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Brexpiprazole (Rexulti) Uses, Side Effects & Drug Interactions

What is brexpiprazole, and how does it work (mechanism of action)?

Brexpiprazole is an oral atypical
antipsychotic used to treat schizophrenia. Other atypical antipsychotic drugs
include olanzapine (Zyprexa), quetiapine (Seroquel), ziprasidone (Geodon), and
aripiprazole (Abilify).

Atypical antipsychotics differ from typical antipsychotics because they cause
a lesser degree of movement (extrapyramidal) side effects and constipation.

The exact mechanism of action of brexpiprazole is not known, but, like other
anti-psychotics, it is believed that brexpiprazole affects the way the brain
works by interfering with communication among the brain's nerves. Nerves
communicate with each other by making and releasing chemicals called
neurotransmitters. The neurotransmitters travel to other nearby nerves where
they attach to receptors on the nerves. The attachment of the neurotransmitters
either stimulates or inhibits the function of the nearby nerves. Brexpiprazole
blocks several of the receptors on nerves including dopamine type 2, serotonin
type 2, and alpha 2 adrenergic receptors. It is believed that many psychotic
illnesses are caused by abnormal communication among nerves in the brain and
that by altering communication through neurotransmitters, brexpiprazole can
alter the psychotic state. The FDA approved Rexulti in December, 2006.

What brand names are available for brexpiprazole?


Is brexpiprazole available as a generic drug?


Do I need a prescription for brexpiprazole?


What are the side effects of brexpiprazole?

The most common side effects include

Brexpiprazole may increase
blood levels of prolactin.

Less common but serious side effects include:

  • Increased risk of stroke and death in elderly patients with dementia-related
  • Neuroleptic malignant syndrome (NMS). NMS is a rare but serious side effect
    associated with the use of antipsychotics. NMS may result in death and must be
    treated in the hospital. Signs and symptoms of NMS may include

Extrapyramidal side effects (EPS) including:

  • Dystonia: painful spasms of the oral, throat, or neck muscles that may cause
    problems with speech, swallowing, and
    stiff neck.
  • Pseudoparkinsonism: drug induced Parkinson’s symptoms.
  • Tardive dyskinesia (TD). Tardive dyskinesia usually occurs after long-term
    use of antipsychotics and usually presents with abnormal uncontrollable movement
    problems affecting the tongue, lips, jaw, face, and extremities.
  • Metabolic changes including high blood sugar (hyperglycemia),
    diabetes, increase in blood cholesterol, and weight gain.
  • High blood levels of prolactin. Prolactin is a hormone that allows the
    production of breast milk. High levels of prolactin may cause menstrual
    abnormalities, leakage of milk from the breast, development of breasts in males
    and erection problems in men.
  • Brexpiprazole may increase risk of seizures.


Schizophrenia is the most disabling mental illness.
See Answer

What is the dosage for brexpiprazole?

  • Brexpiprazole is administered once daily by mouth with or without food.
  • The starting dose for schizophrenia is 1 mg once daily on days 1 to 4.
    Increase to 2 mg a day on day 5 through Day 7, then to 4 mg on Day 8 based on
    patient response.
  • The maximum dose is 4 mg daily.
  • The starting dose for treating depression is 0.5 mg or 1 mg once daily. The
    dose may be increased in weekly intervals up to a maximum dose of 3 mg daily.

Which drugs or supplements interact with brexpiprazole?

Brexpiprazole can cause low blood pressure especially when standing up from a
sitting down or laying down position (orthostatic hypotension). Therefore, brexpiprazole should be used cautiously with other drugs also associated with
causing orthostatic hypotension.

Brexpiprazole is metabolized or broken down by liver enzymes. Drugs that
induce these enzymes will increase their activity and consequently decrease
blood levels of brexpiprazole. The dose of brexpiprazole should be increased in
people also taking carbamazepine (Tegretol), rifampin (Rifadin), St. John’s Wort,
and other drugs that may decrease its blood levels.

Drugs that block the action of enzymes that breakdown brexpiprazole will
increase blood levels and side effects of brexpiprazole. The dose of
brexpiprazole should be reduced in people who are also taking itraconazole (Sporanox),
clarithromycin (Biaxin), ketoconazole, paroxetine (Paxil), fluoxetine (Prozac),
quinidine, and other drugs that may increase its blood levels. The dose of
brexpiprazole also should be reduced in people whose liver enzymes are less
active than the general population.

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Is brexpiprazole safe to take if I’m pregnant or breastfeeding?

Unborn babies exposed to antipsychotics during the third trimester
of pregnancy are at risk for extrapyramidal and withdrawal symptoms after birth.
Symptoms reported included agitation, hypertonia, hypotonia, tremor, somnolence,
depressed breathing, and feeding disorder. Currently there is no data on the use
of brexpiprazole during pregnancy. Brexpiprazole should only be used during
pregnancy if the potential benefit to the mother outweighs the potential for
side effects in the unborn baby.

A pregnancy exposure registry has been established to monitor the use of
atypical antipsychotics, including brexpiprazole, during pregnancy. All pregnant
women treated with atypical antipsychotics are advised to enroll in this
pregnancy registry and report any side effects.

Brexpiprazole is known to enter human milk but its effects
on the breastfeeding infant or milk production is not yet known.

What else should I know about brexpiprazole?

What preparations of brexpiprazole are available?

Tablets: 0.25, 0.5, 1, 2, 3, and 4 mg

How should I keep brexpiprazole stored?

Brexpiprazole should be stored at room temperature, between 15 C and
30 C (59 F and 86 F).


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