scale scores and other schizophrenia symptoms in patients with acute schizophrenia...
April 2016: CNS Drugs
Kate McKeage
Brexpiprazole (Rexulti(®)) is a serotonin-dopamine activity modulator, with a unique receptor binding profile and low intrinsic D2 activity suggestive of a lower potential than aripiprazole to cause activation-like adverse effects, such as akathisia. The drug was recently approved by the US FDA for adjunctive therapy with antidepressant treatment (ADT) in patients with major depressive disorder (MDD). In two phase III trials, adjunctive oral brexpiprazole 2 or 3 mg once daily was more effective than monotherapy with ADT in improving depressive symptoms in adults with MDD who demonstrated an incomplete response to previous treatment with ADT...
February 2016: CNS Drugs
Kunj Gohil
Sacubitril/valsartan (Entresto) for chronic heart failure; brexpiprazole (Rexulti) for major depressive disorder and schizophrenia; and lumacaftor/ivacaftor (Orkambi) for cystic fibrosis involving specific CFTR mutations.
September 2015: P & T: a Peer-reviewed Journal for Formulary Management
Sarah L Greig
Brexpiprazole (Rexulti®) is an atypical antipsychotic that has been developed by Otsuka Pharmaceutical Co. Ltd and H. Lundbeck A/S as an oral treatment for several psychiatric disorders. Brexpiprazole is a novel serotonin-dopamine activity modulator that acts as a partial agonist of serotonin 1A (5-HT1A) and dopamine D2 receptors, as well as a potent antagonist of 5-HT2A receptors and noradrenergic α1B and α2C receptors. In July 2015, brexpiprazole received its first approval in the USA for use as an adjunctive treatment of major depressive disorder (MDD) and the treatment of schizophrenia...
September 2015: Drugs
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August 17, 2015: Medical Letter on Drugs and Therapeutics
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