Comparative Pharmacology
Head-to-head clinical analysis: BREXPIPRAZOLE versus ZYPREXA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREXPIPRAZOLE versus ZYPREXA.
BREXPIPRAZOLE vs ZYPREXA
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.
Olanzapine is an atypical antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors, with higher affinity for 5-HT2A than D2. It also blocks histamine H1, alpha-1 adrenergic, and muscarinic M1 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.
5-10 mg orally once daily; may increase by 5 mg/day at intervals of at least 1 week; maximum 20 mg/day.
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 ~30 hours (range 21–54 h) in adults, allowing once-daily dosing; steady-state reached in ~5–7 days. Half-life prolonged in elderly, females, and hepatic impairment.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; ~25% renal excretion (mostly as metabolites), ~60% fecal excretion (mostly as metabolites).
Primarily hepatic metabolism via CYP1A2 and CYP2D6; ~7% excreted unchanged in urine, ~57% in urine as metabolites, ~30% in feces (mostly metabolites).
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."