Reviewed on 7/10/2023

What Is Brexpiprazole and How Does It Work?

Brexpiprazole is a prescription medicine used for the treatment of schizophrenia, depression and agitation associated with Alzheimer's dementia.

  • Brexpiprazole is available under the following different brand names: Rexulti

What Are Side Effects Associated with Using Brexpiprazole?

Common side effects of Brexpiprazole include:

  • weight gain
  • agitation
  • distress
  • restlessness
  • constipation
  • fatigue
  • runny or stuffy nose
  • increased appetite
  • headache
  • drowsiness
  • tremor
  • dizziness
  • anxiety

Serious side effects of Brexpiprazole include:

  • trouble walking
  • difficulty speaking (and being understood)
  • sudden weakness on one side of the body
  • vision problems
  • slurred speech
  • very high fever
  • irregular pulse
  • fast heartbeats
  • increased breathing
  • stiff (rigid) muscles
  • high or low blood pressure
  • altered mental status
  • involuntary muscle movements (grimacing or eye blinking)
  • high blood sugar
  • increased thirst
  • increased urination
  • fatigue
  • weight loss
  • blurred vision
  • too high or low blood lipid levels
  • other compulsive behaviors
  • abnormal blood tests (low white blood cell counts)
  • lightheadedness
  • confusion
  • nausea
  • fainting
  • seizures

Rare side effects of Brexpiprazole include:

  • none 

Seek medical care or call 911 at once if you have the following serious side effects:

  • Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
  • Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
  • Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.
This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

What Are Dosages of Brexpiprazole?

Adult and pediatric dosage


  • 0.25 mg
  • 0.5 mg
  • 1 mg
  • 2 mg
  • 3 mg
  • 4 mg


Adult dosage

  • Days 1-4: 1 mg orally once daily
  • Day 5-7: Titrate to 2 mg once daily
  • Day 8: Titrate to 4 mg/day based on the patient’s clinical response and tolerability
  • Target dose: 2-4 mg orally once daily; not to exceed 4 mg/day
  • Periodically reassess to determine the continued need and appropriate dose

Pediatric dosage

  • Children below 13 years: Safety and efficacy not established
  • Children aged 13 to 17 years: 
    • Days 1-4: 0.5 mg orally once daily
    • Days 5-7: Titrate to 1 mg orally once daily
    • Day 8: 2 mg orally once daily based on clinical response and tolerability
    • Target dose: 2-4 mg orally once daily; weekly 1-mg dose increments can be made, not to exceed 4 mg/day
    • Periodically reassess to determine continued need and appropriate dose


Adult dosage

  • 0.5 mg or 1 mg orally once daily initially
  • Titrate according to clinical response and tolerability in weekly intervals to 1 mg/day and then up to 2 mg/day; not to exceed 3 mg/day
  • Periodically reassess to determine the continued need and appropriate dose

Agitation Associated With Alzheimer Dementia

Adult dosage

  • Days 1-7: 0.5 mg orally every day
  • Days 8-14: Increase to 1 mg orally every day
  • Days 15: Increase to 2 mg orally every day
  • Target dose: 2 mg orally every day

Dosage Considerations – Should be Given as Follows: 

  • See “Dosages”

What Other Drugs Interact with Brexpiprazole?

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first

  • Brexpiprazole has severe interactions with the following drug:
    • amisulpride
  • Brexpiprazole has serious interactions with at least 35 other drugs.
  • Brexpiprazole has moderate interactions with at least 271 other drugs
  • Brexpiprazole has minor interactions with the following drugs:
    • acetazolamide
    • anastrozole
    • cyclophosphamide
    • larotrectinib

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions, concerns.

What Are Warnings and Precautions for Brexpiprazole?


  • Hypersensitivity to brexpiprazole or any of its components; reactions have included rash, facial swelling, urticaria, and angioedema

Effects of drug abuse

  • None

Short-Term Effects

  • See “What Are Side Effects Associated with Using Brexpiprazole?”

Long-Term Effects

  • See “What Are Side Effects Associated with Using Brexpiprazole?”


  • Increased mortality in elderly patients with dementia-related psychosis; in placebo-controlled trials, the majority of patients treated with atypical antipsychotic drugs had a 1.6-1.7 times higher risk of death than placebo
  • Suicidal thoughts and behaviors reported in patients below 24 years who are taking antidepressant drugs; unknown whether the risk of suicidal thoughts and behaviors in children, adolescents, and young adults extends to longer-term use (i.e., more than 4 months)
  • May cause leukopenia, neutropenia, and agranulocytosis; monitor and discontinue if severe neutropenia (ANC less than 1000/mm3); in patients with a pre-existing low WBC or ANC or a history of drug-induced leukopenia or neutropenia, perform a complete blood cell count (CBC) frequently during the first few months of therapy
  • Orthostatic hypotension or syncope may occur; the risk is greatest during initial dose titration and when increasing the dose; monitor orthostatic vital signs in patients who are vulnerable to hypotension, (e.g., elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medication, patients with known cardiovascular disease, patients with cerebrovascular disease)
  • May cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; perform complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy
  • Caution with a history of seizures or with conditions/drugs that potentially lower the seizure threshold
  • May disrupt the body’s ability to reduce core body temperature; use with caution in patients who experience these conditions
  • Esophageal dysmotility and aspiration pneumonia reported; use cautiously in patients at risk for aspiration
  • Sedation and hypersomnia reported that may cause impaired judgment, thinking, or motor skills; exercise caution if operating hazardous machinery, including motor vehicles, until certain therapy does not adversely affect them
  • Postmarketing case reports suggest that patients can experience intense urges, particularly for gambling, and inability to control urges; consider dose reduction or stopping the medication if a patient develops such urges
  • Neuroleptic malignant syndrome (NMS)
    • Potentially fatal NMS has been associated with antipsychotic drugs administration
    • Clinical manifestations are hyperpyrexia, muscle rigidity, altered mental status, and evidence of autonomic instability
    • If NMS is suspected, immediately discontinue therapy, and provide intensive symptomatic treatment and monitoring
  • Tardive dyskinesia
    • Tardive dyskinesia was reported in patients treated with antipsychotic drugs
    • Incidence highest in elderly persons, especially elderly women
    • Increased duration of treatment and the cumulative dose may increase the risk of tardive dyskinesia and the potential for it to be irreversible
    • Use the lowest dose and shortest duration of treatment needed to produce a satisfactory clinical response; periodically reassess the need for continued treatment
    • If signs and symptoms of tardive dyskinesia appear, consider discontinuing therapy
    • Reserve chronic antipsychotic treatment for the following patients
      • Who suffer from chronic illness and is responsive to antipsychotics
      • For whom alternative therapies are not available or appropriate
  • Metabolic changes
    • Atypical antipsychotic drugs have been associated with metabolic changes that include hyperglycemia/diabetes mellitus (including extreme cases associated with ketoacidosis or hyperosmolar coma or death), dyslipidemia, and body weight gain
    • Assess fasting plasma glucose, fasting lipid profile, and weight before or soon after initiation of antipsychotic medication, and monitor periodically during long-term treatment
  • Drug interaction overview
    • Strong CYP3A4 inhibitors
    • Reduce brexpiprazole dose
    • Strong CYP3A4 inhibitors may increase the exposure of brexpiprazole
    • Strong CYP2D6 inhibitors
    • Reduce brexpiprazole dose
    • Strong CY2D6 inhibitors may increase the exposure of brexpiprazole
    • Both CYP3A4 and CYP2D6 inhibitors
    • Reduce brexpiprazole dose
    • Drugs that are strong or moderate CYP3A4 and CYP2D6 inhibitors may increase the exposure of brexpiprazole
    • Strong CYP3A4 inducers
    • Increase brexpiprazole dose
    • Strong CYP3A4 inducers may decrease the exposure of brexpiprazole

Pregnancy and Lactation

  • Adequate and well-controlled studies have not been conducted with brexpiprazole in pregnant females inform drug-associated risks
  • Pregnancy exposure registry
    • Monitors pregnancy outcomes in women exposed to brexpiprazole during pregnancy; for more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit
    • Clinical considerations
    • Neonates whose mothers are exposed to antipsychotic drugs, like brexpiprazole, during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms (eg, agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder)
  • Lactation
    • Unknown if distributed in human breast milk
    • Present in rat milk
    • The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant from the drug or the underlying maternal condition 
Medscape. Brexpiprazole.

Health Solutions From Our Sponsors