Comparative Pharmacology
Head-to-head clinical analysis: QUETIAPINE FUMARATE versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: QUETIAPINE FUMARATE versus SAPHRIS.
QUETIAPINE FUMARATE vs SAPHRIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Antagonist at serotonin 5-HT2A, dopamine D2, histamine H1, alpha1-adrenergic, and muscarinic M1 receptors. Also partial agonist at serotonin 5-HT1A and dopamine D2 receptors (depending on dose).
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.
Immediate release: 25-100 mg orally twice daily, titrated as needed up to 400-800 mg/day divided twice daily. Extended release: 50-200 mg orally once daily, titrated up to 400-800 mg/day once daily.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
None Documented
None Documented
Terminal elimination half-life is approximately 6-7 hours (quetiapine) and 9-12 hours for the active metabolite norquetiapine; with extended-release formulation, effective half-life is ~7 hours due to slower absorption. Clinical steady-state achieved within 2 days.
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Renal: 73% (20% unchanged, remainder as metabolites); Fecal: 21%; Approximately 5% excreted in feces as unchanged drug.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic