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brexpiprazole

N05AX16

Forms & Strengths

Tablets: 0.25mg, 0.5mg, 1mg, 2mg, 3mg, 4mg
Oral tablets are white to off-white, round, flat, beveled-edged

Adult Dosing

Schizophrenia: 1mg/day, titrate to 2-4mg/day
Major depressive disorder (adjunct): 0.5-1mg/day, titrate to 1-3mg/day
Administration with food, no dose adjustment for renal impairment

Pediatric Dosing

Safety and efficacy not established for patients under 18 years
No recommendation for pediatric use

Indications

Treatment of schizophrenia
Adjunctive treatment of major depressive disorder

Mechanism of Action

Partial agonist at serotonin 1A and dopamine D2 receptors
Antagonist at serotonin 5-HT2A and noradrenaline alpha1B/2C receptors

Contraindications

Known hypersensitivity to brexpiprazole or any component
CYP2D6 poor metabolizers with concomitant use of strong CYP3A4 inhibitors

Adverse Reactions

Headache, anxiety, akathisia, weight gain, nasopharyngitis, somnolence
Increased risk of suicidal thoughts and behaviors in pediatric and young adult patients

Drug Interactions

Strong CYP3A4 inhibitors and CYP2D6 poor metabolizers may increase exposure
Strong CYP3A4 inducers may decrease exposure
Concomitant use with antihypertensive agents may increase the risk of orthostatic hypotension

Curated Content: Needs Vetting Before Put to Clinical Use