Rexulti

Name: Rexulti

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of aripiprazole in elderly patients. This medicine should not be used to treat behavioral problems in elderly patients who have dementia.

Rexulti Dosage

Take this medication exactly as prescribed by your doctor.  Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight
  • your height
  • your age
  • your gender

The starting dose of Rexulti for Major Depressive Disorder is 0.5mg per day or 1mg per day. The recommended dose of Rexulti for Major Depressive Disorder (MDD) is 2mg per day, with a maximum of 3mg per day.

The starting dose of Rexulti for Schizophrenia is 1mg per day. The recommended dose range of Rexulti for schizophrenia is 2 to 4mg per day, with a maximum of 4mg per day.

Rexulti Overdose

If you take too much Rexulti, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

Rexulti FDA Warning

WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS; and SUICIDAL THOUGHTS AND BEHAVIORS 

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.

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.

 

What is the most important information I should know about brexpiprazole?

Brexpiprazole is not approved for use in psychotic conditions related to dementia.

Some young people have thoughts about suicide when first taking an antidepressant. Stay alert to changes in your mood or symptoms. Report any new or worsening symptoms to your doctor.

Brexpiprazole is not approved for use by anyone younger than 18 years old.

How should I take brexpiprazole?

Follow all directions on your prescription label. Your doctor may occasionally change your dose. Do not use this medicine in larger or smaller amounts or for longer than recommended.

You may take brexpiprazole with or without food.

Drink plenty of fluids, especially in hot weather and during exercise. You may get dehydrated easily while taking brexpiprazole.

You should not stop using brexpiprazole suddenly. Stopping suddenly may make your condition worse.

Brexpiprazole may cause you to have high blood sugar (hyperglycemia). If you are diabetic, check your blood sugar levels on a regular basis while you are taking brexpiprazole.

Store at room temperature away from moisture and heat.

Stability

Storage

Oral

Tablets

20–25°C (may be exposed to 15–30°C).1

Actions

  • Exact mechanism of action in major depressive disorder and schizophrenia unknown; efficacy may be mediated through a combination of partial agonist activity at dopamine type 2 (D2) and serotonin type 1 (5-hydroxytryptamine [5-HT1A]) receptors and antagonist activity at serotonin type 2 (5-HT2A) receptors.1

  • Demonstrates partial agonist activity at D2 and D3 receptors and 5-HT1A receptors and antagonist activity at 5-HT2A, 5-HT2B, and 5-HT7 receptors and α1A-, α1B-, α1D-, and α2C-adrenergic receptors.1 6 7 8 9

  • Compared with aripiprazole, brexpiprazole appears to have lower intrinsic activity at D2 receptors and higher activity at 5-HT1A and 5-HT1B receptors and demonstrates stronger antagonism at 5-HT2A receptors.2 4 7 8 9

  • Exhibits moderate affinity for histamine (H1) receptors, which are associated with sedation, and very low affinity for muscarinic (M1) receptors.1 4 9

How is this medicine (Rexulti) best taken?

Use this medicine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take with or without food.
  • To gain the most benefit, do not miss doses.
  • Keep taking Rexulti as you have been told by your doctor or other health care provider, even if you feel well.
  • Drink lots of noncaffeine liquids unless told to drink less liquid by your doctor.

What do I do if I miss a dose?

  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.
  • If you are not sure what to do if you miss a dose, call your doctor.

What are some other side effects of Rexulti?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Dizziness.
  • Feeling sleepy.
  • Feeling tired or weak.
  • Restlessness.
  • Headache.
  • Weight gain.
  • Nose and throat irritation.
  • Shakiness.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

How do I store and/or throw out Rexulti?

  • Store at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.

Drug Abuse and Dependence

Controlled Substance

Rexulti is not a controlled substance.

Abuse

Animals given access to Rexulti did not self-administer the drug, suggesting that Rexulti does not have rewarding properties.

Dependence

Humans and animals that received chronic Rexulti administration did not demonstrate any withdrawal signs upon drug discontinuation. This suggests that Rexulti does not produce physical dependence.

PRINCIPAL DISPLAY PANEL- 4 mg Tablet Carton Label

NDC 59148-040-13

30 Tablets
4 mg

Rexulti™
brexpiprazole
tablets

Rx only

Keep out of the reach of children

DISPENSE THE ACCOMPANYING MEDICATION GUIDE TO EACH PATIENT

Manufactured by Otsuka Pharmaceutical Co., Ltd., Tokyo, 101-8535 Japan

Distributed and marketed by Otsuka America Pharmaceutical, Inc., Rockville, MD 20850 USA

Marketed by Lundbeck, Deerfield, IL 60015 USA

Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-035
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 0.25 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
FERRIC OXIDE RED  
FERRIC OXIDE YELLOW  
FERROSOFERRIC OXIDE  
Product Characteristics
Color BROWN (light brown) Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;0;25
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-035-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-036
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 0.5 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
FERRIC OXIDE RED  
FERRIC OXIDE YELLOW  
Product Characteristics
Color ORANGE (light orange) Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;0;5
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-036-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-037
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 1 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
FERRIC OXIDE YELLOW  
Product Characteristics
Color YELLOW (light yellow) Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;1
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-037-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-038
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 2 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
FERRIC OXIDE YELLOW  
FERROSOFERRIC OXIDE  
Product Characteristics
Color GREEN (light green) Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;2
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-038-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-039
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 3 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
FERRIC OXIDE RED  
FERROSOFERRIC OXIDE  
Product Characteristics
Color PURPLE (light purple) Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;3
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-039-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Rexulti 
brexpiprazole tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59148-040
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
brexpiprazole (brexpiprazole) brexpiprazole 4 mg
Inactive Ingredients
Ingredient Name Strength
lactose monohydrate  
starch, corn  
MICROCRYSTALLINE CELLULOSE  
HYDROXYPROPYL CELLULOSE (1200000 MW)  
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIED  
magnesium stearate  
HYPROMELLOSE, UNSPECIFIED  
talc  
TITANIUM DIOXIDE  
Product Characteristics
Color WHITE Score no score
Shape ROUND (shallow convex; bevel-edged) Size 6mm
Flavor Imprint Code BRX;and;4
Contains     
Packaging
# Item Code Package Description
1 NDC:59148-040-13 30 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA205422 07/10/2015
Labeler - Otsuka America Pharmaceutical, Inc. (008314390)
Revised: 02/2017   Otsuka America Pharmaceutical, Inc.

Before taking this medicine

Rexulti is not approved for use in psychotic conditions related to dementia. Rexulti may increase the risk of death in older adults with dementia-related conditions.

You should not use Rexulti if you are allergic to brexpiprazole.

To make sure Rexulti is safe for you, tell your doctor if you have:

  • liver disease;

  • kidney disease;

  • high cholesterol or triglycerides (a type of fat in the blood);

  • heart disease, high or low blood pressure;

  • a history of low white blood cell (WBC) counts;

  • a history of heart attack or stroke;

  • a history of seizures, head injury or brain tumor;

  • a personal or family history of diabetes or high blood sugar; or

  • trouble swallowing.

Some young people have thoughts about suicide when first taking an antidepressant. Your doctor should check your progress at regular visits. Your family or other caregivers should also be alert to changes in your mood or symptoms.

It is not known whether Rexulti will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

If you are pregnant, your name may be listed on a pregnancy registry. This is to track the outcome of the pregnancy and to evaluate any effects of Rexulti on the baby.

It is not known whether brexpiprazole passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Rexulti is not approved for use by anyone younger than 18 years old.

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