Comparative Pharmacology
Head-to-head clinical analysis: BREXPIPRAZOLE versus REXULTI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREXPIPRAZOLE versus REXULTI.
BREXPIPRAZOLE vs REXULTI
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Partial agonist at dopamine D2 and serotonin 5-HT1A receptors; antagonist at serotonin 5-HT2A receptors.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A and α1B/α2C adrenergic receptors.
Oral: 1 mg once daily initially, titrate to 2 mg once daily after 3-7 days, then to 4 mg once daily based on response; maximum 4 mg once daily.
2 mg orally once daily initially; increase to 4 mg once daily no sooner than week 2; target dose 4 mg once daily; range 2-4 mg once daily.
None Documented
None Documented
91 hours (range 70–120 hours) for the parent drug; repeated dosing leads to steady state in ~3–4 weeks. The active metabolite DM-3411 has a half-life of ~86 hours.
Clinical Note
moderateBrexpiprazole + Haloperidol
"The serum concentration of Haloperidol can be increased when it is combined with Brexpiprazole."
Clinical Note
moderateBrexpiprazole + Methylphenidate
"The risk or severity of adverse effects can be increased when Brexpiprazole is combined with Methylphenidate."
Clinical Note
moderateBrexpiprazole + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Brexpiprazole."
Clinical Note
moderateTerminal elimination half-life is approximately 19–23 days for brexpiprazole and its major metabolite DM-3411, requiring up to 2–3 months to reach steady state.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; ~25% renal excretion (mostly as metabolites), ~60% fecal excretion (mostly as metabolites).
Approximately 25% of the dose is excreted in urine as unchanged drug and metabolites; about 54% is excreted in feces. Renal excretion of unchanged drug is minor (<1%).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic
Brexpiprazole + Sulfisoxazole
"The serum concentration of Sulfisoxazole can be increased when it is combined with Brexpiprazole."