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Resources › Psychotropics A-Z › Asenapine | Saphris | Saphris
Atypical (Second-Generation) Antipsychotic

Asenapine | Saphris

Clinical Overview

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.

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.

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
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.