Brexpiprazole

Brexpiprazole (Rexulti): An Atypical Antipsychotic for Schizophrenia and Major Depressive Disorder

Brexpiprazole, sold under the brand name Rexulti, is an atypical antipsychotic medication primarily used in the treatment of schizophrenia and as an adjunctive therapy to antidepressants in major depressive disorder (MDD). This article discusses the therapeutic applications, mechanism of action, pharmacokinetics, side effects, and clinical considerations of Brexpiprazole.

Introduction

Brexpiprazole belongs to the class of atypical antipsychotics, which are known for their use in treating psychiatric disorders. It has been approved for clinical use in various countries and offers an alternative to other medications in its class.

• Brexpiprazole (Rexulti) is an atypical antipsychotic used to treat schizophrenia and as an add on to an antidepressant to treat major depressive disorder.

What are the uses of this medicine?

This medicine is used to treat:

• Major depressive disorder (MDD): Rexulti is used with antidepressant medicines, when your healthcare provider determines that an antidepressant alone is not enough to treat your depression.
• Schizophrenia

How does this medicine work?

• 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.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• a known hypersensitivity to brexpiprazole or any of its components.

What drug interactions can this medicine cause?

Factors	Dosage Adjustments for Rexulti
*Rexulti may be administered without dosage adjustment in patients with MDD when administered with strong CYP2D6 inhibitors (e.g., paroxetine, fluoxetine).
Strong CYP2D6* or CYP3A4 inhibitors	Administer half of usual dose.
Strong/moderate CYP2D6 with Strong/moderate CYP3A4 inhibitors	Administer a quarter of usual dose.

Therapeutic Uses

Brexpiprazole is utilized in treating two primary conditions:

• Schizophrenia, where it helps to manage symptoms such as hallucinations, delusions, and disorganized thinking.
• As an add-on treatment to an antidepressant for patients with MDD who have not responded adequately to antidepressant therapy alone.

Pharmacology

Brexpiprazole acts on various receptors in the brain, which is believed to contribute to its antipsychotic and antidepressant effects.

Mechanism of Action

Brexpiprazole modulates the activity of several neurotransmitter pathways in the brain, including dopamine and serotonin systems, which are implicated in schizophrenia and depression.

Pharmacokinetics

The medication is absorbed orally, with its bioavailability unaffected by food. It undergoes hepatic metabolism and is excreted through urine and feces.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage: Adjunctive Treatment of Major Depressive Disorder

• The recommended starting dosage for Rexulti as adjunctive treatment is 0.5 mg or 1 mg once daily, taken orally with or without food.
• Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily.
• Dosage increases should occur at weekly intervals based on the patient's clinical response and tolerability.
• The maximum recommended daily dosage is 3 mg.
• Periodically reassess to determine the continued need and appropriate dosage for treatment.

Treatment of Schizophrenia

• The recommended starting dosage for Rexulti is 1 mg once daily on Days 1 to 4, taken orally with or without food.
• The recommended target Rexulti dosage is 2 mg to 4 mg once daily.
• Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient's clinical response and tolerability.
• The maximum recommended daily dosage is 4 mg.

Dosage Adjustments for Hepatic Impairment

• Moderate to Severe Hepatic Impairment (Child-Pugh score ≥7): Maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia.
• Moderate, Severe or End-Stage Renal Impairment (CLcr<60 mL/minute): Maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia.

Dosage Adjustments for Renal Impairment

• For patients with moderate, severe or end-stage renal impairment (creatinine clearance CLcr<60 mL/minute), the maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia.

Administration

• Take Rexulti exactly as your healthcare provider tells you to take it.
• Do not change the dose or stop taking Rexulti yourself.
• Rexulti can be taken with or without food.
• You should not miss a dose of Rexulti.
• If you miss a dose, take the missed dose as soon as you remember.
• If you are close to your next dose, just skip the missed dose and take your next dose at your regular time.
• Do not take 2 doses of Rexulti at the same time.
• If you are not sure about your dosing, call your healthcare provider.
• If you take too much Rexulti, call your healthcare provider or Poison Control Center at 1-800-222-1222 right away, or go to the nearest hospital emergency room.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg

This medicine is available in fallowing brand namesː

• Rexulti

What side effects can this medication cause?

