Comparative Pharmacology
Head-to-head clinical analysis: BREXPIPRAZOLE versus SEROQUEL XR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREXPIPRAZOLE versus SEROQUEL XR.
BREXPIPRAZOLE vs SEROQUEL XR
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.
SEROQUEL XR (quetiapine fumarate) is an atypical antipsychotic that acts as an antagonist at multiple neurotransmitter receptors: serotonin 5-HT1A and 5-HT2A, dopamine D1 and D2, histamine H1, and adrenergic α1 and α2 receptors. It also has partial agonist activity at 5-HT1A receptors. The therapeutic efficacy in schizophrenia and bipolar disorder is primarily attributed to dopamine D2 and serotonin 5-HT2A antagonism.
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.
Initial: 300 mg orally once daily; may increase by 300 mg/day every 2-3 days. Target dose: 400-800 mg/day for schizophrenia; 300-600 mg/day for bipolar depression; 400-800 mg/day for acute mania. Maximum: 800 mg/day.
None Documented
None Documented
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
moderate91 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.
Terminal elimination half-life: approximately 7 hours (range 6-9 hours) for the extended-release formulation. Clinical context: once-daily dosing achieves steady-state within 2 days.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; ~25% renal excretion (mostly as metabolites), ~60% fecal excretion (mostly as metabolites).
Primarily hepatic; 70-73% excreted in urine as metabolites (mostly inactive), 20-24% in feces. Less than 1% excreted unchanged in urine.
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."