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Generic name: brexipiprazole (breks PIP ray zole)
Brand name: Rexulti®
All FDA warnings are at the end of this fact sheet. Please consult them before taking this medication.
Brexpiprazole is a medication that works in the brain to treat schizophrenia. It is also known as a second-generation antipsychotic (SGA) or atypical antipsychotic. Brexpiprazole rebalances dopamine and serotonin to improve thinking, mood, and behavior.
Symptoms of schizophrenia include:
Brexpiprazole may help some or all of these symptoms.
Brexpiprazole is also FDA approved for the following indications:
This medication sheet will focus primarily on schizophrenia. You can find more information about depression here.
This medication may be prescribed for other uses; ask your health care provider for more information.
Schizophrenia requires long-term treatment. Do not stop taking brexpiprazole, even when you feel better.
With input from you, your health care provider will assess how long you will need to take the medication.
Missing doses of brexpiprazole may increase your risk for a relapse in your symptoms.
Do not stop taking brexpiprazole or change your dose without talking with your health care provider first.
For brexpiprazole to work properly, it should be taken every day as ordered by your health care provider.
If you are planning on becoming pregnant, notify your health care provider to best manage your medications. People living with schizophrenia or certain other mental illness who wish to become pregnant face important decisions. This is a complex decision since untreated schizophrenia or other mental illness has risks to the fetus, as well as the mother. It is important to discuss the risks and benefits of treatment with your doctor and caregivers.
Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (extrapyramidal symptoms [EPS]) and/or withdrawal symptoms in newborns following delivery that may need to be monitored. These may resolve within hours/days without treatment or require hospitalization for monitoring/treatment.
Caution is advised with breastfeeding since brexpiprazole has been shown to pass into animal milk. No studies have been conducted to assess for brexpiprazole in breastfed infants or how this medication may affect milk production.
Brexpiprazole may help control your symptoms but will not cure your condition.
It may take two to three months before you feel the full effect of brexpiprazole.
Brexpiprazole tablets are usually taken once a day with or without food.
Typically, patients begin at a low dose of medication and the dose is increased slowly over several weeks. Only your health care provider can determine the correct dose for you.
The dose usually ranges from 0.5 mg to 4 mg. Only your health care provider can determine the correct dose for you.
Use a calendar, pillbox, alarm clock, or cell phone alert to help you remember to take your medication. You may also ask a family member or a friend to remind you or check in with you to be sure you are taking your medication.
It is important to take your medication everyday as directed by your health care provider. Do not miss or skip a dose.
If you miss a dose of brexpiprazole, take it as soon as you remember, unless it is closer to the time of your next dose. Discuss this with your health care provider. Do not double your next dose or take more than what is prescribed.
Avoid drinking alcohol or using illegal drugs while you are taking brexpiprazole. They may decrease the benefits (e.g., worsen your symptoms) and increase adverse effects (e.g., sedation) of the medication.
If an overdose occurs call your doctor or 911. You may need urgent medical care. You may also contact the poison control center at 1-800-222-1222.
A specific treatment to reverse the effects of brexpiprazole does not exist. Management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms.
This is not a complete list. Talk with your health care provider for more information.
Common side effects
Restlessness, weight gain, cholesterol abnormalities
Rare/serious side effects
Brexpiprazole may increase the blood levels of a hormone called prolactin. Side effects of increased prolactin levels include females losing their period, production of breast milk and males losing their sex drive or possibly experiencing erectile problems. Long term (months or years) of elevated prolactin can lead to osteoporosis, or increased risk of bone fractures.
Some people may develop muscle-related side effects while taking brexpiprazole. The technical terms for these are “extrapyramidal symptoms” (EPS) and “tardive dyskinesia” (TD). Symptoms of EPS include restlessness, tremor, and stiffness. TD symptoms include slow or jerky movements that one cannot control, often starting in the mouth with tongue rolling or chewing movements.
Antipsychotics can also affect temperature regulation especially if you exercise a lot or are in an area that is very hot. While taking brexpiprazole, it is especially important to try to drink water to avoid dehydration.
Second generation antipsychotics (SGAs) increase the risk of weight gain, high blood sugar, and high cholesterol. This is also known as metabolic syndrome. Your health care provider may ask you for a blood sample to check your cholesterol, blood sugar, and hemoglobin A1c (a measure of blood sugar over time) while you take this medication.
All antipsychotics have been associated with the risk of sudden cardiac death due to an arrhythmia (irregular heart beat). To minimize this risk, antipsychotic medications should be used in the smallest effective dose when the benefits outweigh the risks. Your doctor may order an EKG to monitor for irregular heartbeat.
Neuroleptic malignant syndrome is a rare, life-threatening adverse effect of antipsychotics which occurs in <1% of patients. Symptoms include confusion, fever, extreme muscle stiffness, and sweating. If any of these symptoms occur, contact your health care provider immediately.
All antipsychotics can cause sedation, dizziness, or orthostatic hypotension (a drop in blood pressure when standing up from sitting or lying down). These side effects may lead to falls which could cause bone fractures or other injuries. This risk is higher for people with conditions or other medications that could worsen these effects. If falls or any of these symptoms occur, contact your health care provider.
Tardive dyskinesia (TD) is a side effect that develops with prolonged use of antipsychotics. The risk is greater in people with diabetes, older adults, especially older women, longer use or higher doses but may also occur after short term use with low doses. Medications such as brexpiprazole have been shown to have a lower risk of TD compared to older antipsychotics, such as Haldol® (haloperidol). If you develop symptoms of TD, such as grimacing, sucking, and smacking of lips, or other movements that you cannot control, contact your health care provider immediately. All patients taking either first- or second-generation antipsychotics should have an Abnormal Involuntary Movement Scale (AIMS) completed regularly by their health care provider to monitor for TD.
Second generation antipsychotics (SGAs) increase the risk of diabetes, weight gain, high cholesterol, and high triglycerides. (See “Serious Side Effects” section for monitoring recommendations).
Tell your health care provider about all medications that you take, have recently taken or plan to take including prescription and nonprescription medications, vitamins, herbal products, and nutritional supplements. This medication may affect the way other medications work, and other medications may affect how this medication works.
Brexpiprazole may block the effects of agents used to treat Parkinson’s disease such as levodopa/carbidopa (Sinemet®), bromocriptine, pramipexole (Mirapex®), ropinirole (Requip®), and others.
The following medications may increase the levels and effects of brexpiprazole:
It is especially important to tell your doctor how you feel things are going during the first few weeks after you start taking brexpiprazole. It will probably take several weeks to see big enough changes in your symptoms to decide if brexpiprazole is the right medication for you.
Antipsychotic treatment is generally needed lifelong for persons with schizophrenia. Your doctor can best discuss the duration of treatment you need based on your symptoms and illness.
Increased Mortality in Elderly Patients with Dementia Related Psychosis
Last Reviewed: January 2024
Important Disclosure: This information is being provided as a community outreach effort of the American Association of Psychiatric Pharmacists. This information is for educational and informational purposes only and is not medical advice. This information contains a summary of important points and is not an exhaustive review of information about the medication. Always seek the advice of a physician or other qualified medical professional with any questions you may have regarding medications or medical conditions. Never delay seeking professional medical advice or disregard medical professional advice as a result of any information provided herein. The American Association of Psychiatric Pharmacists disclaims any and all liability alleged as a result of the information provided herein.
©2023 The American Association of Psychiatric Pharmacists (AAPP) and the National Alliance on Mental Illness (NAMI). AAPP and NAMI make this document available under the Creative Commons Attribution-NoDerivatives 4.0 International License. Last Updated: January 2016.