Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus UZEDY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus UZEDY.
SAPHRIS vs UZEDY
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.
Atypical antipsychotic; antagonist at dopamine D2 and serotonin 5-HT1A/5-HT2A receptors; partial agonist at serotonin 5-HT1A receptors
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
UZEDY (risperidone) extended-release injectable suspension: 75 mg, 100 mg, 150 mg, or 200 mg IM gluteal injection every 2 weeks after a single oral dose of 2 mg risperidone for 2 days; or 25 mg, 50 mg, 75 mg, 100 mg, 125 mg, or 150 mg IM every 4 weeks after oral overlap for 2 days. Oral risperidone may be omitted if patient is stable on oral risperidone 2 mg/day.
None Documented
None Documented
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Terminal half-life approximately 30 days (range 23–37 days) after subcutaneous injection, supporting monthly 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).
Primarily renal: 80% as metabolites, 1% unchanged. Biliary/fecal: 20%.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic