Pronunciation:

brex-PIP-ra-zole

Brand Names:

• Rexulti

Dosage Forms:

• Tablet

Warnings:

Warning: Increased Mortality in Elderly Patients with Dementia-Related Psychosis and Suicidal Thoughts and BehaviorsIncreased Mortality in Elderly Patients with Dementia-Related PsychosisElderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Brexpiprazole is not approved for the treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer’s disease.Suicidal Thoughts and BehaviorsAntidepressants 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 effectiveness of brexpiprazole have not been established in pediatric patients with major depressive disorder .

Classifications:

Therapeutic—

Antipsychotic

Uses of This Medicine:

Brexpiprazole is used to treat mental conditions, including depression and schizophrenia. It is also used to treat agitation that may happen with dementia caused by Alzheimer's disease. Brexpiprazole is an antipsychotic agent. It works in the brain to change how certain chemicals affect patients.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of brexpiprazole for the treatment of schizophrenia in children younger than 13 years of age and for the treatment of depression and agitation in children. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of brexpiprazole in elderly patients. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving brexpiprazole. This medicine should not be used to treat behavioral problems in elderly patients who have dementia.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Metoclopramide

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Aprepitant
• Atazanavir
• Boceprevir
• Bupropion
• Carbamazepine
• Cinacalcet
• Clarithromycin
• Conivaptan
• Diltiazem
• Dronedarone
• Duloxetine
• Erythromycin
• Fluconazole
• Fluoxetine
• Fosaprepitant
• Fosphenytoin
• Imatinib
• Indinavir
• Itraconazole
• Ketoconazole
• Letermovir
• Lopinavir
• Nefazodone
• Nelfinavir
• Paroxetine
• Phenytoin
• Posaconazole
• Quinidine
• Rifampin
• Ritonavir
• Saquinavir
• St John's Wort
• Telaprevir
• Telithromycin
• Terbinafine
• Verapamil
• Voriconazole

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Blood vessel disease or
• Dehydration or
• Heart attack, history of or
• Heart disease or
• Heart failure, history of or
• Heart rhythm problems, history of or
• Hypotension (low blood pressure) or
• Hypovolemia (decrease in blood volume) or
• Ischemic heart disease, history of or
• Stroke, history of or
• Trouble swallowing—Use with caution. May cause side effects to become worse.

• Diabetes, or family history of or
• Hyperglycemia (high blood sugar)—This medicine may raise your blood sugar levels.

• Dyslipidemia (high cholesterol or fats in the blood) or
• Neuroleptic malignant syndrome (NMS), history of or
• Seizures, history of—Use with caution. May make these conditions worse.

• Kidney disease, moderate to severe or
• Liver disease, moderate to severe—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of This Medicine:

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

This medicine should come with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.

You may take this medicine with or without food.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For agitation related with dementia caused by Alzheimer's disease:
    • Adults—At first, 0.5 milligram (mg) once a day on Days 1 to 7. Your doctor may increase your dose to 1 mg once a day on Days 8 to 14, and then to 2 mg once a day on Day 15. However, the dose is usually not more than 3 mg per day.
    • Children—Use and dose must be determined by your doctor.
  • For depression:
    • Adults—At first, 0.5 or 1 milligram (mg) once a day. Your doctor may increase your dose as needed and tolerated. However, the dose is usually not more than 3 mg per day.
    • Children—Use and dose must be determined by your doctor.
  • For schizophrenia
    • Adults—At first, 1 milligram (mg) once a day on Days 1 to 4. Your doctor may increase your dose to 2 mg once a day on Days 5 to 7, and then to 4 mg on Day 8 as tolerated. However, the dose is usually not more than 4 mg per day.
    • Children 13 years of age and older—At first, 0.5 mg once a day on Days 1 to 4. Your doctor may increase your dose to 1 mg once a day on Days 5 to 7, and then to 2 mg on Day 8 as tolerated. However, the dose is usually not more than 4 mg per day.
    • Children younger than 13 years of age—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to allow for changes in your dose and to make sure this medicine is working properly. Blood and urine tests may be needed to check for any unwanted effects.

For some patients, this medicine can increase thoughts of suicide. Tell your doctor right away if you start to feel more depressed and have thoughts about hurting yourself. Report any unusual thoughts or behaviors that trouble you, especially if they are new or are getting worse quickly. Make sure the doctor knows if you have trouble sleeping, get upset easily, have a big increase in energy, or start to act reckless. Also tell the doctor if you have sudden or strong feelings, such as feeling nervous, angry, restless, violent, or scared. Let the doctor know if you or anyone in your family has bipolar disorder (manic-depressive illness) or has tried to commit suicide.

