Brand Name

Rexulti

Generic Name
Brexpiprazole
View Brand Information
FDA approval date: July 10, 2015
Classification: Atypical Antipsychotic
Form: Tablet, Kit

What is Rexulti (Brexpiprazole)?

Living with depression or schizophrenia can deeply affect every aspect of life, from relationships to work to simple daily motivation. Rexulti (brexpiprazole) offers a modern treatment option designed to help restore emotional balance and reduce distressing symptoms in people struggling with these conditions. As a newer-generation antipsychotic medication, Rexulti is often prescribed to support mood stabilization, improve clarity of thought, and enhance overall quality of life.

Approved by the U.S. Food and Drug Administration (FDA) in 2015, Rexulti belongs to a class of medications known as atypical antipsychotics. It’s typically used as an adjunct therapy for major depressive disorder (MDD) or as a primary treatment for schizophrenia. Its balanced approach to dopamine and serotonin regulation helps patients achieve symptom control with fewer sedative or movement-related side effects than older antipsychotic medications.

What does Rexulti do?

Rexulti is prescribed for:

  • Major depressive disorder (MDD): Used along with antidepressants when symptoms like low mood, loss of interest, or fatigue do not fully respond to antidepressant therapy alone.
  • Schizophrenia: Helps reduce symptoms such as hallucinations, disorganized thinking, and emotional withdrawal.

By restoring balance to brain chemicals that influence mood, behavior, and perception, Rexulti can help patients experience more stable emotions, clearer thinking, and improved daily functioning.

Clinical studies have shown that Rexulti, when combined with antidepressants, can lead to significant improvements in depressive symptoms and overall quality of life compared with antidepressants alone (FDA, 2015; Mayo Clinic, 2024). In schizophrenia, many patients report a calmer mood, reduced paranoia, and improved ability to engage in everyday activities.

How does Rexulti work?

Rexulti works by modulating dopamine and serotonin receptors in the brain, two key neurotransmitters involved in mood, motivation, and cognition. Specifically, it acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors.

In simpler terms, Rexulti helps balance chemical signals in the brain that are either overactive (as in schizophrenia) or underactive (as in depression). This fine-tuning reduces extreme mood swings, stabilizes thought patterns, and helps patients feel more emotionally grounded.

Clinically, this mechanism matters because it provides the benefits of dopamine regulation without causing the intense receptor blockade that can lead to stiffness, restlessness, or excessive sedation; side effects often seen with older antipsychotics.

Rexulti side effects

Like all prescription medications, Rexulti can cause side effects, though many are mild and manageable. Understanding them helps patients make informed decisions and know when to reach out for support.

Common side effects:

  • Weight gain
  • Drowsiness or fatigue
  • Headache
  • Dizziness or lightheadedness
  • Restlessness (akathisia)

Less common side effects:

  • Constipation
  • Increased appetite
  • Anxiety or sleep disturbances

Serious but rare side effects:

  • Uncontrolled muscle movements (tardive dyskinesia)
  • Increased blood sugar, cholesterol, or triglycerides
  • Signs of neuroleptic malignant syndrome (severe muscle rigidity, fever, confusion) — a medical emergency

Patients should contact a doctor immediately if they experience severe stiffness, rapid heartbeat, confusion, or unusual involuntary movements.

Who should avoid Rexulti:

  • Individuals with a history of allergic reaction to brexpiprazole
  • Patients with significant liver or kidney impairment may require dosage adjustments
  • Rexulti is not approved for use in children under 13 years old for depression or under 18 for schizophrenia

The medication carries a boxed warning regarding increased risk of suicidal thoughts in young adults, a risk shared by most antidepressant and adjunctive treatments. Regular follow-up with a healthcare provider is essential to monitor safety and emotional well-being (NIH, 2024).

Rexulti dosage

Rexulti is available as an oral tablet taken once daily, with or without food. The dose is individualized based on the condition being treated, patient response, and other medications in use.

Because Rexulti affects brain chemistry and metabolism, healthcare providers often monitor:

  • Mood and behavioral changes, especially during early treatment
  • Weight and blood sugar levels over time
  • Lipid profile and blood pressure for patients on long-term therapy

Regular communication with your healthcare provider helps ensure the dose remains both effective and safe.

Special considerations:

  • Older adults with dementia-related psychosis should not take Rexulti due to increased mortality risk.
  • Patients taking strong CYP2D6 or CYP3A4 inhibitors (certain antidepressants or antifungals) may need lower doses to prevent side effects.

