Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus ZYPREXA RELPREVV.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus ZYPREXA RELPREVV.
SAPHRIS vs ZYPREXA RELPREVV
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.
Olanzapine pamoate is a second-generation antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also binds to adrenergic α1, histamine H1, and muscarinic M1 receptors.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
210 mg intramuscular injection every 2 weeks; range 150-300 mg; max 300 mg per dose. For olanzapine-naive patients, establish tolerability with oral olanzapine before initiation.
None Documented
None Documented
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
The terminal elimination half-life ranges from 30 to 60 days (mean ~45 days) after intramuscular injection, consistent with extended release from the depot formulation.
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 57% of the dose is excreted in urine (30% as unchanged drug, 27% as metabolites) and 30% in feces (primarily as metabolites).
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic