Brexpiprazole (Oral)

The antipsychotic medication Brexpiprazole is often prescribed for the treatment of mental illnesses such as depression and schizophrenia, but its use is not without significant risks to older patients.

Overview

Brexpiprazole is a medication prescribed to patients suffering from mental problems resulting from severe depression and schizophrenia. Its antipsychotic properties can prevent patients from having psychotic breaks with reality, delusions, hallucinations, and other problems associated with specific mental illnesses. It is a powerful antipsychotic and is only available with a prescription. In the United States, it is marketed under the brand name Reluxti.

As an antipsychotic medication, Brexpiprazole works by changing chemical actions in the brain to bring them into a closer baseline with normal brain function. It is used as a primary treatment for Schizophrenia but is also prescribed with other medications as a treatment for major depressive disorder in adults. Although it is very effective when used for these purposes, it is not approved for use for older adults suffering from mental conditions associated with dementia.

Conditions Treated

  • Schizophrenia
  • Major Depressive Disorder
  • sychosis

Type of Medicine

  • Antipsychotic

Side Effects

As with any medication, Brexpiprazole can have unintended side effects in some patients. While all of these effects may not necessarily occur, some may be serious enough to require medical attention. If any of the following rarely-seen side effects occur you should inform a physician and seek prompt treatment as needed.

Rarely seen but serious side effects include breaking out in a cold sweat and chills, experiencing general mental confusion, and dizziness or a sense of lightheadedness when getting up or sitting up from a lying position. In some cases, this can result in a loss of consciousness or a fainting spell.

Although their exact incidence is not known, other serious side effects have been recorded when using Brexpiprazole. These can be both mental and physical effects and differ in severity. They include, but are not restricted to, the side effects listed below:

  • Inability to move eyes
  • Changes in behavior
  • Increased blinking or spasms of the eyelid
  • General feeling of tiredness or weakness
  • Lip smacking or puckering
  • Trouble breathing, speaking, or swallowing
  • Suicidal thoughts
  • Uncontrolled movements of the arms and legs
  • Uncontrolled chewing movements
  • Uncontrolled twisting movements of the neck, trunk, arms, or legs
  • Unusual bleeding or bruising
  • Unusual tiredness or weakness
  • Unusual facial expressions
  • Unusually pale skin
  • Difficulty breathing
  • Cough or hoarseness
  • Chest pain
  • Fast heartbeat
  • Black, tarry stools
  • Convulsions
  • High fever
  • Loss of bladder control
  • Painful or difficult urination
  • Lower back or side pain
  • Puffing of the cheeks
  • Rapid or worm-like movements of the tongue
  • Severe muscle stiffness
  • Sores, ulcers, or white spots on the lips or in the mouth
  • Sore throat
  • Increased sweating
  • Sticking out of the tongue

Some side effects associated with Brexpiprazole will not necessarily require medical attention, as they are routine and usually will subside as the body gets used to the medication. If the symptoms persist past an acceptable period of adjustment or if they are severe your doctor may adjust the prescription or take other measures to control the side effects.

Some of the more common routine side effects associated with Brexpiprazole include the following:

  • Acid or sour stomach
  • Heartburn
  • Indigestion
  • Headache
  • Belching
  • Sore throat
  • Stomach discomfort, upset, or pain
  • Weight gain
  • Muscle aches
  • Restlessness
  • Inability to sit still
  • Need to keep moving
  • Sleepiness or unusual drowsiness
  • Stuffy or runny nose

Some of the less commonly seen but still routine side effects include:

  • Insomnia
  • Shakiness in the legs, arms, hands, or feet
  • Blurred vision
  • Dizziness
  • Difficulty with moving
  • Dry mouth
  • Gas
  • Diarrhea
  • Bloated or full feeling
  • Bloody or cloudy urine
  • Difficulty having a bowel movement
  • Frequent urge to urinate
  • Fear or nervousness
  • Joint pain
  • Swollen joints
  • muscle aching or cramping
  • muscle pains or stiffness
  • increased appetite
  • increased sweating

Although this is not a comprehensive list of possible side effects it includes the most notable ones that have been recorded. If any side effect not listed occurs consult with a doctor immediately as this may be an indication of a greater health problem or allergic reaction.

Dosage

As is the case with all prescription-strength medication, Brexpiprazole should be taken only as prescribed and for only the interval that it is intended as a treatment. The dose that is prescribed may vary based on the severity of the condition, the general health of the patient, and other factors that the doctor may take into consideration. The following manufacturer's guidelines for Brexpiprazole are only intended as an average dose and your prescription may vary. Follow all directions from your doctor and prescription label when using this medication. Do not alter the dose without a doctor's permission.

Brexpiprazole is taken as an oral dose in the form of tablets. The dose depends upon the condition that it is prescribed to treat.

For treatment of depression, adults start with either a half milligram or 1-milligram dose once per day. This may increase if a stronger dose is needed and the body builds up a tolerance for the medication. The maximum dose generally is not to exceed 3 mg per day.

If prescribed for children with depression, the dose will be determined by a pediatrician.

Prescription of Brexpiprazole for adults with schizophrenia usually starts with a 1 mg dose once per day for the first four days. This dose may increase to 2 mg on days 5 to 7 and then up to 4 mg on day 8 if the patient can tolerate it. The maximum dose is normally 4 mg daily.

If prescribed to children with schizophrenia the dose will be determined by a pediatrician.

If a dose of Brexpiprazole is missed, it is recommended that any missed dose be taken immediately. However, if the next dose is due the missed dose should be skipped. Double dosing to make up for the missed dose is dangerous and should be avoided. This drug comes with a potential for overdose, and if an overdose is expected 911 should be called immediately.

Major Drug Interactions

Certain medications should not be used together under any circumstances because of unintended interactions. The risk of the interactions can also be small or the condition of the patient may be serious enough that the risk has to be taken. Taking any of the following medications is not recommended and your doctor may need to alter the doses or directions of one or both prescriptions.

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

In addition, avoid taking Brexpiprazole at mealtime. An adverse reaction is known to be associated with eating certain categories of food while taking the medicine. The most notable example is that grapefruit juice has been known to cause a very unfavorable reaction to this medication.

Warnings

When using Brexpiprazole it is very important that progress is checked at regular intervals by the prescribing physician. This is a medication that requires a great deal of discretion when determining the dose and intervals between doses. Both blood and urine tests must be taken to determine if the medication is having unwanted effects on the body. Additionally, regular mental health screening while taking this medication is mandatory as the medicine has been known to increase thoughts of suicide and have other ill effects on a patient's mental state. Any changes in behavior or suicidal ideation should be reported to your healthcare provider immediately. Such changes in behavior could include difficulty sleeping, getting upset easily, rapid fluctuations of energy, reckless behavior, or unusually high intensity of feeling. Your doctor should know if you have a history of bipolar disorder or suicide attempts prior to prescribing this medication.

Check with a doctor immediately if any of the following symptoms occur when using Brexpiprazole as they can be indicative of a greater health problem or reaction to the medication. They may also be symptoms of a serious condition called neuroleptic malignant syndrome (NMS). They include:

  • Difficulty with breathing
  • Rapid heartbeat
  • Convulsions
  • Seizures
  • High fever
  • High or low blood pressure
  • Loss of bladder control
  • Increased sweating
  • Loss of bladder control
  • Severe muscle stiffness
  • Unusually pale skin
  • Fatigue

This medication has been known to cause a movement disorder called tardive dyskinesia. This is more commonly seen in elderly female patients. Check with a doctor immediately if any of the following symptoms surface while using Brexpiprazole:

  • Puffing of the cheeks
  • Lip smacking or puckering
  • Rapid or worm-like movements of the tongue
  • Uncontrolled movements of the arms and legs
  • Uncontrolled chewing movements

Brexpiprazole has been known to increase blood sugar, and increased thirst or urination may be an indication that there is a blood sugar problem. If you have diabetes, carefully monitor blood sugar for any changes the medication may cause. Taking this medication may also lead to significant weight gain and a doctor will need to check your weight on a regular basis while using Brexpiprazole.

Another possible effect of Brexpiprazole is that it can lower the number of white blood cells in the body and lead to an increased risk of infection. If it is possible, people with infections or viruses should be avoided. If you have been in contact with such an individual or if you get a fever, chills, cough, lower back pain or painful urination contact a doctor immediately. If you experience dizziness or lightheadedness while using Brexpiprazole, getting up slowly from a lying position may help. However, if it persists or gets worse with time you should contact your doctor.

Brexpiprazole can affect the body's natural process of cooling down and may reduce how much you sweat. If your body feels like it is overheating or you experience dizziness, weakness, fatigue or confusion you may need to seek immediate medical attention. Upset stomach and vomiting may be another indicator of this side effect. Remove yourself from any heat and drink cool water while contacting your doctor about this effect, but if it is severe, emergency response personnel may need to be contacted as this can be a life-threatening condition.

As this medication is known to cause dizziness and drowsy feelings in patients, it is not recommended that they drive or operate heavy machinery while under the influence of this medicine.

Do not change the dose of this medication or stop taking it without a doctor's permission. Medications and supplements that have not been discussed with your doctor should not be taken. This includes vitamins, non-prescription remedies, herbal supplements and over-the-counter (OTC) medications.

Inform your doctor about any allergies or unusual reactions that you have had to this medicine or any other medications. Your healthcare professional should know about these events in your medical history so that they can make a better decision regarding how to proceed with your treatment.

Pediatric treatment with Brexpiprazole may not be possible as appropriate studies to determine the safety of the medication have not been performed. Until such safety guidelines have been established, your pediatrician may rule this out as a treatment.

This medication should not be used to treat geriatric patients who show any signs of dementia as there is a known increased risk of death.

The presence of certain medical problems may affect the effectiveness of Brexpiprazole. Other conditions can be significantly worsened by use of the drug and it should not be used at all if there is this risk. These interctions between the drug and the conditions can be potentially fatal. Keep your doctor apprised of the general state of your health and any of the following health problems or a family history of them:

  • Blood vessel disease
  • Dehydration
  • Heart attack or stroke
  • Heart disease
  • Heart failure
  • Heart rhythm problems
  • Hypotension
  • Hypovolemia
  • Ischemic heart disease
  • Trouble swallowing
  • Diabetes
  • Hyperglycemia
  • Dyslipidemia
  • Neuroleptic malignant syndrome (NMS)
  • Seizures
  • Kidney disease
  • Liver disease

Storage

Brexpiprazole should be stored in adherence to the guidelines required of most medications, but special care should be taken in the case of this medication because of the ill effects antipsychotics can have on those who are not supposed to take them. They should be separated and securely stored away from other medications. Storage should be at room temperature and away from any sources of heat, moisture, and direct sunlight. The medication should not be frozen. Special care should be taken to keep this medication in a secure container and away from the reach of children. If the medication has expired or is no longer needed it should be disposed of immediately. Seek guidance from your physician if you have any questions regarding how to dispose of this medication.

Summary

Brexpiprazole is the active ingredient in Rexulti and can be effective when used as an antipsychotic treatment for patients struggling with mental illness. However, it comes with serious warnings and may not be a long-term solution for patients suffering from major depression and/or schizophrenia. There is also a serious concern in using it for older adults. For these adults struggling with dementia, studies have shown that taking antipsychotic medication such as Brexpiprazole increases the chance of death. One of the increased risk factors includes the possibility of a mini-stroke during treatments with these antipsychotic medications. For this reason, the FDA has not approved Brexpiprazole as a treatment for any behavioral disorders in adults with dementia.

In addition, there are some concerns when Brexpiprazole is used as a treatment for depression, and it should not be used as a sole treatment for the disorder. A small number of patients who took medications for depression during clinical trials became suicidal. Under normal circumstances, children younger than 18 years old shouldn't take this medication to treat depression but a pediatrician may determine that brexpiprazole is the best available medication for the child. One of the concerns in this area is that there has not been sufficient studies to determine the risk to children when this medication is used and how much the risk is altered by using it in combination with antidepressants.

All patients should be advised when taking Brexpiprazole that mental health can be altered in unexpected ways by the use of antipsychotic medication. This can be true even if antipsychotics have been taken in the past. The risks are higher at the beginning of treatment or anytime the dose is increased or decreased. Behavioral changes that can indicate that there is a problem with the dose include irritability, worsening anxiety, increased depression, panic attacks, aggressive behavior, impulsivity, agitation, and mania.

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Last Reviewed:
December 24, 2017
Last Updated:
April 04, 2018
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