REXULTI (Brexpiprazole)

What is this medication?

Brexpiprazole, Rexulti
Second Generation (Atypical) Antipsychotic

Brexpiprazole, Rexulti is officially indicated as adjunct therapy for major depressive disorder and for the treatment of schizophrenia. It is also sometimes prescribed off-label for agitation, aggression, and psychosis associated with severe dementia. (may be used for other conditions not listed)

“ALERT: US Boxed Warning

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. Brexpiprazole is not approved for the treatment of patients with dementia-related psychosis.

Suicidal thoughts and behaviors:
Antidepressants increased the risk of suicidal thoughts and behavior 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 brexpiprazole have not been established in pediatric patients.”

How does this medication work?

Brexpiprazole exhibits partial agonist activity for 5-HT1A and D2 receptors and antagonist activity for 5-HT2A receptors.

How should I take this medication?

Major depressive disorder (adjunct to antidepressants): Oral: Initial: 0.5 mg or 1 mg once daily; titrate at weekly intervals based on response and tolerability to 1 mg once daily (if initial dose is 0.5 mg), followed by 2 mg once daily; maximum daily dose: 3 mg.

Schizophrenia: Oral: Initial: 1 mg once daily for 4 days, titrate based on response and tolerability to 2 mg once daily for 3 days, followed by 4 mg on day 8; target dose: 2 to 4 mg/day; maximum daily dose: 4 mg.

How to Take: Follow instructions provided by physician/pharmacy label, take consistently at same times each day unless otherwise directed, store at room temperature

You Need to Avoid: Operating heavy machinery or driving at least until you know how the medication affects you.  Do not stop this medication suddenly, make sure your physician is aware and can create a tapering schedule so you can come off slowly and prevent any withdrawal symptoms.  This medication has many drug interactions so ask your pharmacist before starting any over the counter medications or supplements.

What should I watch for while using this medication?

Before starting Brexpiprazole, Rexulti make sure your physician is aware of any allergies or medications you currently take, if you have cardiovascular disease, dementia, a history of seizures or are pregnant or breastfeeding.  Brexpiprazole use has rarely been associated with severe side effects such as: blood dyscrasias, cerebrovascular effects, CNS depression, dyslipidemia, esophageal dysmotility, increased risk of falls, impulse control disorders, neuroleptic malignant syndrome, orthostatic hypotension, suicidal ideation, weight gain, and temperature regulation issues.   

This medication also requires regular bloodwork and follow up with your physician to monitor for adverse reactions

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible.  However, if it is almost time for your next dose, take only that scheduled dose.  Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times.  Store at room temperature, 59 to 86° F (15 to 30° C).  Protect from light.  Keep the container tightly closed.  Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication?

>10%:

Endocrine & metabolic: Increased serum triglycerides (<500 mg/dL: 8% to 13%; ≥500 mg/dL: <1%), weight gain (3% to 11%)

Nervous system: Akathisia (4% to 14%; dose related)

Note- this is not a complete list of side effects, only common ones.