Check with your doctor right away if you have difficulty with breathing, a fast heartbeat, a high fever, high or low blood pressure, increased sweating, loss of bladder control, seizures, severe muscle stiffness, unusually pale skin, or tiredness. These could be symptoms of a serious condition called neuroleptic malignant syndrome (NMS).

This medicine may increase risk of transient ischemic attack or stroke in elderly patients. Tell your doctor right away if you have confusion, double vision, headache, inability to move the arms, legs, or facial muscles, slow speech, or trouble speaking, thinking, or walking while using this medicine.

This medicine may cause tardive dyskinesia (a movement disorder) especially in elderly women. Check with your doctor right away if you have any of the following symptoms while taking this medicine: lip smacking or puckering, puffing of the cheeks, rapid or worm-like movements of the tongue, uncontrolled chewing movements, or uncontrolled movements of the arms and legs.

This medicine may increase the amount of sugar in your blood. Check with your doctor right away if you have increased thirst or increased urination. If you have diabetes, you may notice a change in the results of your urine or blood sugar tests. If you have any questions, check with your doctor.

This medicine may increase your cholesterol and fats in the blood. If this condition occurs, your doctor may give you some medicines that can lower the amount of cholesterol and fats in the blood.

This medicine may increase your weight. Your doctor may need to check your weight on a regular basis while you are using this medicine. Talk to your doctor about ways to prevent weight gain.

Some people who have used this medicine had unusual changes in their behavior. Talk with your doctor right away if you start having unusual urges, such as gambling urges, binge or compulsive eating, compulsive shopping, or sexual urges while using this medicine.

This medicine can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.

Dizziness, lightheadedness, or fainting may occur, especially when you get up from a lying or sitting position. Getting up slowly may help. If this problem continues or gets worse, check with your doctor.

This medicine may make it more difficult for your body to cool down. It might also reduce how much you sweat. Your body could get too hot if you do not sweat enough. If your body gets too hot, you might feel dizzy, weak, tired, or confused. You might have an upset stomach or vomit. Call your doctor if drinking cool water and moving away from the heat does not cool you down.

This medicine may cause drowsiness, dizziness, trouble with thinking, or trouble with controlling movements, which may lead to falls, fractures, or other injuries. Do not drive or do anything else that could be dangerous until you know how this medicine affects you. Stand or sit up slowly if you feel lightheaded or dizzy.

Do not change the dose or stop using this medicine without checking first with your doctor.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines) and herbal (eg, St. John's wort) or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Rare

Chills

cold sweats

confusion

dizziness, faintness, or lightheadedness when getting up from a lying or sitting position

fainting

Incidence not known

Black, tarry stools

changes in behavior

chest pain

cough

difficulty breathing

fast heartbeat

fever with or without chills

general feeling of tiredness or weakness

high fever

hoarseness

inability to move the eyes

increased blinking or spasms of the eyelid

increased sweating

lip smacking or puckering

loss of bladder control

lower back or side pain

painful or difficult urination

puffing of the cheeks

rapid or worm-like movements of the tongue

seizures

severe muscle stiffness

sore throat

sores, ulcers, or white spots on the lips or in the mouth

sticking out of the tongue

swollen glands

thoughts of killing oneself

trouble breathing, speaking, or swallowing

uncontrolled chewing movements

uncontrolled movements of the arms and legs

uncontrolled twisting movements of the neck, trunk, arms, or legs

unusual bleeding or bruising

unusual facial expressions

unusual tiredness or weakness

unusually pale skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Belching

headache

heartburn

inability to sit still

indigestion

muscle aches

need to keep moving

restlessness

sleepiness or unusual drowsiness

stomach discomfort, upset, or pain

stuffy or runny nose

weight gain

Less common

Bloated or full feeling

bloody or cloudy urine

blurred vision

diarrhea

difficulty having a bowel movement

difficulty with moving

dizziness

dry mouth

excess air or gas in the stomach or bowels

fear or nervousness

frequent urge to urinate

increased appetite

increased sweating

joint pain

muscle ache, cramp, pain, or stiffness

passing gas

shakiness in the legs, arms, hands, or feet

swollen joints

trouble sleeping

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

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