Comparative Pharmacology
Head-to-head clinical analysis: ASENAPINE MALEATE versus INVEGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASENAPINE MALEATE versus INVEGA.
ASENAPINE MALEATE vs INVEGA
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.
Paliperidone is the major active metabolite of risperidone. It is a benzisoxazole derivative antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also acts as an antagonist at α1 and α2 adrenergic receptors and H1 histaminergic receptors. It has no affinity for muscarinic receptors.
Sublingual: 5-10 mg twice daily; initial dose 5 mg twice daily, max 10 mg twice daily.
Oral: 6 mg once daily; may increase to 9 mg/day if needed. IM (extended-release): 234 mg on day 1, 156 mg on day 8, then 117 mg monthly; adjust within range 39-234 mg per month.
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.
Terminal elimination half-life is approximately 23-29 hours for oral administration (paliperidone extended-release). Once-daily dosing achieves steady-state within 4-5 days.
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.
Primarily renal: 59-80% of dose excreted unchanged in urine (as parent drug and metabolites). Fecal: ~20-30%. Biliary elimination is minimal.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic