Rexulti Uses, Dosage, Side Effects, Food Interaction and all others data.

The mechanism of action of brexpiprazole in the treatment of major depressive disorder or schizophrenia is unknown. However, the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors.

Trade Name Rexulti
Availability Prescription only
Generic Brexpiprazole
Brexpiprazole Other Names Brexpiprazole
Related Drugs Rexulti, sertraline, trazodone, Lexapro, Zoloft, citalopram, quetiapine, Abilify, Cymbalta, Prozac
Weight 0.25mg, 0.5mg, 1mg, 2mg, 3mg, 4mg,
Type Tablet, Oral Tablet
Formula C25H27N3O2S
Weight Average: 433.57
Monoisotopic: 433.182398295
Protein binding

>99% protein bound in plasma to serum albumin and α1-acid glycoprotein. Based on in vitro studies, protein binding is not affected by warfarin, diazepam, or digitoxin.

Groups Approved, Investigational
Therapeutic Class Benzodiazepine antagonist
Manufacturer Aja Pharmaceutical Industries
Available Country Canada, Australia, Saudi Arabia, United States,
Last Updated: September 19, 2023 at 7:00 am


Rexulti is an atypical antipsychotic used for:

  • Use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD)
  • Treatment of schizophrenia

Dosage Adjustments for Hepatic Impairment: For patients with moderate to severe hepatic impairment, the 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

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

Geriatric Use: In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, and cardiac function, concomitant diseases, and other drug therapy.

Rexulti is also used to associated treatment for these conditions: Major Depressive Disorder (MDD), Schizophrenia

How Rexulti works

Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.


Rexulti 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.


The most commonly observed adverse effects include: weight increase, akathisia, somnolence, tremor and nasopharyngitis. Neonates are at risk for extrapyramidal and/or withdrawal symptoms if exposed to an antipsychotic drug during the third trimester of development.


Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-

  • Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g. stroke, transient ischemic attack)
  • Neuroleptic Malignant Syndrome: Manage with immediate discontinuation and close monitoring
  • Tardive Dyskinesia: Discontinue if clinically appropriate
  • Metabolic Changes: Monitor for hyperglycemia/diabetes mellitus, dyslipidemia and weight gain
  • Pathological Gambling and Other Compulsive Behaviors: Consider dose reduction or discontinuation
  • Leukopenia, Neutropenia, and Agranulocytosis: 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: Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope
  • Seizures: Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold

Food Interaction

  • Avoid St. John's Wort. This herb induces the CYP3A metabolism of brexpiprazole and may reduce its serum concentration. The dose of Rexulti should be doubled if administered with St. John's wort.
  • Drink plenty of fluids.
  • Take with or without food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Rexulti Cholesterol interaction

[Moderate] Atypical antipsychotic drugs have been associated with undesirable alterations in lipid levels.

While all agents in the class have been shown to produce some changes, each drug has its own specific risk profile.

Before or soon after initiation of antipsychotic medication, obtain a fasting lipid profile at baseline and monitor periodically during treatment.

Volume of Distribution

Intravenous volume of distribution is 1.56L/kg.

Elimination Route

Rexulti reaches peak plasma concentration within 4 hours of administration, and steady state occurs within 10-12 days of dosing. Oral bioavailability is 95%, and can be administered with or without food.

Half Life

Rexulti and its major metabolite, DM-3411 have half lives of 91 and 96 hours respectively.



Elimination Route

Approximately 25% urinary and 46% fecal excretion. <1% and ~14% of the unchanged drug was recovered in the urine and feces, respectively.

Pregnancy & Breastfeeding use

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to Rexulti during pregnancy.

Lactation studies have not been conducted to assess the presence of brexpiprazole in human milk, the effects of brexpiprazole on the breastfed infant, or the effects of brexpiprazole on milk production. Rexulti is present in rat milk. The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for Rexulti and any potential adverse effects on the breastfed infant from Rexulti or from the underlying maternal condition.


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.

Storage Condition

Store Rexulti tablets at 20°C to 25°C; excursions permitted to 15°C to 30°C

Innovators Monograph

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