Rexulti treats the symptoms of schizophrenia. It can also be given in combination with an antidepressant to treat depression in adults.

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Pharmacist Anyssa S. Garza, PharmD overviews the uses and common side effects of Rexulti.
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Rexulti Overview

Reviewed: July 13, 2015

Rexulti is a prescription medication used to treat the symptoms of major depressive disorder (MDD) and schizophrenia in adults. It belongs to a group of drugs called atypical antipsychotics. These medications work by altering the activity of certain natural substances in the brain.

This medication comes in tablet form and is usually taken once a day, with or without food.

Common side effects of Rexulti include weight gain, headache, and restlessness.

Rexulti can also cause drowsiness. Do not drive or operate heavy machinery until you know how Rexulti affects you.

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Rexulti Cautionary Labels


Uses of Rexulti

Rexulti is a prescription medicine 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

It is not known if Rexulti is safe and effective in people under 18 years of age. 



Rexulti Drug Class

Rexulti is part of the drug class:

Side Effects of Rexulti

Serious side effects have been reported with Rexulti.  See the “Rexulti Precautions” section.

Common side effects include the following:

  • weight gain
  • headache
  • restlessness
  • nausea
  • dizziness
  • drowsiness
  • anxiety
  • insomnia

This is not a complete list of Rexulti side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away. Call your doctor for medical advice about side effects. 

You may report side effects to the FDA at 1-800-FDA-1088.

Rexulti Interactions

Tell your doctor about all the medicines you take including prescription and nonprescription medications, vitamins, and herbal supplements. Especially tell your doctor if you take:

  • antidepressants (mood elevators)
  • antifungals such as itraconazole (Sporanox) and ketoconazole (Nizoral)
  • antihistamines
  • bupropion (Wellbutrin)
  • carbamazepine (Tegretol)
  • clarithromycin (Biaxin)
  • fluoxetine (Prozac, Sarafem)
  • HIV protease inhibitors such as atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), and saquinavir (Invirase)
  • ipratropium (Atrovent)
  • medications for anxiety, high blood pressure, irritable bowel syndrome, mental illness, motion sickness, Parkinson's disease, seizures, ulcers, or urinary problems
  • nefazodone (Serzone)
  • paroxetine (Paxil, Pexeva)
  • quinidine (Cardioquine, Quinact, Duraquin)
  • rifampin (Rifadin, Rimactane)
  • sedatives
  • sleeping pills
  • telithromycin (Ketek)
  • tranquilizers

This is not a complete list of Rexulti drug interactions. Ask your doctor or pharmacist for more information.

Rexulti Precautions

Serious side effects have been reported with Rexulti including the following:

  • Stroke in elderly people (cerebrovascular problems) that can lead to death.
  • Neuroleptic Malignant Syndrome (NMS). Tell your healthcare provider right away if you have some or all of the following symptoms of this life-threatening nervous system disorder:
    • high fever
    • stiff muscles
    • confusion
    • sweating
    • changes in pulse, heart rate, and blood pressure
  • High blood sugar. Increases in blood sugar can happen in some people who take Rexulti.
  • Call your healthcare provider if you have any of these symptoms of high blood sugar while taking Rexulti:
    • feel very thirsty
    • need to urinate more than usual
    • feel very hungry
    • feel weak or tired
    • feel sick to your stomach
    • feel confused, or your breath smells fruity
  • Increase in weight. Weight gain has been reported in patients taking medicines like Rexulti, so you and your healthcare provider should check your weight regularly. 
  • Difficulty swallowing. This may lead to aspiration and choking.
  • Tardive dyskinesia. Call your healthcare provider about any movements you cannot control in your face, tongue, or other body parts. These may be signs of a serious condition. Tardive dyskinesia may not go away, even if you stop taking Rexulti. Tardive dyskinesia may also start after you stop taking Rexulti.
  • Orthostatic hypotension (decreased blood pressure). Lightheadedness or fainting can occur when rising too quickly from a sitting or lying position.
  • Low white blood cell count
  • Seizures (convulsions)
  • Problems controlling your body temperature so that you feel too warm. Avoid getting over-heated or dehydrated. Do not over-exercise. In hot weather, stay inside in a cool place if possible. Stay out of the sun. Do not wear too much or heavy clothing. Drink plenty of water while taking Rexulti.
  • Increased risk of death in elderly people with dementia related psychosis. Medicines like Rexulti can raise the risk of death in elderly who have lost touch with reality (psychosis) due to confusion and memory loss (dementia). Rexulti is not approved for the treatment of patients with dementia-related psychosis.
  • Risk of suicidal thoughts or actions. Antidepressant medicines, depression and other serious mental illnesses, may cause suicidal thoughts or actions. Rexulti is not approved for the treatment of people younger than 18 years of age.
    • Antidepressant medicines may increase suicidal thoughts or actions in some children, teenagers, or young adults within the first few months of treatment.
    • Depression and other serious mental illnesses are the most important causes of suicidal thoughts or actions. Some people may have a particularly high risk of having suicidal thoughts or actions. These include people who have (or have a family history of) bipolar illness (also called manicdepressive illness) or suicidal thoughts or actions.

Pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings. This is very important when an antidepressant medicine is started or when the dose is changed. 

Call the healthcare provider right away to report new or sudden changes in mood, behavior, thoughts, or feelings. „ 

Keep all follow-up visits with the healthcare provider as scheduled. 

  • Call the healthcare provider between visits as needed, especially if you have concerns about symptoms. Call a healthcare provider right away if you or your family member has any of the following symptoms, especially if they are new, worse, or worry you:
    • thoughts about suicide or dying
    • attempts to commit suicide
    • new or worsening depression
    • new or worsening anxiety
    • feeling very agitated or restless
    • acting on dangerous impulses
    • panic attacks
    • trouble sleeping (insomnia)
    • new or worsening irritability
    • acting aggressive, being angry, or violent
    • an extreme increase in activity or talking (mania)
    • other unusual changes in behavior or mood

​Do not drive, operate heavy machinery, or do other dangerous activities until you know how Rexulti affects you. Rexulti may make you drowsy. Do not drink alcohol while taking Rexulti.

Do not take Rexulti if you are allergic to brexpiprazole or any of the ingredients in Rexulti.

Rexulti Food Interactions

Grapefruit and grapefruit juice may interact with Rexulti and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Inform MD

Before taking Rexulti, tell your healthcare provider if you: 

  • have diabetes or high blood sugar or a family history of diabetes or high blood sugar. Your healthcare provider should check your blood sugar before you start Rexulti and during your treatment. 
  • have high levels of cholesterol, triglycerides, LDL-cholesterol, or low levels of HDL cholesterol 
  • have or had seizures (convulsions)
  • have or had abnormal thyroid tests
  • have or had low or high blood pressure
  • have or had heart problems or a stroke
  • have or had low white blood cell count 
  • are pregnant or plan to become pregnant. It is not known if Rexulti may harm your unborn baby.
  • are breastfeeding or plan to breastfeed. It is not known if Rexulti passes into your breast milk. You and your healthcare provider should decide if you will take Rexulti or breastfeed. 

Tell your healthcare provider about all the medicines you take or recently have taken, including prescription medicines, non-prescription medicines, vitamins and herbal supplements. 


Rexulti and Pregnancy

Tell your doctor if you are pregnant or plan to become pregnant.

In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

If you become pregnant while taking Rexulti, talk to your healthcare provider about registering with the National Pregnancy Registry for Atypical Antipsychotics.

You can register by calling 1-866-961-2388 or visit http://womensmentalhealth. org/clinical-and-research programs/pregnancyregistry/ 



Rexulti and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. 

It is not known if Rexulti crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using Rexulti.

Rexulti Usage

Take Rexulti exactly as prescribed.

Rexulti comes in tablet form and is taken once a day, with or without food.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of Rexulti at the same time.

Rexulti Dosage

Take this medication exactly as prescribed by your doctor.  Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight
  • your height
  • your age
  • your gender

The starting dose of Rexulti for Major Depressive Disorder is 0.5mg per day or 1mg per day. The recommended dose of Rexulti for Major Depressive Disorder (MDD) is 2mg per day, with a maximum of 3mg per day.

The starting dose of Rexulti for Schizophrenia is 1mg per day. The recommended dose range of Rexulti for schizophrenia is 2 to 4mg per day, with a maximum of 4mg per day.

Rexulti Overdose

If you take too much Rexulti, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

Other Requirements

  • Store Rexulti at room temperature
  • Keep this and all medicines out of the reach of children

Rexulti FDA Warning


Increased Mortality in Elderly Patients with Dementia-Related Psychosis 

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.

Suicidal Thoughts and Behaviors 

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.