Resources Medication Resource Centre Rexulti (brexiprazole)

Rexulti (brexiprazole)

Rexulti (brexiprazole)

Brand name: Rexulti®

Active ingredient name: Brexpiprazole

Type of drug: Atypical antipsychotic

Available in Canada from: Otsuka and Lundbeck Alliance

Form: Oral tablets

Generic: No

Listed on Ontario formulary: No*

*What this means is that for most individuals with schizophrenia, Rexulti will not be a first-line medication choice as it is not covered on the provincial Formulary. Physicians will assess each patient on a case-by-case basis.

What is Rexulti used for?

Rexulti is used to treat the symptoms of schizophrenia in adults. It can be used alone or in combination with other therapies for schizophrenia. Rexulti is sometimes used to treat other conditions, such as major depressive disorder. Talk to your doctor to understand why you are taking Rexulti.


How should I take Rexulti?
Rexulti can be taken with or without food. It is usually taken once daily, preferably at a similar time each day. 

How much Rexulti should I take?

Rexulti is available in 0.25, 0.5, 1, 2, 3, and 4 mg tablets in Canada. 

Adults: The dose range for Rexulti is 2-4 mg daily. The usual dose for most adults is 4 mg once per day. Your doctor may prescribe doses that are higher than 4 mg based on your individual situation. Talk to your doctor about your dose.


What are the common side effects seen with Rexulti? 

The most common side effects of Rexulti include:

  • Weight gain
  • Increased triglycerides
  • Abnormal movements (extrapyramidal side effects)
  • Restlessness (akathisia)
  • Headache
  • Drowsiness

{c    What are rare, but potentially serious side effects seen with Rexulti?

  • Decreased white blood cell count (agranulocytosis)
  • Cerebrovascular event (stroke)
  • Anaphylactic reaction (severe allergy)
  • Diabetic ketoacidosis (DKA)
  • Neuroleptic Malignant Syndrome (NMS)



Elderly individuals with dementia-related psychosis treated with antipsychotic medication are at an increased risk of death compared to individuals not receiving antipsychotics. Most deaths appear to be either cardiovascular or infectious. Rexulti is not approved for the treatment of dementia-related psychosis. Some individuals with dementia may, however, be treated with this medication. Discuss the potential risks and benefits of this medication with your doctor for this indication.


What medications interact with Rexulti?
Tell all your doctors, pharmacists, and dentist that you are taking Rexulti. You should also tell your doctor or pharmacist if you are taking any other medications, including those obtained without a prescription and herbal and vitamin products. When the levels of a medication are increased or decreased in your bloodstream, this can affect the medication’s efficacy and safety.

The following drugs might increase the levels of Rexulti in your bloodstream:

  • Ketoconazole (antifungal)
  • Quinidine
  • Bupropion

The following drug might decrease the levels of Rexulti in your bloodstream:

  • Rifampin
  • Carbamazepine
  • St. John’s wort

 The following are other types of medications that may interact with Rexulti:


  • Certain medications for allergies (e.g., Benadryl [diphenhydramine])
  • Certain medications for sleep (e.g., lorazepam, zopiclone)
  • Certain medications for pain (e.g., fentanyl)
  • Antiparkinson agents (e.g., dopamine agonists)