Asenapine
SAPHRIS
What it isSecond-generation antipsychotic; schizophrenia and bipolar disorder.
Why this oneSublingual and transdermal routes bypass first-pass metabolism, which suits poor oral adherence.
What limits itIt must not be swallowed and nothing eaten or drunk for ten minutes. Oral hypoesthesia and dysgeusia.
FDA-approved for
- schizophrenia (2009)
- bipolar mania (2009)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Schizophrenia, acute | adults | 5 mg SL BID | 5 mg SL BID | 10 mg SL BID |
| Schizophrenia, maintenance | adults | 5 mg SL BID | 5-10 mg SL BID | 10 mg SL BID |
| Bipolar I mania, monotherapy (acute & maintenance) | adults | 5-10 mg SL BID | 5-10 mg SL BID | 10 mg SL BID |
| Bipolar I mania, monotherapy | peds 10-17 y | 2.5 mg SL BID | 2.5-10 mg SL BID | 10 mg SL BID |
| Bipolar I mania, adjunct to lithium/valproate | adults | 5 mg SL BID | 5-10 mg SL BID | 10 mg SL BID |
Titration Schizophrenia: may increase to 10 mg SL BID after ≥1 week if tolerated.
Renal No adjustment needed
Hepatic Severe (Child-Pugh C): contraindicated; mild-moderate: no adjustment.
Instructions
- Place sublingual tablet under the tongue and let it dissolve completely (dissolves within seconds).
- Do not split, crush, chew, or swallow the tablet.
- No eating or drinking for 10 minutes after administration.
Contraindications
- Severe hepatic impairment (Child-Pugh C)
Cautions
- Elderly dementia-related psychosis: increased cerebrovascular events
- Neuroleptic malignant syndrome
- Tardive dyskinesia
- Metabolic changes: hyperglycemia/diabetes, dyslipidemia, weight gain
- Orthostatic hypotension and syncope
- Leukopenia, neutropenia, agranulocytosis
- QT interval prolongation — avoid other QT-prolonging drugs
- Hyperprolactinemia
- Seizures
- Hypersensitivity reactions (anaphylaxis, angioedema)
Adverse reactions
- Akathisia
- Oral hypoesthesia
- Somnolence
- Dizziness
- Extrapyramidal symptoms
Pregnancy Third-trimester exposure: risk of neonatal extrapyramidal and/or withdrawal symptoms; no human data.
Lactation No human data; excreted in rat milk.
⚠ BOXED WARNING
- Increased mortality in elderly patients with dementia-related psychosis
Cost, est. cash$300–$2,500/month
Generic entry2033 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityMetabolic effects, extrapyramidal symptoms/tardive dyskinesia and agent-specific QT or orthostatic risk.
Mechanism of action: Asenapine ballicule
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Saphris is sublingual
