Rexulti (Brexpiprazole): Uses, Side Effects, Warning, & More

What Is Rexulti (Brexpiprazole)?

Rexulti, or brexpiprazole, belongs to the class of atypical antipsychotic medications that act on neurotransmitters in the brain. Approved by the FDA, it’s prescribed for treating schizophrenia and major depressive disorder (MDD) in adults.

FDA approval signifies that rigorous testing has demonstrated the drug’s safety and efficacy, assuring healthcare professionals and patients that it meets established standards for treating specific medical conditions. Rexulti’s main physiological effects involve modulating neurotransmitter activity to help manage symptoms associated with these mental health disorders.¹

Is Rexulti a Mood Stabilizer?

No, Rexulti is not classified as a traditional mood stabilizer. However, it does exhibit mood-regulating effects. As an atypical antipsychotic, Rexulti mainly influences dopamine and serotonin receptors in the brain. It helps regulate certain neurotransmitters in the brain, which could contribute to its therapeutic effects in mood-related disorders.²

Rexulti Vs. Abilify

Rexulti and Abilify (aripiprazole) belong to the same class of medications, atypical antipsychotics, and share similarities in their mechanism of action. Both drugs act on dopamine and serotonin receptors in the brain, contributing to their efficacy in treating schizophrenia and major depressive disorder (MDD). However, they differ in their chemical structures and specific receptor affinities.

Rexulti is approved for schizophrenia and MDD, while Abilify has a broader range of uses. Factors such as side effects, dosing, and patient preferences may influence the choice between the two. Consulting a healthcare professional is crucial for determining the most appropriate option based on the patient’s medical history and treatment goals.

Rexulti Vs. Latuda

Rexulti and Latuda (lurasidone) are both atypical antipsychotic medications used in the treatment of schizophrenia and depression symptoms. While they share the same therapeutic class, they have notable differences. Rexulti primarily acts on dopamine and serotonin receptors, whereas Latuda has a higher affinity for dopamine receptors.^{1, 3}

Rexulti is used for schizophrenia and major depressive disorder, while Latuda is used for schizophrenia and depressive episodes related to bipolar depression. Rexulti is taken once daily, while Latuda may be taken with food once daily or in the evening. Consult your healthcare provider to determine the most suitable treatment based on your circumstances.³

How Does Rexulti Work?

Rexulti works by affecting the levels of certain chemicals in the brain, specifically dopamine and serotonin, which are known to impact mood and behavior. By balancing these chemicals, Rexulti may help improve symptoms associated with mental health conditions such as schizophrenia, bipolar disorder, and major depressive disorder.¹

How Does Rexulti Make You Feel?

Rexulti helps stabilize mood and alleviate extreme highs or lows. People may experience emotional balance and improved well-being or notice a reduction in specific symptoms. It’s important to communicate changes in how one feels to their healthcare provider for optimal results.²

What Is Rexulti Used to Treat?

Rexulti is FDA-approved to treat schizophrenia and major depressive disorder (MDD) in adults. FDA approval signifies that the medication has undergone rigorous testing to establish its safety and efficacy for specific medical conditions. It means the regulatory agency has reviewed compelling evidence supporting the drug’s benefits and risks.²

However, healthcare providers may sometimes prescribe medications off-label, meaning for uses not officially approved by the FDA. An off-label use could occur when a prescriber believes, based on their professional judgment, that the medication may provide benefits in a situation beyond its approved uses. In the case of Rexulti, using it off-label would involve prescribing it for conditions other than schizophrenia or MDD.

Common Side Effects of Rexulti

Rexulti may cause common side effects that some individuals may experience during treatment. While not exhaustive, the following highlights key information from the medication’s prescribing information. It’s essential to note that not everyone will encounter these effects, and individual responses may vary. If any of these symptoms persist or worsen, seeking medical advice is recommended.

Common side effects of Rexulti include:²

• Weight gain
• Drowsiness
• Headache
• Increased appetite
• Akathisia (overwhelming sense of restlessness, need to move)
• Fatigue
• Sedation (drowsiness)

*All medications, including Rexulti, can cause side effects which can be mild or serious. This is not a comprehensive list of all possible side effects. You should talk with your doctor about any questions you have and understand the potential side effects and benefits of any medication.

Serious Side Effects of Rexulti

Rexulti may lead to serious side effects that necessitate immediate medical attention. Individuals experiencing any of these effects should seek prompt medical care. The severity and impact of these side effects can vary, affecting different areas of the body. It’s crucial to be vigilant and promptly report any concerning symptoms to a healthcare professional.

