OverviewDosageSide EffectsInteractionsHalf-Life

Generic Name: Brexpiprazole

Brands: Rexulti

Class: Atypical antipsychotics

Availability: Prescription

Molecular Formula: C25H27N3O2S

Substance UNII: 2J3YBM1K8C

What is Rexulti?

Rexulti is a dopamine D₂ receptor partial agonist, of the class of drugs called atypical antipsychotics. It is the brand name of the drug brexpiprazole.

What is Rexulti Used For?

Rexulti is used to treat major depressive disorders and schizophrenia. It does so by helping you think more clearly and feel less anxious in your everyday life. It may also help to decrease hallucinations as well as work to improve your mood, sleep, appetite, and energy levels.

How Does Rexulti Work?

The exact mechanism of action of Rexulti is unknown. However, experts believe that a combination of certain actions may make this medication effective. Specifically, experts believe it works through a combination of partial agonist activity at serotonin 5-HT 1A and dopamine D2 receptors as well as antagonist activity at serotonin 5-HT 2A receptors.

Let’s break that down.

In biochemistry, an agonist refers to a type of chemical. Its job is to bind to a receptor to activate it. An antagonist does the reverse: it blocks agonist activity. Therefore, this drug partially helps stimulate serotonin and dopamine activity (at the 5-HT 1A and D2 receptor sites), two neurotransmitters highly associated with mood. Additionally, the antagonist activity at 5-HT 2A receptors is important as research suggests that having more of these receptors can play a role in forming depression. Therefore, helping to inhibit the activity of these receptors may help reduce symptoms of depression.

How Long Does it Take for Rexulti to Work?

Rexulti’s effect may vary from patient to patient as not everyone responds to this medication the same way. Keep your doctor updated on how you are feeling, including any side effects, so that they can better understand what effect the treatment is having on you and adjust it if necessary.

That being said, it can take a week or two for some symptoms to start improving. Although, it may take up to 3 months before you start to feel the full effects of brexpiprazole.

Do Not Use Rexulti If:

There are several situations where this medication may not be the right choice for you. According to the FDA, the following should not use Rexulti:

  • Patients with a known hypersensitivity to brexpiprazole or any of its components
  • Those who have diabetes or high blood sugar (hyperglycemia) or a family history of diabetes or high blood sugar
  • People with high levels of cholesterol, triglycerides, LDL (“bad”) cholesterol, or low levels of HDL (“good”) cholesterol
  • Patients who have or had seizures (convulsions)
  • People with low or high blood pressure (hypotension and hypertension, respectively), or a history of low or high blood pressure
  • Patients who have or had heart problems or a stroke
  • Patients with a low white blood cell count
  • Pregnant individuals or people planning to become pregnant
  • Breastfeeding individuals

In addition, you should tell your doctor if you are taking any other prescription medicines, over-the-counter medicines, vitamins, and herbal supplements as they can interact with this drug. Please note that this list may not be complete, and there may be other situations where Rexulti use is not advisable.

Disclaimer: this article does not constitute or replace medical advice. If you have an emergency or a serious medical question, please contact a medical professional or call 911 immediately. To see our full medical disclaimer, visit our Terms of Use page.

More About Rexulti


Written by

Fact Checked by