Comparative Pharmacology
Head-to-head clinical analysis: ASENAPINE MALEATE versus ZYPREXA ZYDIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ASENAPINE MALEATE versus ZYPREXA ZYDIS.
ASENAPINE MALEATE vs ZYPREXA ZYDIS
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.
Olanzapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A and 5-HT2C receptors, dopamine D1-D4 receptors, muscarinic M1-M5 receptors, histamine H1 receptors, and alpha1-adrenergic receptors. Antagonism at D2 and 5-HT2A receptors is primarily responsible for its antipsychotic effects.
Sublingual: 5-10 mg twice daily; initial dose 5 mg twice daily, max 10 mg twice daily.
10 mg orally once daily; range 5-20 mg once daily. Initial dose 5-10 mg, titrate by 5 mg weekly. Maximum 20 mg/day. Orally disintegrating tablet.
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: ~30 hours (range 21–54 hours) in healthy adults; prolonged in elderly (mean 51.8 h) and hepatic 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: ~57% (as metabolites); Fecal: ~30% (as metabolites); Unchanged olanzapine in urine <7%.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic