Comparative Pharmacology
Head-to-head clinical analysis: BREXPIPRAZOLE versus SECUADO.
Head-to-head clinical analysis: BREXPIPRAZOLE versus SECUADO.
BREXPIPRAZOLE vs SECUADO
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.
SECUADO (asenapine) is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors, as well as dopamine D2, D3, and D4 receptors. It also exhibits moderate affinity for histamine H1 and alpha2-adrenergic receptors, and low affinity for alpha1 and muscarinic receptors. The therapeutic effect in schizophrenia and bipolar disorder is primarily mediated through antagonism at D2 and 5-HT2A 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.
Adults: 3.8 mg/24 hours applied transdermally once daily; initially 3.8 mg/24 hours, may titrate to 5.7 mg/24 hours, 7.6 mg/24 hours, or 11.4 mg/24 hours based on tolerability and efficacy. Maximum dose: 11.4 mg/24 hours.
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: 20-24 hours; steady-state achieved within 5 days.
Primarily hepatic metabolism via CYP3A4 and CYP2D6; ~25% renal excretion (mostly as metabolites), ~60% fecal excretion (mostly as metabolites).
Primarily renal: 50-80% as unchanged drug; biliary/fecal: <15%.
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."