Rexulti

Rexulti is an atypical antipsychotic used to treat major depressive disorder, schizophrenia, or agitation associated with dementia due to Alzheimer’s disease. It is an oral tablet taken once a day.

Rexulti’s mechanism of action involves adjusting the imbalance of natural chemicals in the brain (also called neurotransmitters), such as dopamine and serotonin. These neurotransmitters help cells to send messages to each other. An imbalance of these natural chemicals is thought to be associated with several psychiatric conditions, including schizophrenia, depression, and agitation associated with dementia due to Alzheimer’s disease (see What is Rexulti used for and how well does it work?).

Rexulti (brexpiprazole) first gained FDA approval on July 10, 2015. Rexulti belongs to the drug class called atypical antipsychotics.

Rexulti is available as a generic under the name brexpiprazole. The brexpiprazole generic is only approved for depression and schizophrenia in adults, whereas the brand Rexulti is also approved for adolescents aged 13 and older with schizophrenia and for dementia-related agitation in Alzheimer's disease.

Rexulti is an atypical antipsychotic used:

• along with antidepressant medicines to treat major depressive disorder (MDD) in adults
• to treat schizophrenia in adults and children aged 13 years and older
• to treat agitation associated with dementia due to Alzheimer’s disease.

Rexulti should not be used as an “as-needed” treatment for agitation that may happen with dementia due to Alzheimer’s disease.

It is not known if Rexulti is safe and effective for the treatment of MDD in children or the treatment of schizophrenia in children under 13 years of age.

Take Rexulti exactly as your healthcare provider tells you to take it. Your healthcare provider may change your dose if needed. Do not change the dose or stop taking Rexulti without first talking to your healthcare provider.

• Take Rexulti 1 time each day.
• Rexulti may be taken with or without food.

Do not take Rexulti if you are allergic to brexpiprazole, Rexulti, or any inactive ingredients in the tablets (see the end of this guide for a list of inactive ingredients).

Before taking Rexulti, tell your healthcare provider about all of your medical conditions, including if you:

• Have or have had heart problems or a stroke
• Have or have had low or high blood pressure
• Have or have had diabetes or high blood sugar or a family history of diabetes or high blood sugar.
• Have or have had high levels of total cholesterol, LDL cholesterol, or triglycerides, or low levels of HDL cholesterol
• Have or have had seizures (convulsions)
• Have or have had kidney or liver problems
• Have or have had a low white blood cell count
• Are pregnant or plan to become pregnant
• Are breastfeeding or plan to breastfeed.

Pregnancy

Rexulti may harm your unborn baby. Taking Rexulti during your third trimester of pregnancy may cause your baby to have abnormal muscle movements or withdrawal symptoms after birth. Talk to your healthcare provider about the risk to your unborn baby if you take Rexulti during pregnancy.

Tell your healthcare provider if you become pregnant or think you are pregnant during treatment with Rexulti.

There is a pregnancy exposure registry for women who are exposed to Rexulti during pregnancy. If you become pregnant during treatment with Rexulti, talk to your healthcare provider about registering with the National Pregnancy Registry for Psychiatric Medications. You can register by calling 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-researchprograms/pregnancyregistry/.

Breastfeeding

It is not known if Rexulti passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby during treatment with Rexulti.

Rexult carries a Boxed Warning for a serious side effect of increased mortality in elderly patients with dementia-related psychosis and suicidal thoughts and behaviors:

• Increased risk of death in elderly people with dementia-related psychosis Medicines like Rexulti can increase the risk of death in elderly people who have lost touch with reality (psychosis) due to confusion and memory loss (dementia). Rexulti is not approved for dementia-related psychosis without agitation that may happen with Alzheimer’s disease.
• Increased risk of suicidal thoughts and actions Rexulti and antidepressant medicines may increase the risk of suicidal thoughts and actions in people 24 years of age and younger, especially within the first few months of treatment or when the dose is changed. Depression and other mental illnesses are the most important causes of suicidal thoughts and actions. Pay close attention to any changes, especially sudden changes in mood, behaviors, thoughts, or feelings, or if you develop suicidal thoughts or actions. This is very important when Rexulti or the antidepressant medicine is started or when the dose is changed. Call your healthcare provider right away to report new or sudden changes in mood, behavior, thoughts, or feelings, or if you develop suicidal thoughts or actions. Keep all follow-up visits with your healthcare provider as scheduled. Call your healthcare provider between visits as needed, especially if you have concerns about symptoms.

Common Side Effects

The most common side effects of Rexulti are:

• Weight gain
• Sleepiness
• Dizziness
• Common cold symptoms
• Restlessness or a feeling like you need to move (akathisia).

The most common side effects of brexpiprazole in children 13 to 17 years of age include difficulty moving or slow movement, tremors (shaking), abnormal eye movements, and muscle stiffness.

