Rexulti (brexpiprazole): Dosage, Side Effects & Pregnancy Safety

What is Rexulti (brexpiprazole), and what is it used for?

Rexulti (brexpiprazole) is an atypical antipsychotic indicated for use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) and for treatment of schizophrenia.

Rexulti is a prescription medicine used to treat:

Major depressive disorder (MDD): Rexulti is used with antidepressant medicines, when your healthcare provider determines that an antidepressant alone is not enough to treat your depression.
Schizophrenia

It is not known if Rexulti is safe and effective in people under 18 years of age.

Do not take Rexulti if you are allergic to brexpiprazole or any of the ingredients in Rexulti.

Before taking Rexulti, tell your healthcare provider if you:

have diabetes or high blood sugar or a family history of diabetes or high blood sugar. Your healthcare provider should check your blood sugar before you start Rexulti and during your treatment.
have high levels of cholesterol, triglycerides, LDL-cholesterol, or low levels of HDL cholesterol
have or had seizures (convulsions)
have or had low or high blood pressure
have or had heart problems or a stroke
have or had a low white blood cell count

What are the side effects of Rexulti (brexpiprazole)?

WARNING

Increased Mortality in Elderly Patients with Dementia-Related Psychosis; and Suicidal Thoughts and Behaviors

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.

Suicidal Thoughts and Behaviors

Antidepressants increased the risk of suicidal thoughts and behaviors in patients aged 24 years and younger in short-term studies. Monitor closely for clinical worsening and for emergence of suicidal thoughts and behaviors. The safety and efficacy of Rexulti have not been established in pediatric patients

Rexulti may cause serious side effects, including:

Stroke in elderly people (cerebrovascular problems) that can lead to death.
Neuroleptic Malignant Syndrome (NMS): Tell your healthcare provider right away if you have some or all of the following symptoms: high fever, stiff muscles, confusion, sweating, changes in pulse, heart rate, and blood pressure. These may be symptoms of a rare and serious condition that can lead to death. Call your healthcare provider right away if you have any of these symptoms.
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 urges. Some people taking REXULTI have had unusual urges, such as gambling, binge eating or eating that you cannot control (compulsive), compulsive shopping and sexual urges. If you or your family members notice that you are having unusual urges or behaviors, talk to your healthcare provider.
Low white blood cell count
Decreased blood pressure (orthostatic hypotension). You may feel lightheaded or faint when you rise too quickly from a sitting or lying position.
Seizures (convulsions)
Problems controlling your body temperature so that you feel too warm.
Difficulty swallowing that can cause food or liquid to get into your lungs.
Problems with your metabolism such as:
- high blood sugar (hyperglycemia): Increases in blood sugar can happen in some people who take Rexulti. Extremely high blood sugar can lead to coma or death. If you have diabetes or risk factors for diabetes (such as being overweight or having a family history of diabetes), your healthcare provider should check your blood sugar before you start taking Rexulti and during your treatment.
  - increased fat levels (cholesterol and triglycerides) in your blood.
  - weight gain: You and your healthcare provider should check your weight regularly.

Call your healthcare provider if you have any of these symptoms of high blood sugar while taking Rexulti:

feel very thirsty
feel sick to your stomach
need to urinate more than usual
feel very hungry
feel weak or tired
feel confused, or your breath smells fruity

The most common side effects of Rexulti include weight gain and an inner sense of restlessness such as feeling like you need to move.

These are not all the possible side effects of Rexulti. For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What is the dosage of Rexulti (brexpiprazole)?

Adjunctive Treatment of Major Depressive Disorder

The recommended starting dosage for Rexulti as adjunctive treatment is 0.5 mg or 1 mg once daily, taken orally with or without food.

Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient's clinical response and tolerability. The maximum recommended daily dosage is 3 mg.

Periodically reassess to determine the continued need and appropriate dosage for treatment.

Treatment of Schizophrenia

The recommended starting dosage for Rexulti is 1 mg once daily on Days 1 to 4, taken orally with or without food.

The recommended target Rexulti dosage is 2 mg to 4 mg once daily. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient's clinical response and tolerability. The maximum recommended daily dosage is 4 mg.

Dosage Adjustments for Hepatic Impairment

For patients with moderate to severe hepatic impairment (Child-Pugh score ≥7), the maximum recommended dosage is 2 mg once daily for patients with MDD, and 3 mg once daily for patients with schizophrenia.

Dosage Adjustments for Renal Impairment

For patients with moderate, severe or end-stage renal impairment (creatinine clearance CLcr<60 mL/minute), the maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia [see Use In Specific Populations, CLINICAL PHARMACOLOGY].

Dosage Modifications for CYP2D6 Poor Metabolizers and for Concomitant Use with CYP Inhibitors or Inducers

Dosage adjustments are recommended in patients who are known cytochrome P450 (CYP) 2D6 poor metabolizers and in patients taking concomitant CYP3A4 inhibitors or CYP2D6 inhibitors or strong CYP3A4 inducers (see Table 1). If the coadministered drug is discontinued, adjust the Rexulti dosage to its original level. If the coadministered CYP3A4 inducer is discontinued, reduce the Rexulti dosage to the original level over 1 to 2 weeks.

Table 1: Dosage Adjustments of REXULTI for CYP2D6 Poor
Metabolizers and for Concomitant Use with CYP3A4 and CYP2D6 Inhibitors and/or
CYP3A4 Inducers

Factors
Adjusted REXULTI Dosage

CYP2D6 Poor Metabolizers

CYP2D6 poor metabolizers
Administer half of the usual dose

Known CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitors
Administer a quarter of the usual dose

Patients Taking CYP2D6 Inhibitors and/or CYP3A4 Inhibitors

Strong CYP2D6 inhibitors*
Administer half of the usual dose

Strong CYP3A4 inhibitors
Administer half of the usual dose

Strong/moderate CYP2D6 inhibitors with strong/moderate CYP3A4 inhibitors
Administer a quarter of the usual dose

Patients Taking CYP3A4 Inducers

Strong CYP3A4 inducers
Double usual dose over 1 to 2 weeks

*In clinical trials examining the adjunctive use of
REXULTI in the treatment of MDD, dosage was not adjusted for strong CYP2D6 inhibitors
(e.g., paroxetine, fluoxetine). Thus, CYP considerations are already factored
into general dosing recommendations and REXULTI may be administered without
dosage adjustment in patients with MDD.

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What drugs interact with Rexulti (brexpiprazole)?

Drugs Having Clinically Important Interactions with Rexulti

Table 10: Clinically Important Drug Interactions with REXULTI

Is Rexulti (brexpiprazole) safe to use while pregnant or breastfeeding?

Before taking REXULTI, tell your healthcare provider if you:

are pregnant or plan to become pregnant. It is not known if REXULTI may harm your unborn baby. Using REXULTI in the last trimester of pregnancy may cause muscle movement problems, medicine withdrawal symptoms, or both of these in your newborn.
- If you become pregnant while taking REXULTI, talk to your healthcare provider about registering with the National Pregnancy Registry for AtypicalAntipsychotics. You can register by calling 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/
are breastfeeding or plan to breastfeed. It is not known if REXULTI passes into your breast milk. You and your healthcare provider should decide if you will take REXULTI or breastfeed.