Comparative Pharmacology
Head-to-head clinical analysis: ASENAPINE MALEATE versus NUPLAZID.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASENAPINE MALEATE versus NUPLAZID.
ASENAPINE MALEATE vs NUPLAZID
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.
Selective serotonin 5-HT2A receptor inverse agonist and antagonist; also has moderate affinity for 5-HT2C and 5-HT1A receptors.
Sublingual: 5-10 mg twice daily; initial dose 5 mg twice daily, max 10 mg twice daily.
34 mg orally once daily.
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 50 hours (range 40-70 hours), allowing once-daily dosing.
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.
Fecal (approximately 60%) as unchanged drug and metabolites; renal (approximately 13%) as unchanged drug and metabolites.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic