Comparative Pharmacology
Head-to-head clinical analysis: RISPERDAL versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: RISPERDAL versus SAPHRIS.
RISPERDAL vs SAPHRIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Risperidone is a benzisoxazole atypical antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors. It also blocks alpha1-adrenergic, alpha2-adrenergic, and histamine H1 receptors.
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.
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
None Documented
None Documented
20 hours (parent drug), 23 hours (active metabolite 9-hydroxyrisperidone). Steady state reached in 5-6 days. Extended in elderly and hepatic/renal impairment.
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Renal: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
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 C
Category C
Atypical Antipsychotic
Atypical Antipsychotic