Comparative Pharmacology
Head-to-head clinical analysis: UZEDY versus ZIPRASIDONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: UZEDY versus ZIPRASIDONE HYDROCHLORIDE.
UZEDY vs ZIPRASIDONE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Atypical antipsychotic; antagonist at dopamine D2 and serotonin 5-HT1A/5-HT2A receptors; partial agonist at serotonin 5-HT1A 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.
UZEDY (risperidone) extended-release injectable suspension: 75 mg, 100 mg, 150 mg, or 200 mg IM gluteal injection every 2 weeks after a single oral dose of 2 mg risperidone for 2 days; or 25 mg, 50 mg, 75 mg, 100 mg, 125 mg, or 150 mg IM every 4 weeks after oral overlap for 2 days. Oral risperidone may be omitted if patient is stable on oral risperidone 2 mg/day.
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 half-life approximately 30 days (range 23–37 days) after subcutaneous injection, supporting monthly dosing.
Terminal elimination half-life is approximately 7 hours (range 6–10 hours) for oral administration; clinically, steady state is achieved within 1–3 days.
Primarily renal: 80% as metabolites, 1% unchanged. Biliary/fecal: 20%.
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