Rexulti (brexiprazole)

Rexulti (brexiprazole)

Brand name: Rexulti®.
Active ingredient name: Brexpiprazole.
Type of medication: Atypical antipsychotic.
Available in Canada from: Otsuka and Lundbeck Alliance.
Form: Oral tablets.
Generic: No.
Listed on Ontario formulary: Yes.
OHIP+ coverage: Yes.

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. 
  • Rexulti is available in 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg tablets in Canada. 
  • Adults: The dose range for Rexulti is 2 mg - 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 most 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

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 medications might increase the levels of Rexulti in your bloodstream:
  • Ketoconazole (anti-fungal)
  • Quinidine
  • Bupropion
The following medications might decrease the levels of Rexulti in your bloodstream:
  • Rifampin
  • Carbamazepine
  • St. John’s Wort

 The following types of medications 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)
  • Anti-Parkinson agents (e.g., dopamine agonists)