asenapine

Antipsychotic

Brands: Saphris, Secuado

Last reviewed 2025-12-29

Reviewed by PsychMed Editorial Team.

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Quick answers

What is asenapine?
Asenapine (brand Saphris sublingual tablets; Secuado transdermal system) is a second-generation (atypical) antipsychotic formulated to avoid extensive first-pass metabolism and provide rapid absorption.
What is Saphris?
Saphris is a brand name for asenapine (other brands: Secuado).
What is Saphris (asenapine) used for?
Label indications include: Schizophrenia (sublingual tablet); Schizophrenia (transdermal patch); Acute manic/mixed episodes in bipolar I disorder (adults); Acute manic/mixed episodes in bipolar I disorder (pediatrics ≥10).
What drug class is Saphris (asenapine)?
Antipsychotic.
What is the mechanism of action of Saphris (asenapine)?
Second-generation antipsychotic with antagonism at dopamine D2/D3 and serotonin 5-HT2A receptors; also blocks H1 and α1 receptors.
What strengths does Saphris (asenapine) come in?
Sublingual tablets: 2.5 mg, 5 mg, 10 mg (taken twice daily; must dissolve under the tongue).
Is Saphris (asenapine) a controlled substance?
No — it is not scheduled as a controlled substance under U.S. federal law.
What is Saphris (asenapine) dosing for schizophrenia?
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.

Snapshot

Class: Antipsychotic
Common US brands: Saphris, Secuado
Therapeutic drug monitoring not routinely recommended.
Last reviewed: 2025-12-29

Clinical Highlights

Asenapine (brand Saphris sublingual tablets; Secuado transdermal system) is a second-generation (atypical) antipsychotic formulated to avoid extensive first-pass metabolism and provide rapid absorption. This profile focuses on its use in schizophrenia and bipolar I disorder; U.S. approvals include schizophrenia in adults (sublingual 2009, transdermal 2019) and acute manic or mixed episodes in adults and pediatric patients ≥10 years, as monotherapy or adjunct to lithium/valproate.

Sublingual tablets can cause oral numbness and require avoiding food or drink for 10 minutes after dosing. The patch can be helpful when swallowing is unreliable or when a patient declines LAIs, but cost and skin reactions can be limiting.
The compare view to benchmark sedation, metabolic, and formulation considerations, and review asenapine-focused evidence alongside resources in the schizophrenia hub and bipolar disorder hub when coordinating long-term care.
Schizophrenia (sublingual tablet) (FDA 2009)
Schizophrenia (transdermal patch) (FDA 2019)
Acute manic/mixed episodes in bipolar I disorder (adults) (FDA 2009)

Dosing & Formulations

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.

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.
Bipolar I acute manic/mixed episodes (adults): start 10 mg sublingually twice daily on day 1, then 5–10 mg twice daily; adjunct dosing with lithium/valproate mirrors monotherapy.
Pediatric bipolar I (≥10 years): initiate 2.5 mg twice daily; titrate by 2.5–5 mg to a maximum 10 mg twice daily.
Therapeutic drug monitoring is not routinely recommended; serum levels have not correlated with efficacy.

Monitoring & Risks

Boxed warning: Increased mortality in elderly patients with dementia-related psychosis (antipsychotic class warning). Somnolence/sedation: Reported in ~13–24% of patients; leading reason for discontinuation.

Akathisia/restlessness: Occurs in ~10–12%, often within first 3 weeks.
Oral hypoesthesia/dysgeusia: Unique to sublingual formulation (7–15%); typically transient.
Weight gain: ≥7% weight gain in roughly 7–9% over 3–6 months.
Dizziness/orthostatic hypotension: Around 10%, more common during initial titration.

Drug Interactions

Strong CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) raise concentrations—monitor for sedation and EPS; dose reduction may be needed. CYP1A2 inducers, including cigarette smoking and carbamazepine, lower exposure—monitor efficacy and adjust dose within labeling limits.

Potent enzyme inducers affecting UGT pathways (e.g., rifampin) can reduce levels; consider alternatives or monitor closely.
Additive CNS depression with benzodiazepines, opioids, alcohol, or antihistamines.
May antagonize effects of levodopa and dopamine agonists; avoid coadministration in Parkinson’s disease when possible.

Practice Notes

Store sublingual tablets in original blister packaging; handle with dry hands and allow to dissolve fully under the tongue. Oral numbness usually resolves within an hour; severe dysesthesia, swelling, or signs of hypersensitivity warrant urgent evaluation.

Rotate patch sites daily (upper arm, abdomen, hip, back) and inspect for erythema; mild application-site reactions occur in <10%.
Weight, fasting lipids, and glucose are typically monitored periodically despite relatively modest metabolic liability.
Changes in smoking status can alter plasma exposure through CYP1A2 induction or cessation; dosing may need reassessment when tobacco use changes.
Consider baseline and follow-up ECGs in patients with cardiac risk factors or concomitant QT-prolonging regimens.
Share printable counseling sheets from the asenapine print view, compare alternatives via the contrast table, and align relapse-prevention plans with the schizophrenia hub and bipolar disorder hub.

References

SAPHRIS (asenapine) prescribing information — DailyMed (2024)
SECUADO (asenapine transdermal system) prescribing information — DailyMed (2024)
A 3 Week, Randomized, Placebo Controlled Trial OF Asenapine IN THE Treatment OF Acute Mania IN Bipolar I Disorder — Bipolar Disorders (2009)
Asenapine review, part II: clinical efficacy, safety and tolerability — Expert Opinion on Drug Safety (2014)
AGNP Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology — Pharmacopsychiatry (2018)