Does Rexulti have a generic version?

As of 2025, no FDA-approved generic version of Rexulti (brexpiprazole) is available in the United States. It is currently sold only as the brand-name product developed by Otsuka Pharmaceutical and Lundbeck. However, international versions may exist in other markets.

Once a generic version becomes available, it will meet the same rigorous FDA standards for quality, strength, and clinical effectiveness as the brand-name product. Patients can also inquire about manufacturer assistance programs or copay savings cards that help reduce out-of-pocket costs.

Conclusion

Rexulti provides a well-tolerated, effective treatment option for adults living with major depressive disorder or schizophrenia. Targeting key brain receptors that regulate mood and cognition helps reduce symptoms and support long-term emotional stability.

While every patient’s experience may differ, many find Rexulti easier to tolerate than older antipsychotic medications, especially regarding movement and metabolic side effects. Consistent follow-up, healthy lifestyle choices, and open dialogue with a healthcare provider can further enhance treatment success.

When prescribed and monitored by a qualified professional, Rexulti can be a safe and empowering part of a broader mental health plan, helping patients regain clarity, connection, and confidence in their daily lives.

References

  1. U.S. Food and Drug Administration. (2015). Rexulti (brexpiprazole) prescribing information. Retrieved from https://www.fda.gov
  2. Mayo Clinic. (2024). Brexpiprazole (oral route): Uses and side effects. Retrieved from https://www.mayoclinic.org
  3. National Institutes of Health. (2024). Brexpiprazole – Drug information. Retrieved from https://medlineplus.gov