Other Serious Side Effects

Other serious side effects of Rexulti include:

• Cerebrovascular problems (these involve the blood vessels of the brain), including stroke, in elderly people with dementia-related psychosis, which can lead to death.
• Neuroleptic malignant syndrome (NMS) is a rare and life-threatening reaction to antipsychotic drugs. Call your healthcare provider or go to the nearest hospital emergency room right away if you have some or all of the following signs and symptoms of NMS: High fever Stiff muscles Confusion Changes in your pulse, blood pressure, heart rate, and breathing Increased sweating.
• Uncontrolled body movements (tardive dyskinesia). Rexulti may cause movements that you cannot control in your face, tongue, or other body parts. Tardive dyskinesia may not go away, even if you stop taking Rexulti. Tardive dyskinesia may also start after you stop taking Rexulti.
• Unusual and uncontrollable (compulsive) urges. Some people taking Rexulti have had strong, unusual urges to gamble and gambling that cannot be controlled (compulsive gambling). Other compulsive urges include sexual urges, shopping, and eating or binge eating. If you or your family members notice that you are having new or unusually strong urges or behaviors, talk to your healthcare provider.
• Low white blood cell count. Your healthcare provider may do blood tests during the first few months of treatment with Rexulti.
• Decreased blood pressure (orthostatic hypotension) and fainting. You may feel dizzy, lightheaded, or pass out (faint) when you rise too quickly from a sitting or lying position.
• Falls. Rexulti may make you sleepy or dizzy, may cause a decrease in your blood pressure when changing position (orthostatic hypotension), and can slow your thinking and motor skills, which may lead to falls that can cause fractures or other injuries.
• Seizures (convulsions). Rexulti may increase your risk of seizures.
• Problems controlling your body temperature so that you feel too warm. See “What should I avoid while taking Rexulti?”
• Difficulty swallowing, which can cause food or liquid to get into your lungs.
• Sleepiness, drowsiness, feeling tired, difficulty thinking, and doing normal activities. See “What should I avoid while taking Rexulti?”

Rexulti may also cause problems with your metabolism, such as:

• High blood sugar (hyperglycemia) and diabetes. Increases in blood sugar can happen in some people who take Rexulti. Extremely high blood sugar can lead to coma or death. Your healthcare provider should check your blood sugar before you start, or soon after you start Rexulti, and then regularly during long-term treatment with Rexulti. Call your healthcare provider if you have any of these symptoms of high blood sugar during treatment with Rexulti: Feel very thirsty Feel very hungry Feel sick to your stomach Need to urinate more than usual Feel weak or tired Feel confused, or your breath smells fruity.
• Increased fat levels (cholesterol and triglycerides) in your blood. Your healthcare provider should check the fat levels in your blood before you start, or soon after you start Rexulti, and then periodically during treatment with Rexulti.
• Weight gain. You and your healthcare provider should check your weight before you start and often during treatment with Rexulti.

Rexulti may harm an unborn baby.

Notes:

These are not all the possible side effects of Rexulti. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA1088.

The dosage of Rexulti varies depending on the condition being treated and the age of the patient. The dosage may need to be adjusted for moderate to severe liver disease, kidney disease, and interacting medications. See the Rexulti prescribing information for more details.

Dose of Rexulti for Major Depressive Disorder (Adults)

• Starting dose: 0.5 to 1 mg orally daily
• Target dose: 2 mg orally daily
• Maximum dose: 3 mg orally daily

Dose of Rexulti for Schizophrenia (Adults)

• Starting dose: 1 mg orally daily
• Target dose: 2 to 4 mg orally daily
• Maximum dose: 4 mg orally daily

Dose of Rexulti for Schizophrenia (Adolescents 13-17)

• Starting dose: 0.5 mg orally daily
• Target dose: 2 to 4 mg orally daily
• Maximum dose: 4 mg orally daily

Dose of Rexulti for Agitation Associated With Dementia

• Starting dose: 0.5 mg orally daily
• Target dose: 2 mg orally daily
• Maximum dose: 3 mg orally daily

Do not drive a car, operate machinery, or do other dangerous activities until you know how Rexulti affects you. Rexulti may make you feel drowsy.

Do not become too hot or dehydrated during treatment with Rexulti.

• Do not exercise too much.
• In hot weather, stay inside in a cool place if possible.
• Stay out of the sun.
• Do not wear too much clothing or heavy clothing.
• Drink plenty of water.

If you take too much Rexulti, call your healthcare provider or Poison Help Line at 1-800-222-1222 or go to the nearest hospital emergency room right away.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Rexulti and other medicines may affect each other causing possible serious side effects. Rexulti may affect the way other medicines work, and other medicines may affect how Rexulti works. Especially tell your healthcare provider if you take:

• Strong CYP2D6 or CYP3A4 inhibitors, such as clarithromycin, diltiazem, erythromycin, itraconazole, ketoconazole, paroxetine, fluoxetine, or bupropion. Administer half the recommended dosage of Rexulti
• Strong/moderate CYP2D6 with strong/moderate CYP3A4 inhibitors: Administer one-quarter of the recommended dosage of Rexulti
• strong/moderate CYP3A4 inhibitors, and you are a known CYP2D6 poor metabolizer: Administer one-quarter of the recommended dosage of Rexulti
• Strong CYP3A4 inducers, such as phenobarbital, phenytoin, rifampicin, St. John's Wort, or glucocorticoids. Double the recommended dosage of Rexulti and further adjust based on the clinical response.

Your healthcare provider can tell you if it is safe to take Rexulti with your other medicines. Do not start or stop any medicines during treatment with Rexulti without first talking to your healthcare provider. Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Store Rexulti tablets at room temperature between 68°F to 77°F (20°C to 25°C). Keep out of the reach of children.

Active ingredient: brexpiprazole

Inactive ingredients: lactose monohydrate, corn starch, microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate, hypromellose, and talc. For color: titanium dioxide, iron oxide, and ferrosoferric oxide.

Rexulti is available as 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg oral tablets.

Rexulti is manufactured through a partnership between two pharmaceutical companies:

• Otsuka Pharmaceutical (Tokyo, Japan) Also makes Abilify, Samsca, and other medications
• Lundbeck (Copenhagen, Denmark) Also makes Lexapro, Vyepti, and other medications

These companies have a long-standing partnership in developing psychiatric medications, with Rexulti being one of their major joint products.