Comparative Pharmacology
Head-to-head clinical analysis: REXULTI versus ZIPRASIDONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: REXULTI versus ZIPRASIDONE HYDROCHLORIDE.
REXULTI vs ZIPRASIDONE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A and α1B/α2C adrenergic receptors.
Ziprasidone is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also antagonizes 5-HT2C, 5-HT1D, and alpha1-adrenergic receptors, and has moderate affinity for histamine H1 and alpha2-adrenergic receptors. It exhibits partial agonism at 5-HT1A receptors.
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.
20 mg PO BID with food, titrated up to max 80 mg PO BID; IM: 10-20 mg q2h or q4h, max 40 mg/day
None Documented
None Documented
Terminal 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.
Terminal elimination half-life is approximately 7 hours (range 6–10 hours) for oral administration; clinically, steady state is achieved within 1–3 days.
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%).
Primarily hepatic metabolism via aldehyde oxidase and CYP3A4; <1% excreted unchanged in urine, approximately 20% in feces as metabolites.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic