Asenapine
Asenapine is an atypical antipsychotic available as sublingual tablets (Saphris) and transdermal patch (Secuado), indicated for schizophrenia and manic or mixed episodes of bipolar I disorder. It has a unique receptor binding profile with high affinity for multiple serotonin and dopamine receptors, potentially offering broad therapeutic effects.
Clinical Overview
Primary Clinical Applications
Asenapine is indicated for acute treatment of schizophrenia in adults, manic or mixed episodes associated with bipolar I disorder in adults, and manic or mixed episodes in pediatric patients (10-17 years). The transdermal patch formulation provides an alternative for patients with adherence issues or swallowing difficulties.
Mechanism and Clinical Benefits
Asenapine has high affinity for dopamine D2, D3, D4, serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, 5-HT7, and histamine H1 receptors. This broad receptor profile may contribute to efficacy for both positive and negative symptoms while potentially offering mood-stabilizing effects.
Administration Considerations
The sublingual formulation requires specific administration techniques (dissolve under tongue, avoid eating/drinking for 10 minutes) and may cause oral numbness. The transdermal patch provides steady drug delivery over 24 hours and eliminates first-pass metabolism, potentially improving tolerability.
Key Clinical Points
Sublingual administration is not optional
The tablet must dissolve under the tongue with no eating or drinking for ten minutes afterwards. Swallowing it defeats absorption entirely, which makes administration technique a common and silent cause of apparent treatment failure.
Oral numbness is the characteristic complaint
Oral hypoesthesia is among the most frequently reported adverse effects of the sublingual formulation and a common reason for discontinuation. The transdermal patch avoids it.
Transdermal option for adherence problems
Secuado delivers over 24 hours, bypasses first-pass metabolism, and removes the administration-technique problem entirely. Useful where swallowing difficulty or adherence is the limiting factor.
Contraindicated in severe hepatic impairment
Child-Pugh C is an absolute contraindication. No adjustment is needed for mild to moderate impairment, and none for renal impairment at any stage.
Fluvoxamine substantially raises levels
As a strong CYP1A2 inhibitor, fluvoxamine significantly increases asenapine concentrations. Strong CYP1A2 inducers have the opposite effect. Angioedema and anaphylaxis have also been reported.
Prescribing Information
Dosing & Administration
Schizophrenia (Saphris) – Adults:
- Initial: 5 mg twice daily
- Range: 5-10 mg twice daily
- Maximum: 10 mg twice daily
Schizophrenia (Secuado patch) – Adults:
- Initial: 3.8 mg/24 hours patch daily
- Range: 3.8-7.6 mg/24 hours daily
- Maximum: 7.6 mg/24 hours daily
Bipolar I Disorder – Manic/Mixed Episodes (Adults):
- Monotherapy: 10 mg twice daily initially, may decrease to 5 mg twice daily if tolerated
- Adjunctive therapy: 5 mg twice daily initially, may increase to 10 mg twice daily
Bipolar I Disorder – Pediatric (10-17 years):
- Initial: 2.5 mg twice daily
- Target: 5 mg twice daily after 3 days
- Maximum: 10 mg twice daily
Administration:
- Sublingual: Place under tongue, allow to dissolve completely, avoid eating/drinking for 10 minutes
- Patch: Apply to clean, dry skin on upper arm, back, abdomen, or hip; rotate sites
Indications
- Treatment of schizophrenia (adults)
- Acute treatment of manic or mixed episodes associated with bipolar I disorder (adults and pediatric patients 10-17 years)
Contraindications
- Known hypersensitivity to asenapine or any component
- Severe hepatic impairment (Child-Pugh C)
Warnings & Precautions
- Boxed Warning: Increased mortality in elderly patients with dementia-related psychosis; increased suicidal risk in children, adolescents, and young adults
- Neuroleptic malignant syndrome: Rare but serious risk
- Tardive dyskinesia: Risk with long-term use
- Metabolic changes: Monitor glucose, lipids, and weight
- QT prolongation: Use caution in patients with cardiac risk factors
- Orthostatic hypotension: Monitor blood pressure
- Hypersensitivity reactions: Angioedema and anaphylaxis reported
Drug Interactions
- Strong CYP1A2 inducers: May decrease asenapine levels
- Fluvoxamine (CYP1A2 inhibitor): Significantly increases asenapine levels
- QT-prolonging drugs: Use caution, monitor ECG
- CNS depressants: Enhanced sedation
Adverse Reactions
Common (≥5%) – Sublingual:
- Oral hypoesthesia (numbness), dizziness, akathisia
- Weight gain, sedation, extrapyramidal symptoms
Common – Transdermal:
- Application site reactions, weight gain, somnolence
Serious:
- Neuroleptic malignant syndrome, tardive dyskinesia, severe hypersensitivity
Special Populations
- Hepatic Impairment: Mild-moderate: no adjustment; Severe: contraindicated
- Renal Impairment: No dose adjustment needed
- Elderly: Increased mortality risk in dementia-related psychosis
- Pregnancy: Category C – use only if benefits outweigh risks
- Patch application: Avoid heat sources, remove before MRI
Frequently Asked Questions
What is Asenapine used for?
Asenapine is an atypical antipsychotic available as sublingual tablets (Saphris) and transdermal patch (Secuado), indicated for schizophrenia and manic or mixed episodes of bipolar I disorder. It has a unique receptor binding profile with high affinity for multiple serotonin and dopamine receptors, potentially offering broad therapeutic effects.
What class of drug is Asenapine?
Asenapine is classified as: Atypical (Second-Generation) Antipsychotic.
Sublingual administration is not optional?
The tablet must dissolve under the tongue with no eating or drinking for ten minutes afterwards. Swallowing it defeats absorption entirely, which makes administration technique a common and silent cause of apparent treatment failure.
Oral numbness is the characteristic complaint?
Oral hypoesthesia is among the most frequently reported adverse effects of the sublingual formulation and a common reason for discontinuation. The transdermal patch avoids it.
Transdermal option for adherence problems?
Secuado delivers over 24 hours, bypasses first-pass metabolism, and removes the administration-technique problem entirely. Useful where swallowing difficulty or adherence is the limiting factor.
Contraindicated in severe hepatic impairment?
Child-Pugh C is an absolute contraindication. No adjustment is needed for mild to moderate impairment, and none for renal impairment at any stage.
Source: FDA prescribing information (DailyMed)