Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus SEROQUEL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus SEROQUEL.
SAPHRIS vs SEROQUEL
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.
Antagonist at dopamine D2 and serotonin 5-HT2A receptors; also blocks histamine H1 and adrenergic α1 receptors.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
Initial: 25 mg twice daily; titrate by 25-50 mg twice daily on day 2 and 3 to target 300-400 mg daily in 2-3 divided doses. Maintenance: 400-800 mg daily. Maximum: 800 mg daily.
None Documented
None Documented
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Terminal elimination half-life approximately 7 hours for quetiapine; for metabolite N-desalkylquetiapine (norquetiapine), approximately 12 hours. Steady-state reached within 2 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; <1% excreted unchanged renally. Metabolites excreted in urine (73%) and feces (20%).
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic