Asenapine, sold as Saphris and (in patch form) Secuado, was approved by the FDA in 2009 for schizophrenia and bipolar I disorder. It is unusual among antipsychotics for two reasons: the standard formulation is taken sublingually (dissolved under the tongue), and a transdermal patch version was approved in 2019. The sublingual route is necessary because asenapine has very poor oral bioavailability — swallowing the tablet wastes most of the dose.
Asenapine is a second-generation antipsychotic available as a sublingual tablet or transdermal patch — useful for schizophrenia and bipolar mania, with side effects shaped by its unusual delivery routes.
What asenapine is
Asenapine is a "dibenzo-oxepino pyrrole" with broad receptor activity — antagonism at dopamine D2, serotonin 5-HT2A, 5-HT2C, 5-HT7, alpha-adrenergic, and histamine receptors. The full FDA prescribing information is available through Drugs@FDA.
What it treats
- Schizophrenia in adults (Saphris) and the patch (Secuado) for adults
- Acute mania or mixed episodes in bipolar I disorder, in adults and children ages 10 and up
- Maintenance treatment of bipolar I disorder as monotherapy
Typical dosing range
FDA-labelled adult dose ranges:
- Sublingual Saphris: 5 to 10 mg twice daily for schizophrenia
- Secuado patch: 3.8, 5.7, or 7.6 mg per 24 hours, applied once daily
Specific dosing should come from your prescriber.
How sublingual administration works
The sublingual tablet must be placed under the tongue and allowed to dissolve completely (typically about 10 seconds). After dissolving, patients are advised not to eat or drink for 10 minutes. Swallowing the tablet whole essentially wastes the dose — only about 2% is absorbed when swallowed compared to roughly 35% sublingually.
This is a real adherence challenge. Patients have to plan to take medication apart from meals and drinks. For those who can manage it, the sublingual route bypasses first-pass liver metabolism and produces a quick onset, useful in acute mania.
The patch (Secuado)
Secuado is a once-daily patch applied to the upper arm, abdomen, hip, or back, and rotated daily. The transdermal route avoids the eat/drink restrictions of the sublingual form and provides steady drug levels. Skin reactions at the patch site are the most common new side effect.
Common side effects
- Sedation — common
- Dizziness
- Akathisia and other extrapyramidal symptoms — moderate
- Mild to moderate weight gain
- Oral hypoaesthesia (tongue/mouth numbness) — distinctive to the sublingual form, lasting 1–2 hours after each dose
- Bitter taste
- Skin reactions — with the patch
Serious side effects
Severe allergic reactions, including swelling of the face, tongue, or throat (asenapine has been associated with serious hypersensitivity reactions, including anaphylaxis); high fever with rigidity (possible neuroleptic malignant syndrome); persistent involuntary movements (possible tardive dyskinesia).
- Hypersensitivity reactions, including anaphylaxis (the FDA issued a specific warning for this in 2011)
- QT prolongation (mild)
- Tardive dyskinesia with long-term use
- Neuroleptic malignant syndrome (rare)
- Standard boxed warnings: increased mortality in elderly with dementia-related psychosis; increased suicidality in young adults treated for depression (when applicable)
What patients commonly say
- "The numbness in my mouth was strange at first, but I got used to it."
- "Remembering not to eat or drink for 10 minutes was harder than I expected."
- "The patch fixed that — I just put it on each morning and didn't think about it."
- "It worked quickly when I was manic."
Questions for your prescriber
- Would the patch be a better fit than the sublingual tablet for me?
- What signs of allergic reaction should I watch for?
- How will we monitor for movement effects?
- Are there other medications I take that might interact?
Putting it together
Asenapine occupies a niche in the antipsychotic landscape. The sublingual route is helpful for some patients — particularly those who struggle to swallow pills or who need rapid onset in acute mania — but the eat/drink restriction limits convenience. The patch form addresses many of those issues. The hypersensitivity warning is worth knowing about. As with every antipsychotic, the choice is best made with a prescriber who weighs the full picture.
This article is for educational purposes only and is not medical advice. Information is summarised from publicly available FDA labelling and peer-reviewed literature. Always consult your prescribing clinician before starting, stopping, or changing any medication. If you or someone you know is in crisis, call or text 988 in the US, or your local emergency number.