asenapine

General information

• Class: Antipsychotic
• Common US brands: Saphris, Secuado
• Typical dose range: Schizophrenia (adults): initiate 5 mg sublingually twice daily; increase to 10 mg twice daily based on response; patch initiation 3.8 mg/24 h once daily with titration to 5.7–7.6 mg/24 h.
• Therapeutic drug monitoring not routinely recommended.
• Last reviewed: 2025-12-29

Dosing & forms

• Forms/strengths: Sublingual tablets: 2.5 mg, 5 mg, 10 mg (taken twice daily; must dissolve under the tongue).; Transdermal patch (Secuado): 3.8 mg/24 h, 5.7 mg/24 h, 7.6 mg/24 h applied once daily to rotating sites.
• Frequency: Schizophrenia (adults): initiate 5 mg sublingually twice daily; increase to 10 mg twice daily based on response; patch initiation 3.8 mg/24 h once daily with titration to 5.7–7.6 mg/24 h.
• Typical range: Schizophrenia (adults): initiate 5 mg sublingually twice daily; increase to 10 mg twice daily based on response; patch initiation 3.8 mg/24 h once daily with titration to 5.7–7.6 mg/24 h.

Mechanism (brief)

Second-generation antipsychotic with antagonism at dopamine D2/D3 and serotonin 5-HT2A receptors; also blocks H1 and α1 receptors.

Metabolism & Half‑life

• Metabolism: UGT1A4, CYP1A2
• Half‑life: Single-dose mean 24 h; Steady-state mean 24 h

Therapeutic Drug Monitoring (TDM)

Recommended: No

Sources

• SAPHRIS (asenapine) prescribing information — DailyMed (2024)
• SECUADO (asenapine transdermal system) prescribing information — DailyMed (2024)
• The American Psychiatric Association Practice Guideline for the Treatment of Patients With Schizophrenia — American Psychiatric Association (2020)
• The CANMAT and ISBD Guidelines for the Management of Patients With Bipolar Disorder: 2021 Update — Bipolar Disorders (2021)
• Asenapine in the treatment of acute mania associated with bipolar I disorder: a randomized double-blind trial — Bipolar Disorders (2009)
• Asenapine review, part II: clinical efficacy, safety and tolerability — Expert Opinion on Drug Safety (2014)