Brexpiprazole

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Information about Brexpiprazole

Brexpiprazole is an atypical antipsychotic used in the treatment of schizophrenia and major depressive disorders.

Liver safety of Brexpiprazole

Brexpiprazole has been associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent acute liver injury.

Mechanism of action of Brexpiprazole

Brexpiprazole (brex pip' ra zole) is a second generation (atypical) antipsychotic agent that is similar in structure and mechanism of action to aripiprazole. These two agents are believed to act as partial antagonists of dopamine type 2 (D2) and serotonin (5-HT)-2A receptors and partial agonists of serotonin 5-HT-1A receptors. In several randomized controlled trials, therapy with brexpiprazole was associated with a lessening of symptoms of schizophrenia and improvement in depression symptom scores in comparison to placebo treatment.

FDA approval information for Brexpiprazole

It was approved for use in the United States in 2015 as therapy for schizophrenia and as adjunctive therapy with antidepressants for major depressive disorders.

Dosage and administration for Brexpiprazole

Brexpiprazole is available as tablets of 0.25, 0.5, 1, 2, 3 and 4 mg under the brand name Rexulti. The standard maintenance dose for schizophrenia in adults is 2 to 4 mg daily. The dose for as an adjunctive therapy for major depression is usually less.

Side effects of Brexpiprazole

Common side effects include restlessness (akathisia), sedation, tremor, dizziness, blurred vision, fatigue, headaches, nausea and weight gain. Rare, but potential severe adverse reactions (mentioned in most antipsychotic product labels) include tardive dyskinesia, major neurologic events, neuroleptic malignant syndrome, orthostatic hypotension, seizures and neutropenia.

Antipsychotic agents

First Generation

Second Generation (Atypicals)


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