The most common side effects of this medicine include:

• MDD: Weight increased and akathisia
• Schizophrenia: Weight increased

What special precautions should I follow?

• Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Rexulti is not approved for the treatment of patients with dementia-related psychosis.
• Antidepressants increased the risk of suicidal thoughts and behaviors in patients aged 24 years and younger in short-term studies. Monitor closely for clinical worsening and for emergence of suicidal thoughts and behaviors. The safety and efficacy of Rexulti have not been established in pediatric patients.
• Rexulti is not approved for the treatment of patients with dementia-related psychosis.
• Neuroleptic malignant syndrome may occur. Manage with immediate discontinuation and close monitoring.
• Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with antipsychotic drugs. Discontinue if clinically appropriate.
• Atypical antipsychotic drugs, including Rexulti, have caused metabolic changes, including hyperglycemia, diabetes mellitus, dyslipidemia, and body weight gain. Monitor for hyperglycemia/diabetes mellitus, dyslipidemia and weight gain.
• Leukopenia and neutropenia have been reported during treatment with antipsychotic agents. Agranulocytosis (including fatal cases) has been reported. Perform complete blood counts (CBC) in patients with pre-existing low white blood cell count (WBC) or history of leukopenia or neutropenia. Consider discontinuing Rexulti if a clinically significant decline in WBC occurs in absence of other causative factors.
• Orthostatic hypotension and syncope may occur. Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope.
• Seizures may occur. Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.

What to do in case of emergency/overdose?

• Consult a Certified Poison Control Center (1-800-222-1222 or www.poison.org) for up-to-date guidance and advice regarding a Rexulti overdosage.

Management for overdosage:

• Management of 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.
• 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.

Can this medicine be used in pregnancy?

• Adequate and well-controlled studies have not been conducted with Rexulti in pregnant women to inform drug-associated risks.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to Rexulti during pregnancy. For more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.
• Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: brexpiprazole
• Inactive ingredients: lactose monohydrate, corn starch, microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate, hypromellose, and talc

Who manufactures and distributes this medicine?

• Manufactured by Otsuka Pharmaceutical Co., Ltd., Tokyo 101-8535, Japan
• Distributed and Marketed by Otsuka America Pharmaceutical, Inc., Rockville

What should I know about storage and disposal of this medication?

• Store Rexulti at room temperature, between 68°F to 77°F (20°C to 25°C).
• Keep Rexulti and all medicines out of the reach of children.

Side Effects

As with any medication, Brexpiprazole can cause side effects. These may include, but are not limited to:

• Weight gain
• Akathisia (a feeling of restlessness)
• Sedation
• Gastrointestinal disturbances

Clinical Considerations

File:Psychiatric consultation.jpg

A psychiatrist discussing medication options with a patient, including the use of Brexpiprazole.

When prescribing Brexpiprazole, clinicians consider several factors:

• Potential drug-drug interactions, particularly with medications metabolized by the liver.
• The risk of side effects, which may require regular monitoring of weight, blood sugar, and cholesterol.
• The patient's overall health and medication history.

Conclusion

Brexpiprazole (Rexulti) offers an important option for patients with schizophrenia or MDD who require adjunctive treatment. Ongoing research continues to clarify its role in the management of psychiatric disorders and its long-term safety profile.

• Dailymed label info on Brexpiprazole
• FDA Brexpiprazole

Brexpiprazole Resources
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Brexpiprazole Resources
Need Help Finding a Doctor? Need help finding a doctor or specialist anywhere in the world? Explore our world directory. WikiMD's DocFinder can assist you in locating millions of physicians.	Medical Knowledge Access the latest research - Most recent articles Ongoing trials.

Translate to: East Asian 中文, 日本, 한국어, South Asian हिन्दी, Urdu, বাংলা, తెలుగు, தமிழ், ಕನ್ನಡ,
Southeast Asian Indonesian, Vietnamese, Thai, မြန်မာဘာသာ, European español, Deutsch, français, русский, português do Brasil, Italian, polski