Serious side effects of Rexulti include:²

• Neuroleptic malignant syndrome (NMS)
• Tardive dyskinesia
• Metabolic changes (hyperglycemia, dyslipidemia)
• Orthostatic hypotension (sudden drop in blood pressure after standing up)
• Seizures
• Suicidal thoughts
• Allergic reactions
• Hyperprolactinemia (abnormally high levels of the hormone prolactin)
• Disorders affecting blood cells
• Dysphagia (difficulty swallowing)

*All medications, including Rexulti, can cause side effects which can be mild or serious. This is not a comprehensive list of all possible side effects. You should talk with your doctor about any questions you have and to understand the potential side effects and benefits of any medication.

Rexulti Warnings & Precautions

Rexulti comes with several warnings and precautions. It may increase the risk of suicidal thoughts, especially in young adults. Inform your healthcare provider about existing medical conditions, including liver problems.

Seek immediate medical attention if unusual or severe reactions occur, such as changes in mood, allergic responses, or difficulties in swallowing. Regular communication with healthcare professionals is crucial for a comprehensive understanding of potential risks and the prompt management of any adverse effects.

Avoid taking Rexulti if you:¹

• Older patients with dementia-related psychosis: Older patients with dementia-related psychosis are advised to avoid taking Rexulti due to an increased risk of death associated with antipsychotic medications in this population.
• Tardive dyskinesia: It is advised to avoid taking Rexulti if you have tardive dyskinesia, a condition characterized by involuntary, repetitive movements, as antipsychotic medications like Rexulti may worsen these symptoms.
• Metabolic changes: Rexulti may contribute to weight gain, increased blood sugar, and lipid changes, potentially exacerbating existing metabolic conditions.
• Leukopenia, neutropenia, andagranulocytosis: Your doctor may perform blood tests if you have a low white blood cell count (WBC) or a history of leukopenia or neutropenia. Based on these results, they will consider whether it is Rexulti is an appropriate medication for you.
• Orthostatic hypotension and syncope: Your doctor will monitor your heart rate and blood pressure and alert you of any risks if you have known heart conditions.
• Seizures: If you have a history of seizures or a condition that lowers the seizure threshold, your doctor may be cautious about prescribing this medication to you.

Rexulti Dosages for FDA-Approved Treatment

The dosage of Rexulti is highly individualized, varying based on factors such as age, the specific condition being treated, and the overall health of the individual. For adults with schizophrenia, the typical starting dosage is 1 mg daily, which may be increased to a target range of 2 to 4 mg daily. In major depressive disorder (MDD), the starting dose is often 0.5 mg daily, with a target range of 1 to 3 mg daily. Rexulti is approved for use in adults aged 18 to 64 years for both schizophrenia and MDD.¹

Lower starting doses are recommended for elderly patients due to age-related factors. Healthcare providers must evaluate individual needs, potential medication interactions, and overall health to determine the appropriate dosage. With off-label uses, practitioners must consider the unique characteristics of each patient. Regular communication between patient and healthcare provider is essential to monitor dosage, effects, and side effect for optimal outcomes.

Rexulti Forms & Strengths

Rexulti is not classified as extended-release, delayed-release, or sustained-release; it is meant for daily administration. Determining the most suitable form and strength is based on individual factors such as specific mental health conditions, age, and overall health. Prescribers carefully consider the severity of symptoms, the patient’s response to treatment, and potential side effects when choosing the dosage.²

Dosages may vary to accommodate these factors, and adjustments are made gradually to minimize side effects and enhance therapeutic benefits. While some individuals may experience symptom improvement within weeks, the full therapeutic effect may take longer, emphasizing the need for ongoing communication between the patient and healthcare provider to tailor the treatment plan for optimal outcomes.

Rexulti is available in the following forms and strengths:¹

• 0.25 milligrams (mg) oral tablet
• 0.5 milligrams (mg) oral tablet
• 1 milligram (mg) oral tablet
• 2 milligrams (mg) oral tablet
• 3 milligrams (mg) oral tablet
• 4 milligrams (mg) oral tablet

How Should I Take Rexulti?

Rexulti is typically taken once daily, with or without food, as directed by a healthcare provider. The specific dosage and timing depend on the individual’s condition and response to treatment.¹

What Happens If I Miss a Dose of Rexulti?

If you miss a dose of Rexulti, take it as soon as you remember. However, if it’s close to the time of the next scheduled dose, skip the missed one and resume the regular dosing schedule. If uncertainties arise or if several doses are missed, consulting with a healthcare provider is advisable to determine the best course of action based on individual circumstances and prevent potential disruptions in the treatment plan.²

Can You Overdose on Rexulti?

There is limited clinical trial experience regarding human overdosage with Rexulti. In case of a Rexulti overdose, the recommended management involves concentrating on supportive therapy, maintaining an adequate airway, oxygenation, and ventilation, along with the management of symptoms. Close medical supervision and monitoring are advised until the patient recovers.¹

What Should You Do If You Take Too Much Rexulti?

If you have taken too much Rexulti, contact your local poison control center or emergency room immediately. Don’t wait for symptoms to worsen. Provide medication details, the amount taken, and ingestion time. Let medical professionals handle the situation. Keep in touch with your healthcare provider to discuss concerns and avoid overdosing on Rexulti.

What to Avoid When Taking Rexulti

Inform your healthcare provider about all medications, including over-the-counter drugs and herbal supplements, before taking Rexulti. Combining Rexulti with certain medications, substances, or herbs can pose potential risks. Regular consultations with healthcare professionals can guide appropriate adjustments to the treatment plan and minimize the risk of adverse effects.

Ten (10) substances you should avoid while taking Rexulti include:¹

• Alcohol: Combining alcohol with Rexulti can cause drowsiness and impairment.
• Strong CYP3A4 inhibitors (e.g., ketoconazole): These medications may interfere with Rexulti metabolism, potentially affecting its effectiveness or increasing the risk of side effects.
• Strong CYP3A4 inducers (e.g., rifampin): These drugs can impact Rexulti metabolism, potentially reducing its efficacy.
• Other antipsychotics: Combining Rexulti with other antipsychotic medications may increase the risk of side effects and adverse reactions.
• Benzodiazepines: Use with benzodiazepines can cause sedation.
• Serotonergic medications (e.g., SSRIs, SNRIs): Combining Rexulti with certain antidepressants can increase the risk of serotonin syndrome, a rare condition. This can occur when taking selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and other antidepressant medications.
• St. John’s wort: St. John’s wort is an herbal supplement. Taking it with Rexulti may affect CYP3A4 levels, affecting Rexulti’s metabolism and effectiveness.
• Anti-seizure medications: Some anti-seizure drugs may interact with Rexulti, influencing its effectiveness and risk of side effects.
• Blood pressure medications: Certain medications for blood pressure control may have interactions with Rexulti, necessitating careful monitoring.
• Dextromethorphan: Found in cough medications, dextromethorphan may increase the risk of serotonin syndrome when combined with Rexulti.

How to Get a Prescription for Rexulti

Rexulti is a prescription-only medication, meaning it can only be obtained through a prescription from a qualified healthcare professional. Typically, psychiatrists, primary care physicians, or limited types of mental health specialists can prescribe Rexulti. Before prescribing, a comprehensive evaluation is essential to determine the appropriateness of Rexulti for an individual.

This evaluation may include a thorough medical history, assessment of current symptoms, and consideration of other medications or conditions. The healthcare provider will weigh the potential benefits of Rexulti against any potential risks or interactions. This personalized evaluation ensures that Rexulti is prescribed based on the specific needs and conditions of the individual, optimizing the likelihood of successful treatment while minimizing potential risks.

Questions to Ask Your Healthcare Provider About Rexulti

If you’re dealing with depression, schizophrenia, or bipolar disorder, you might want to know about Rexulti. You should ask your doctor, psychiatrist, or therapist about how Rexulti works, potential side effects, and whether it’s a good fit for your specific needs. If you need to change prescribers, online psychiatry services can be a great option for finding a new doctor and getting the medication you need.

Questions to ask your care team about Rexulti include:

• Why is Rexulti being recommended for me?
• What are the potential benefits of Rexulti for my specific condition?
• What are the common side effects associated with Rexulti?
• Are there any potential interactions between Rexulti and other medications I am taking?
• How long does it typically take to see improvement in symptoms with Rexulti?
• Are there any specific lifestyle changes I should consider while taking Rexulti?
• What should I do if I miss a dose of Rexulti?
• How often will I need to have follow-up appointments to monitor my progress?
• Are there any particular symptoms I should report immediately?
• If I experience side effects, are there alternative treatments or adjustments to consider?