Asenapine
Saphris · Secuado
Second-Generation AntipsychoticGeneric availableTDM data
Asenapine is a dibenzo-oxepino pyrrole derivative with antagonist activity at multiple receptors including D2, 5-HT2A, 5-HT2C, 5-HT7, alpha1, alpha2, and H1 receptors. Its complex receptor binding profile includes very high 5-HT2A/D2 ratio. Available as sublingual tablet (Saphris) and transdermal patch (Secuado).
Compare Asenapine →FDA-Approved Indications
- Schizophrenia
- Acute treatment of manic or mixed episodes associated with bipolar I disorder
- Schizophrenia (transdermal)
What Sets This Drug Apart
- Sublingual-only administration — oral bioavailability <2% if swallowed, requiring under-tongue dissolution with no eating/drinking for 10 minutes
- Also available as transdermal patch (Secuado) — only SGA with a patch formulation
- Broadest receptor binding profile of any SGA — sub-nanomolar 5-HT2A and 5-HT2C affinity may contribute to lower metabolic risk than olanzapine
- Oral hypoesthesia/dysgeusia unique to sublingual formulation — numb tongue in 5-6% of patients
- Moderate weight gain profile — less than olanzapine/clozapine but more than aripiprazole/ziprasidone
Boxed Warning
Increased mortality in elderly patients with dementia-related psychosis (class effect)