Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus ZIPRASIDONE HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus ZIPRASIDONE HYDROCHLORIDE.
SAPHRIS vs ZIPRASIDONE HYDROCHLORIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Asenapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors; dopamine D2, D3, and D4 receptors; and alpha2-adrenergic receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic receptors, and low affinity for muscarinic M1 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.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
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 30-40 hours, supporting once-daily 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.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
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