From the Guidelines
Brexpiprazole is an atypical antipsychotic medication used primarily to treat schizophrenia and as an add-on treatment for major depressive disorder. It's typically prescribed at starting doses of 1 mg once daily for depression and 1-2 mg daily for schizophrenia, with gradual increases to therapeutic doses of 2-3 mg daily for depression and 2-4 mg daily for schizophrenia. Brexpiprazole works by partially activating serotonin and dopamine receptors while blocking other receptors, providing a balance that helps control symptoms with potentially fewer side effects than older antipsychotics.
Key Points
- Common side effects include weight gain, akathisia (restlessness), and sedation 1.
- The medication should be taken consistently, with or without food, and patients should avoid abrupt discontinuation.
- Regular monitoring for metabolic changes, movement disorders, and other side effects is necessary.
- Brexpiprazole may take several weeks to reach full effectiveness, so patients should continue taking it as prescribed even if they don't notice immediate benefits.
Mechanism of Action
Atypical antipsychotics, including Brexpiprazole, affect a number of neurotransmitter systems, including both antidopaminergic and antiserotonergic activity 1. This mechanism of action is responsible for their antipsychotic properties and characteristic side-effect profile.
Clinical Use
In the adult literature, atypical agents are at least as effective for positive symptoms, and possibly more effective for negative symptoms, compared to traditional neuroleptics 1. However, their potential for other serious side effects, especially weight gain, is a significant clinical issue.
Monitoring and Side Effects
Weekly blood cell counts are obtained during the first 6 months of treatment with certain atypical antipsychotics, then every 2 weeks thereafter, including testing during the 4 weeks after the medication is stopped 1. The guidelines for monitoring and managing side effects, such as weight gain and extrapyramidal symptoms, should be followed closely.
Medication Choice
The choice of medication should be made on the basis of the agent’s relative potency, potential side effects, and the patient’s history of medication response 1. Individual responses to different antipsychotics are variable, and if insufficient effects are evident after a 6-week trial using adequate dosages, a different antipsychotic agent should be tried.
From the FDA Drug Label
Brexpiprazole is an atypical antipsychotic indicated for: Use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults. Treatment of schizophrenia in adults.
Brexpiprazole is an atypical antipsychotic. It is indicated for two main uses:
- As an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults.
- For the treatment of schizophrenia in adults 2, 2. The chemical structure of Brexpiprazole is defined as 7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one 2.
From the Research
Overview of Brexpiprazole
- Brexpiprazole is an atypical antipsychotic medication that received approval by the U.S. Food and Drug Administration for the treatment of schizophrenia and as an adjunctive treatment for major depressive disorder 3, 4, 5, 6, 7.
- It acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A and adrenergic alpha1B and alpha2C receptors 3, 4, 6.
Efficacy and Safety
- Brexpiprazole has demonstrated efficacy in treating schizophrenia and preventing relapse, with a number needed to treat (NNT) of 7 for response in acute schizophrenia treatment and 4 for maintenance 3, 5.
- In major depressive disorder, brexpiprazole has shown efficacy as an adjunct to antidepressants, with an NNT of 12 for response and 17-31 for remission vs placebo 4, 5.
- Common adverse events include akathisia, weight gain, and gastrointestinal side effects, with a relatively favorable safety profile compared to other antipsychotic agents 3, 4, 5, 6, 7.
Dosage and Administration
- The recommended dose range of brexpiprazole for the treatment of schizophrenia is 2-4 mg/day, and 2 mg/day for major depressive disorder 3, 4, 5, 6.
- Brexpiprazole should be titrated up to its target dose over 1-2 weeks and is effective in once-daily dosing 6.
Clinical Role
- Brexpiprazole appears to be a viable option for treating acute exacerbations of schizophrenia and adjunctive treatment of major depressive disorder in patients who have shown an inadequate response to antidepressants 7.
- Further clinical trials are needed to determine the long-term efficacy of brexpiprazole and to establish its place in therapy compared to other antipsychotic agents 4, 7.