Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus ZIPRASIDONE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus ZIPRASIDONE MESYLATE.
SAPHRIS vs ZIPRASIDONE MESYLATE
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 mesylate is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also antagonizes 5-HT1D, 5-HT2C, and alpha1-adrenergic receptors, and inhibits serotonin and norepinephrine reuptake.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
20 mg intramuscularly (IM) as needed, not to exceed 40 mg/day; oral: 20 mg twice daily with food, titrated up to 80 mg twice daily. Maximum: 160 mg/day oral.
None Documented
None Documented
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Terminal elimination half-life is approximately 2.2 hours (range 1.4–3.6 h) for the mesylate salt; clinical context: requires twice-daily dosing.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Approximately 20% renal, 80% fecal/biliary. Unchanged drug accounts for <1% of renal excretion.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic