What is Rexulti: Uses, Warnings & Interactions

Medically reviewed by Gerardo SisonPharm.D.
Licensed Pharmacist
Updated Jan 10, 2024  •  Published Dec 30, 2020
Fact Checked

Rexulti overview

BRAND NAMES:

  • Rexulti

Generic Names:

  • Brexpiprazole

Uses:

  • Treats schizophrenia in adults and children 13 and older

  • Treats major depression in adults in combination with antidepressants

  • Treats agitation linked to dementia from Alzheimer’s disease

Therapeutic Classes:

  • Antipsychotic, atypical

Forms:

  • Tablet

How it’s taken:

  • By mouth

What is Rexulti used for?

Rexulti is an oral medication approved to treat adults and children aged 13 years and older with schizophrenia. It’s also approved as an add-on therapy to help manage major depressive disorder (MDD) in adults when antidepressants alone are not sufficient. In addition, Rexulti may be used to treat agitation caused by Alzheimer's disease. 

Rexulti should not be used in older adults with dementia-related psychosis without agitation caused by Alzheimer’s. Rexulti has not been approved for children under 18 with MDD.

  • Rexulti is an oral medication classified as an atypical antipsychotic. It's mainly prescribed to treat individuals 13 years and older with schizophrenia and as an add-on treatment for adults with major depressive disorder. It has also been approved to manage agitation associated with Alzheimer's dementia.

  • Patients typically take Rexulti once per day as an oral tablet. The correct dosage depends on the condition being treated and the response to the medication. Always follow a healthcare provider's instructions to ensure it’s effective and lower the risk of serious side effects.

  • Those taking Rexulti may encounter side effects, which can include dizziness, restlessness, sleepiness, and common cold symptoms. Some people might also experience changes in metabolism, which may lead to weight gain. Don’t hesitate to report any concerning side effects to a healthcare provider.

  • Before starting treatment with Rexulti, discuss any current medical conditions and other medications being taken, including prescription drugs, over-the-counter medicines, and herbal supplements. Caution may be advised, especially for people with blood pressure problems, diabetes, high cholesterol, seizures, or heart disease. 

  • Keep all follow-up visits with a healthcare provider, as regular monitoring may be needed. Blood pressure, cholesterol, blood sugar, and white blood cell counts may be checked at every visit to ensure the medication is working effectively without causing serious side effects. If something is amiss, a healthcare provider can make the necessary adjustments.

What form(s) does Rexulti come in

  • Tablet

    • 0.25 mg

    • 0.5 mg

    • 1 mg

    • 2 mg

    • 3 mg 

    • 4 mg

What are common Rexulti doses?

  • Major depression: An initial dosage of 0.5 or 1 mg per day gradually increased to a target dosage of 2 mg per day. No more than 3 mg per day.

  • Schizophrenia in adults: An initial dosage of 1 mg per day gradually increased to a target dosage of 2 to 4 mg per day. No more than 4 mg per day. 

  • Schizophrenia in children 13 to 17 years old: An initial dosage of 0.5 mg per day gradually increased to a target dosage of 2 to 4 mg per day. No more than 4 mg per day.

  • Dementia-related agitation due to Alzheimer’s: An initial dosage of 0.5 mg per day gradually increased to a target dosage of 2 mg per day. No more than 3 mg per day.

Common Rexulti prescriptions

  • Rexulti
    0.25mg tablet

  • Rexulti
    0.5mg tablet

  • Rexulti
    1mg tablet

  • Rexulti
    2mg tablet

  • Rexulti
    3mg tablet

  • Rexulti
    4mg tablet

How to take Rexulti

  • Take your medicine as directed. Your dose may need to be changed several times to find what works best for you.

  • Rexulti is typically started at a lower dose and gradually increased over several days. The target dosage is generally based on how the drug is working and whether it’s causing side effects.

  • Rexulti is taken orally, with or without food. Swallow the tablets whole without crushing, chewing, or breaking them.

  • Take the medication at the same time each day to maintain consistency.

  • This medicine should come with a Medication Guide. Ask your pharmacist for a copy if you do not have one.

  • Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light.

What to do if you miss a dose of Rexulti

  • Take a dose as soon as you remember. If it is almost time for your next dose, wait until then and take a regular dose. Do not take extra medicine to make up for a missed dose.

  • If you're unsure about what to do or when to take your next dose, consult your healthcare provider for guidance.

Rexulti contraindications

  • This medicine is not right for everyone. Do not use it if you have had an allergic reaction to brexpiprazole or any of the ingredients in Rexulti.

Rexulti warnings

  • Older adults with dementia-related psychosis may have an increased risk of stroke or heart attacks while taking Rexulti, which may lead to an increased risk of death. 

  • Patients with a history of seizures, difficulty swallowing, or neuroleptic malignant syndrome should use Rexulti with caution. In severe cases, Rexulti may need to be discontinued. 

  • There is a potential risk of metabolic changes. For example, weight gain, high blood sugar, diabetes, and increased cholesterol levels may occur while taking Rexulti.

  • Rexulti may interact with other drugs. Consult a healthcare provider about all medications being taken, including over-the-counter drugs and supplements. 

  • Women who are pregnant or planning to become pregnant, as well as those breastfeeding, should discuss the potential benefits and risks of Rexulti with their healthcare provider.

  • For some children, teenagers, and young adults, this medicine may cause mental or emotional problems, including suicidal thoughts or behaviors. Talk with your doctor right away if you have any thoughts or behavior changes that concern you. Tell your doctor if you or anyone in your family has a history of bipolar disorder or suicide attempts.

  • Tardive dyskinesia is possible while taking Rexulti. It involves involuntary, repetitive body movements. If you experience such symptoms while taking Rexulti, your doctor might consider stopping the medication.

  • If you find yourself experiencing compulsive behaviors, like excessive gambling, while on Rexulti, talk to your healthcare provider. They might suggest lowering the dose or stopping the medication altogether.

  • If you have a low white blood cell count or a history of related conditions, regular blood tests may be recommended while taking Rexulti. If your white blood cell count drops significantly without any other identifiable cause, your doctor might consider stopping the medication.

  • This medicine may make you dizzy or drowsy and may cause trouble with thinking or controlling body movements, which may lead to falls, fractures, or other injuries. Do not drive or do anything else that could be dangerous until you know how this medicine affects you. Stand or sit up slowly if you feel lightheaded or dizzy.

  • You may get overheated or dehydrated more easily while you are using this medicine. Use caution when you exercise or if you are outside in hot or humid weather. Drink plenty of water to stay hydrated.

  • Some people have a genetic variation that makes them process certain drugs more slowly, which is known as being a poor metabolizer. If you're a known CYP2D6 poor metabolizer, you may be at risk of potential side effects and need to take half the usual recommended dose of Rexulti.

  • Do not stop using this medicine suddenly. Your doctor will need to slowly decrease your dose before you stop it completely.

  • Your doctor will do lab tests at regular visits to check on the effects of this medicine. Keep all appointments.

  • Keep all medicine out of the reach of children. Never share your medicine with anyone.

Rexulti interactions

  • Strong CYP3A4 and CYP2D6 Inhibitors: These drugs slow down the metabolism of Rexulti. If you’re taking strong CYP3A4 or CYP2D6 inhibitors, your healthcare provider may reduce the Rexulti dose to half. If you’re taking both types of medications, the dosage may need to be reduced to a quarter of the usual recommendation. 

    • Strong CYP3A4 inhibitors include ketoconazole, clarithromycin, itraconazole, ritonavir, indinavir, cobicistat, and grapefruit juice. Strong CYP2D6 inhibitors include fluoxetine, paroxetine, bupropion, and quinidine.

  • Strong CYP3A4 Inducers: These drugs speed up the metabolism of Rexulti. If you start taking a strong CYP3A4 inducer, you may have to gradually double the Rexulti dose over one to two weeks. 

  • Strong CYP3A4 inducers include phenytoin, rifampin, carbamazepine, oxcarbazepine, phenobarbital, and St. John's wort. 

Rexulti side effects

Similar to other drugs, Rexulti may cause side effects that vary in severity. While some people may experience minimal or no side effects, others might experience more serious reactions.

Serious side effects

  • Increased risk of death in older adults with dementia-related psychosis 

  • Increased risk of suicidal thoughts and behaviors

  • Neuroleptic malignant syndrome, a serious neurological disorder 

  • Tardive dyskinesia, a condition involving uncontrollable movements 

  • Seizures 

  • Changes in metabolism, leading to high blood sugar or diabetes 

  • Altered cholesterol and triglyceride levels 

  • Low white blood cell count

  • Unusual or compulsive behaviors, such as gambling or binge eating

  • Decreased blood pressure and fainting

  • Trouble controlling body temperature

  • Problems swallowing

  • Allergic reactions, with symptoms like itching or hives, swelling in the face or throat, chest tightness, and trouble breathing

Less Serious Side Effects

  • Sleepiness

  • Dizziness

  • Common cold symptoms, such as runny nose or sore throat

  • Restlessness

  • Anxiety or nervousness

  • Irritability 

  • Weight gain

Watch for any side effects while taking Rexulti, especially when starting the medication or adjusting the dosage. If side effects are persistent or worsen, contact a healthcare provider. In cases of serious side effects, you may need to seek immediate medical attention.

Sources:

Medically reviewed by Gerardo SisonPharm.D.
Licensed Pharmacist

Gerardo Sison, Pharm.D., graduated from the University of Florida. He has worked in both community and hospital settings, providing drug information and medication therapy management services. As a medical writer, he hopes to educate and empower patients to better manage their health and navigate their treatment plans.

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