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Brand Information

Rexulti (brexpiprazole)
1INDICATIONS AND USAGE
REXULTI is indicated for:
  • Adjunctive treatment to antidepressants for major depressive disorder (MDD) in adults
  • Treatment of schizophrenia in adults and pediatric patients ages 13 years and older
  • Treatment of agitation associated with dementia due to Alzheimer's disease
Limitations of Use:
REXULTI is not indicated as an as needed ("prn") treatment for agitation associated with dementia due to Alzheimer's disease [see
2DOSAGE FORMS AND STRENGTHS
REXULTI tablets are available in 6 strengths:
  • 0.25 mg tablets are light brown, round, shallow convex, bevel-edged body with "BRX" and "0.25" imprinted on one side.
  • 0.5 mg tablets: are light orange, round, shallow convex, bevel-edged body with "BRX" and "0.5" imprinted on one side.
  • 1 mg tablets are light yellow, round, shallow convex, bevel-edged body with "BRX" and "1" imprinted on one side.
  • 2 mg tablets are light green, round, shallow convex, bevel-edged body with "BRX" and "2" imprinted on one side.
  • 3 mg tablets are light purple, round, shallow convex, bevel-edged body with "BRX" and "3" imprinted on one side.
  • 4 mg tablets are white, round, shallow convex, bevel-edged body with "BRX" and "4" imprinted on one side.
3CONTRAINDICATIONS
REXULTI is contraindicated in patients with a known hypersensitivity to brexpiprazole or any of its components. Reactions have included rash, facial swelling, urticaria, and anaphylaxis.
4ADVERSE REACTIONS
The following adverse reactions are discussed in more detail in other sections of the labeling:
  • Increased Mortality in Elderly Patients with Dementia-Related Psychosis
  • Suicidal Thoughts and Behaviors in Adolescents and Young Adults
  • Cerebrovascular Adverse Reactions Including Stroke in Elderly Patients with Dementia-Related Psychosis
  • Neuroleptic Malignant Syndrome (NMS)
  • Tardive Dyskinesia
  • Metabolic Changes
  • Pathological Gambling and Other Compulsive Behaviors
  • Leukopenia, Neutropenia, and Agranulocytosis
  • Orthostatic Hypotension and Syncope
  • Falls
  • Seizures
  • Body Temperature Dysregulation
  • Dysphagia
  • Potential for Cognitive and Motor Impairment
4.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
The most common adverse reactions in adult patients in clinical trials (≥5%) were weight increased, akathisia, headache, somnolence, and insomnia.
The most common adverse reactions in pediatric patients in clinical trials (≥5%) were weight increased, somnolence, headache, akathisia, and nasopharyngitis.
Brexpiprazole has been evaluated for safety in 12,550 adult patients who participated in multiple-dose clinical trials for major depressive disorder, schizophrenia, agitation associated with dementia due to Alzheimer's disease, attention deficit hyperactivity disorder (ADHD), post-traumatic stress disorder (PTSD), bipolar mania, and borderline personality disorder (BPD). Among them, 3,870 patients were treated with brexpiprazole for at least 180 days, and 1,910 patients were treated for at least one year of exposure.
Additionally, brexpiprazole has been evaluated for safety in 119 pediatric patients who participated in short-term trials, and 314 patients in long-term multiple-dose clinical trials for pediatric schizophrenia and autism spectrum disorders (ASD).
4.2Postmarketing Experience
The following adverse reaction has been identified during post-approval use of REXULTI. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Nervous System disorders: Neuroleptic Malignant Syndrome
5OVERDOSAGE
There is limited clinical trial experience regarding human overdosage with REXULTI.
Management of a REXULTI overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers. Consider contacting the Poison Help Line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.
Oral activated charcoal and sorbitol (50 g/240 mL), administered one hour after ingesting oral REXULTI, decreased brexpiprazole C
There is no information on the effect of hemodialysis in treating an overdose with REXULTI; hemodialysis is unlikely to be useful because brexpiprazole is highly bound to plasma proteins.
6DESCRIPTION
Brexpiprazole, an atypical antipsychotic, is available as REXULTI
REXULTI tablets are for oral administration and are available in 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg strengths. Inactive ingredients include lactose monohydrate, corn starch, microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate, hypromellose, and talc. Colorants include titanium dioxide, iron oxide, and ferrosoferric oxide.
7PATIENT COUNSELING INFORMATION
Advise the patient or caregiver to read the FDA-approved patient labeling (Medication Guide).
8PRINCIPAL DISPLAY PANEL - 0.25 mg Tablet Bottle Label
0.25 mg
30 Tablets
NDC 59148-035-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 0.25 mg Tablet Bottle Label
9PRINCIPAL DISPLAY PANEL - 0.25 mg Tablet Bottle Carton
0.25 mg
30 Tablets
REXULTI
Rx only
Keep out of the
DISPENSE THE
PRINCIPAL DISPLAY PANEL - 0.25 mg Tablet Bottle Carton
10PRINCIPAL DISPLAY PANEL - 0.5 mg Tablet Bottle Label
0.5 mg
30 Tablets
NDC 59148-036-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 0.5 mg Tablet Bottle Label
11PRINCIPAL DISPLAY PANEL - 0.5 mg Tablet Bottle Carton
0.5 mg
30 Tablets
REXULTI
Rx only
Keep out of the
DISPENSE THE
PRINCIPAL DISPLAY PANEL - 0.5 mg Tablet Bottle Carton
12PRINCIPAL DISPLAY PANEL - 1 mg Tablet Bottle Label
1 mg
30 Tablets
NDC 59148-037-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 1 mg Tablet Bottle Label
13PRINCIPAL DISPLAY PANEL - 1 mg Tablet Bottle Carton
1 mg
30 Tablets
REXULTI
Rx only
Keep out of the
DISPENSE THE
PRINCIPAL DISPLAY PANEL - 1 mg Tablet Bottle Carton
14PRINCIPAL DISPLAY PANEL - 2 mg Tablet Bottle Label
2 mg
30 Tablets
NDC 59148-038-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 2 mg Tablet Bottle Label
15PRINCIPAL DISPLAY PANEL - 2 mg Tablet Bottle Carton
2 mg
30 Tablets
REXULTI
Rx only
Keep out of the
DISPENSE THE
PRINCIPAL DISPLAY PANEL - 2 mg Tablet Bottle Carton
16PRINCIPAL DISPLAY PANEL - 3 mg Tablet Bottle Label
3 mg
30 Tablets
NDC 59148-039-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 3 mg Tablet Bottle Label
17PRINCIPAL DISPLAY PANEL - 3 mg Tablet Bottle Carton
3 mg
30 Tablets
REXULTI
Rx only
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DISPENSE THE
PRINCIPAL DISPLAY PANEL - 3 mg Tablet Bottle Carton
18PRINCIPAL DISPLAY PANEL - 4 mg Tablet Bottle Label
4 mg
30 Tablets
NDC 59148-040-13
REXULTI
Rx only
Keep out of the reach of children
DISPENSE THE
Otsuka
Lundbeck
PRINCIPAL DISPLAY PANEL - 4 mg Tablet Bottle Label
19PRINCIPAL DISPLAY PANEL - 4 mg Tablet Bottle Carton
4 mg
30 Tablets
REXULTI
Rx only
Keep out of the
DISPENSE THE
PRINCIPAL DISPLAY PANEL - 4 mg Tablet Bottle Carton