Comparative Pharmacology
Head-to-head clinical analysis: SAPHRIS versus SECUADO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SAPHRIS versus SECUADO.
SAPHRIS vs SECUADO
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-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.
SECUADO (asenapine) is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors, as well as dopamine D2, D3, and D4 receptors. It also exhibits moderate affinity for histamine H1 and alpha2-adrenergic receptors, and low affinity for alpha1 and muscarinic receptors. The therapeutic effect in schizophrenia and bipolar disorder is primarily mediated through antagonism at D2 and 5-HT2A receptors.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
Adults: 3.8 mg/24 hours applied transdermally once daily; initially 3.8 mg/24 hours, may titrate to 5.7 mg/24 hours, 7.6 mg/24 hours, or 11.4 mg/24 hours based on tolerability and efficacy. Maximum dose: 11.4 mg/24 hours.
None Documented
None Documented
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Terminal elimination half-life: 20-24 hours; steady-state achieved within 5 days.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Primarily renal: 50-80% as unchanged drug; biliary/fecal: <15%.
Category C
Category C
Atypical Antipsychotic
Atypical Antipsychotic