Comparative Pharmacology
Head-to-head clinical analysis: ASENAPINE MALEATE versus RISPERDAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASENAPINE MALEATE versus RISPERDAL.
ASENAPINE MALEATE vs RISPERDAL
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-HT1A, and dopamine D2 receptors. It also antagonizes alpha1/alpha2-adrenergic and histamine H1 receptors, with moderate affinity for D3 and D4 receptors. The therapeutic effect in schizophrenia and bipolar disorder is primarily mediated through combined 5-HT2A and D2 receptor antagonism.
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.
Sublingual: 5-10 mg twice daily; initial dose 5 mg twice daily, max 10 mg twice daily.
2-8 mg orally once daily or divided twice daily; maximum 16 mg/day
None Documented
None Documented
Terminal elimination half-life is approximately 24 hours. Steady-state is achieved within 3 days. The half-life allows for twice-daily dosing.
20 hours (parent drug), 23 hours (active metabolite 9-hydroxyrisperidone). Steady state reached in 5-6 days. Extended in elderly and hepatic/renal impairment.
Approximately 50% of the dose is excreted renally, and 40% fecally. After oral administration, about 50% appears in urine (as unchanged drug and metabolites) and 40% in feces.
Renal: 70% (30% as unchanged drug, 40% as metabolites), Fecal/Biliary: 14%
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic