Rexulti

Approved Uses

Rexulti is used to manage symptoms of several different mental health and neurological conditions:

• Schizophrenia: It is used to treat schizophrenia in adults and children 13 years of age and older.
• Major Depressive Disorder: It is used as an add-on (adjunctive) treatment for adults with major depressive disorder who are already taking an antidepressant but still have symptoms. It is not used as a standalone treatment for depression.
• Alzheimer's Disease Agitation: It is used to treat agitation, such as physical or verbal aggression and restlessness, in adults with dementia caused by Alzheimer's disease.

This medication belongs to a class of drugs known as atypical antipsychotics. It works by affecting the levels of certain natural chemicals in the brain.

Mechanism of Action

Rexulti belongs to a class of medications known as atypical antipsychotics. It is thought to work by adjusting the activity of two key chemical messengers in the brain: dopamine and serotonin.

These chemicals, called neurotransmitters, help regulate mood, behavior, and thinking. In certain mental health conditions, these chemicals may be out of balance. Rexulti acts as a modulator, which means it can either increase or decrease the activity of these neurotransmitters depending on the environment in the brain.

How It Affects the Brain

• Dopamine and Serotonin Modulation: Rexulti acts as a partial agonist at specific dopamine and serotonin receptors. This allows it to stimulate these receptors when chemical levels are low or block them when levels are too high.
• Serotonin Blockage: It also acts as an antagonist at other serotonin receptors, which means it blocks activity at those specific sites.

The exact mechanism by which Rexulti works in the body is not fully understood. However, by stabilizing the activity of these neurotransmitters, the medication is believed to help improve symptoms related to mood and thought processes.

Common Side Effects

The most common side effects of Rexulti include:

• Weight gain
• Restlessness or an urgent need to move (akathisia)
• Headache
• Drowsiness or fatigue
• Dizziness
• Tremors
• Cold-like symptoms, such as a runny nose or sore throat

Serious Side Effects

Contact a healthcare provider immediately if you experience any of the following serious side effects:

• Uncontrolled muscle movements: Involuntary or repetitive movements of the face, tongue, or other body parts (tardive dyskinesia).
• Neuroleptic Malignant Syndrome (NMS): A rare but serious reaction characterized by high fever, stiff muscles, confusion, and sweating.
• Compulsive behaviors: New or worsening urges that are difficult to control, such as gambling, binge eating, shopping, or sexual urges.
• Metabolic changes: High blood sugar (hyperglycemia), increased cholesterol or triglycerides, and significant weight gain.
• Low white blood cell count: A decrease in white blood cells that can increase the risk of infection.
• Seizures: An increased risk of convulsions.
• Difficulty swallowing: Problems with the muscles used for swallowing.
• Orthostatic hypotension: Dizziness or fainting when standing up too quickly.
• Body temperature regulation: Difficulty cooling down after becoming overheated.

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death or stroke. Rexulti is not approved for the treatment of patients with dementia-related psychosis unless they have agitation associated with Alzheimer’s disease.

Boxed Warnings

Increased Mortality in Elderly Patients with Dementia-Related Psychosis: Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Rexulti is not approved for the treatment of patients with dementia-related psychosis without agitation associated with Alzheimer's disease.

Suicidal Thoughts and Behaviors: Antidepressants may increase the risk of suicidal thoughts and behaviors in children, adolescents, and young adults. Patients of all ages starting therapy should be monitored closely for worsening symptoms or unusual changes in behavior.

Cerebrovascular Adverse Reactions

In clinical trials, elderly patients with dementia-related psychosis experienced an increased incidence of stroke and transient ischemic attacks (mini-strokes), some of which were fatal.

Neuroleptic Malignant Syndrome (NMS)

NMS is a rare but potentially fatal reaction to antipsychotic drugs. Symptoms include high fever, muscle rigidity, delirium, and autonomic instability, such as irregular pulse or blood pressure. If NMS is suspected, the medication is typically discontinued immediately.

Tardive Dyskinesia

This condition involves involuntary, rhythmic movements of the face, tongue, or other body parts. The risk of developing tardive dyskinesia and the potential for it to become permanent increase with long-term use and higher cumulative doses.

Metabolic Changes

Atypical antipsychotics like Rexulti are associated with metabolic risks that can increase cardiovascular danger:

• Hyperglycemia and Diabetes: Patients may experience high blood sugar, which in severe cases can lead to ketoacidosis or coma.
• Dyslipidemia: Changes in cholesterol and triglyceride levels may occur.
• Weight Gain: Significant weight gain is a common side effect and should be monitored.

Impulse Control Disorders

There have been reports of patients experiencing intense, uncontrollable urges to gamble, spend money, binge eat, or engage in other compulsive behaviors while taking this medication. These urges may stop if the dose is reduced or the drug is discontinued.

Additional Precautions

• Low White Blood Cell Count: Patients with a history of low white blood cell counts may require frequent monitoring, as Rexulti can cause further decreases (leukopenia or neutropenia).
• Orthostatic Hypotension: This medication can cause a sudden drop in blood pressure when standing, leading to dizziness or fainting.
• Seizures: Rexulti should be used with caution in individuals with a history of seizures or conditions that lower the seizure threshold.
• Body Temperature Regulation: The drug may impair the body's ability to cool down, increasing the risk of heatstroke during strenuous exercise or exposure to extreme heat.

Pregnancy

Taking antipsychotic medications like Rexulti during the last three months of pregnancy may cause problems in the newborn after delivery. These issues can include withdrawal symptoms, breathing difficulties, feeding problems, tremors, fussiness, or muscle stiffness. However, stopping the medication during pregnancy may lead to a relapse of your condition.

If you are pregnant or planning to become pregnant, talk to your doctor about the risks and benefits of continuing treatment. There is a pregnancy registry that monitors the health of people who take Rexulti during pregnancy and the health of their babies.

Breastfeeding

It is not known if Rexulti passes into breast milk or how it might affect a nursing baby. Because of the potential for side effects, you should consult your healthcare provider to determine if you should breastfeed while using this medication.

Available Forms

Rexulti is supplied in the following form:

• Oral Tablet: This medication is a tablet taken by mouth.

The tablets are film-coated and come in various colors.

FDA Approval and Indications

Rexulti (brexpiprazole) was first approved by the U.S. Food and Drug Administration (FDA) in 2015. It is currently approved for the following indications:

• Major Depressive Disorder: Used as an add-on (adjunctive) treatment for adults who are already taking an antidepressant.
• Schizophrenia: Used to treat schizophrenia in adults and pediatric patients aged 13 years and older.
• Alzheimer's-Related Agitation: Used to treat agitation associated with dementia due to Alzheimer’s disease. In May 2023, it became the first FDA-approved medication for this specific use.

Boxed Warnings

The FDA requires a Boxed Warning for Rexulti, which is the most serious type of warning for prescription medications. These warnings include:

• Increased Mortality in Elderly Patients: Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Rexulti is not approved for the treatment of patients with dementia-related psychosis who do not have agitation associated with Alzheimer's dementia.
• Suicidal Thoughts and Behaviors: Antidepressants may increase the risk of suicidal thoughts and behaviors in children, adolescents, and young adults. Patients of all ages should be monitored closely for worsening symptoms or changes in behavior when starting treatment.

Regulatory Status

Rexulti is available only by prescription. It is classified as an atypical antipsychotic. While it is not a controlled substance, the FDA monitors its safety profile through ongoing post-marketing surveillance to identify any new safety concerns or adverse reactions.

Generic Status

There is currently no generic version of Rexulti (brexpiprazole) available. Brand-name medications typically cost more than generics because they do not have competition from other manufacturers.

Insurance Coverage

Most insurance plans, including Medicare Part D, provide coverage for Rexulti, though it is often listed on a higher cost tier. This means you may have a higher copayment or coinsurance amount. Some insurers require prior authorization, which means your doctor must confirm the medical necessity of the drug before the plan covers it.

Financial Assistance

The manufacturer may offer support to help reduce costs for eligible patients. This can include:

• Savings Cards: These may reduce out-of-pocket costs for people with commercial insurance.
• Patient Assistance: Programs may be available for those without insurance or those who meet specific financial criteria.

It is also helpful to compare prices at different pharmacies or check if your insurance offers a lower rate for mail-order prescriptions.