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Below are the general guidelines for dosing Rexulti (brexpiprazole). Note that these dosages may be adjusted on a case-by-case basis for individual patients. Always follow your prescribing physician’s instructions for taking Rexulti.

The following information comes from DailyMed, an FDA label information provider.

What if I miss a dose of Rexulti?

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.

What if I overdose on Rexulti?

There is limited clinical trial experience regarding human overdosage with REXULTI.

Consult a Certified Poison Control Center ( 1-800-222-1222 or www.poison.org) for up-to-date guidance and advice regarding a REXULTI overdosage. Management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers. If there is a medical emergency always call 911.

Charcoal

Oral activated charcoal and sorbitol (50 g/240 mL), administered one hour after ingesting oral brexpiprazole, decreased brexpiprazole C max and area under the curve (AUC) by approximately 5% to 23% and 31% to 39% respectively; however, there is insufficient information available on the therapeutic potential of activated charcoal in treating an overdose with REXULTI.

Hemodialysis

There is no information on the effect of hemodialysis in treating an overdose with REXULTI; hemodialysis is unlikely to be useful because brexpiprazole is highly bound to plasma proteins.

How is Rexulti administered?

Adjunctive Treatment of Major Depressive Disorder

The recommended starting dosage for REXULTI as adjunctive treatment is 0.5 mg or 1 mg once daily, taken orally with or without food.

Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 3 mg. Periodically reassess to determine the continued need and appropriate dosage for treatment.

Treatment of Schizophrenia

The recommended starting dosage for REXULTI is 1 mg once daily on Days 1 to 4, taken orally with or without food.

The recommended target REXULTI dosage is 2 mg to 4 mg once daily. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 4 mg.

Dosage Adjustments for Hepatic Impairment

For patients with moderate to severe hepatic impairment (Child-Pugh score ≥7), the maximum recommended dosage is 2 mg once daily for patients with MDD, and 3 mg once daily for patients with schizophrenia.

Dosage Adjustments for Renal Impairment

For patients with moderate, severe or end-stage renal impairment (creatinine clearance CrCl<60 mL/minute), the maximum recommended dosage is 2 mg once daily for patients with MDD and 3 mg once daily for patients with schizophrenia.

Dosage Modifications for CYP2D6 Poor Metabolizers and for Concomitant Use with CYP Inhibitors or Inducers

Dosage adjustments are recommended in patients who are known cytochrome P450 (CYP) 2D6 poor metabolizers and in patients taking concomitant CYP3A4 inhibitors or CYP2D6 inhibitors or strong CYP3A4 inducers (see TABLE 1). If the coadministered drug is discontinued, adjust the REXULTI dosage to its original level. If the coadministered CYP3A4 inducer is discontinued, reduce the REXULTI dosage to the original level over 1 to 2 weeks.

FactorsAdjusted REXULTI Dosage
CYP2D6 Poor Metabolizers
CYP2D6 poor metabolizersAdminister half of the usual dose.
Known CYP2D6 poor metabolizers taking strong/moderate CYP3A4 inhibitorsAdminister a quarter of the usual dose.
Patients Taking CYP2D6 Inhibitors and/or CYP3A4 Inhibitors
Strong CYP2D6 inhibitors *Administer half of the usual dose.
Strong CYP3A4 inhibitorsAdminister half of the usual dose.
Strong/moderate CYP2D6 inhibitors with strong/moderate CYP3A4 inhibitorsAdminister a quarter of the usual dose.
Patients Taking CYP3A4 Inducers
Strong CYP3A4 inducersDouble usual dose over 1 to 2 weeks.
*In the clinical trials examining the adjunctive use of REXULTI in the treatment of MDD, dosage was not adjusted for strong CYP2D6 inhibitors (e.g., paroxetine, fluoxetine). Thus, CYP considerations are already factored into general dosing recommendations, and REXULTI may be administered without dosage adjustment in patients with MDD.

How is Rexulti supplied?

16.1 How Supplied

REXULTI (brexpiprazole) tablets have markings on one side and are available in the following strengths and package configurations (see TABLE 13):

Tablet StrengthTablet Color/ShapeTablet MarkingsPack SizeNDC Code
0.25 mglight brown
round; shallow convex; bevel-edged
“BRX” and “0.25”Bottle of 3059148-035-13
0.5 mglight orange
round; shallow convex; bevel-edged
“BRX” and “0.5”Bottle of 3059148-036-13
1 mglight yellow
round; shallow convex; bevel-edged
“BRX” and “1”Bottle of 3059148-037-13
2 mglight green
round; shallow convex; bevel-edged
“BRX” and “2”Bottle of 3059148-038-13
3 mglight purple
round; shallow convex; bevel-edged
“BRX” and “3”Bottle of 3059148-039-13
4 mgwhite
round; shallow convex; bevel-edged
“BRX” and “4”Bottle of 3059148-040-13

16.2 Storage

How Supplied

REXULTI (brexpiprazole) tablets have markings on one side and are available in the following strengths and package configurations.

Tablet StrengthTablet Color/ShapeTablet MarkingsPack SizeNDC Code
0.25 mglight brown
round; shallow convex; bevel-edged
“BRX” and “0.25”Bottle of 3059148-035-13
0.5 mglight orange
round; shallow convex; bevel-edged
“BRX” and “0.5”Bottle of 3059148-036-13
1 mglight yellow
round; shallow convex; bevel-edged
“BRX” and “1”Bottle of 3059148-037-13
2 mglight green
round; shallow convex; bevel-edged
“BRX” and “2”Bottle of 3059148-038-13
3 mglight purple
round; shallow convex; bevel-edged
“BRX” and “3”Bottle of 3059148-039-13
4 mgwhite
round; shallow convex; bevel-edged
“BRX” and “4”Bottle of 3059148-040-13

Storage

Store REXULTI tablets at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Disclaimer: this article does not constitute or replace medical advice. If you have an emergency or a serious medical question, please contact a medical professional or call 911 immediately. To see our full medical disclaimer, visit our Terms of Use page.


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