Brexpiprazole (Rexulti)

Primer

Brexpiprazole (Trade name: Rexulti) is an antipsychotic in the atypical antipsychotic class commonly used in the treatment of schizophrenia. It is also used as an adjunctive medication in major depressive disorder.

History

Brexpiprazole has features that both overlap and contrast with an older medication, aripiprazole. Brexpiprazole was developed due to concerns about impulse-control problems that developed in the use of aripiprazole (due to dopamine partial agonism). Brexpiprazole was thus designed with dopamine agonism “dialed back” a bit, and it generally has less problems with impulse-control symptoms.

Pharmacokinetics

Pharmacokinetics of Brexpiprazole

Absorption 4 hours to reach peak plasma levels
Distribution
Metabolism
Elimination
Half-life 91 hours (steady state after 10-12 days)

Brexpiprazole: Cytochrome P450 Metabolism

Substrate of (Metabolized by) CYP3A4, CYP3A4
Induces
Inhibits

Pharmacodynamics

Mechanism of Action

  • Serotonin-dopamine activity modulator (D2 partial agonist)

Toxicity

Indications

  • Adult schizophrenia
  • Major depressive disorder, adjunctive therapy with an antidepressant

Dosing

Dosing for Brexpiprazole

Starting 0.25 mg
Titration 0.5 mg q 1-2 weeks
Maximum 3 mg
Taper

Formulations

  • Brexpiprazole comes in

Monitoring

Contraindications

Absolute

Relative

Drug-Drug Interactions

  • Strong CYP3A4 inhibitors (e.g. - ketoconazole) can increase brexpiprazole exposure by 2-fold
  • Strong CYP2D6 inhibitors or poor CYP2D6 metabolizers (e.g. - quinidine) increases brexpiprazole exposure by 2-fold

Side Effects

Adverse Events

Clinical Pearls

Special Populations

Geriatric

Pediatric

Obstetric and Fetal

Medically Ill

Resources