Comparative Pharmacology
Head-to-head clinical analysis: BREXPIPRAZOLE versus RISPERDAL CONSTA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BREXPIPRAZOLE versus RISPERDAL CONSTA.
BREXPIPRAZOLE vs RISPERDAL CONSTA
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.
Risperidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also binds to alpha1-adrenergic, alpha2-adrenergic, and histamine H1 receptors, with low affinity for muscarinic receptors. The combination of 5-HT2A and D2 antagonism is thought to improve negative symptoms and reduce extrapyramidal side effects.
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.
25 mg intramuscular every 2 weeks; may increase to 37.5 mg or 50 mg after 4 weeks if needed.
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.
The terminal elimination half-life of risperidone is approximately 20 hours for CYP2D6 extensive metabolizers and 24 hours for poor metabolizers (accounting for both risperidone and 9-hydroxyrisperidone). The half-life of the active moiety is about 20 hours, allowing for biweekly dosing of the long-acting injection.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; ~25% renal excretion (mostly as metabolites), ~60% fecal excretion (mostly as metabolites).
Risperidone and its active metabolite 9-hydroxyrisperidone are primarily excreted renally (70%), with 14% excreted in feces. The remainder is eliminated via biliary and metabolic pathways.
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."