What is Saphris (Asenapine) Used For?
Saphris (asenapine) is FDA-approved for the acute treatment of manic or mixed episodes associated with bipolar I disorder in adults, and for the acute treatment of schizophrenia in adults. 1
FDA-Approved Indications
Bipolar I Disorder
- Asenapine is indicated for the acute treatment of manic or mixed episodes with or without psychotic features in adults with bipolar I disorder. 2, 3
- The medication can be used as monotherapy or as adjunctive therapy to lithium or valproate for treating acute manic episodes. 3, 4
- Asenapine demonstrated significant superiority over placebo in reducing Young Mania Rating Scale (YMRS) total scores, with significant differences emerging after just 2 days of treatment in pivotal trials. 3
Schizophrenia
- Asenapine is approved for the acute treatment of schizophrenia in adults, demonstrating efficacy in reducing Positive and Negative Syndrome Scale (PANSS) total scores compared to placebo at 6 weeks. 4
Formulation and Administration
- Asenapine is available as a sublingual tablet (5 mg or 10 mg) that dissolves rapidly under the tongue, making it the first atypical antipsychotic formulated in this manner. 2, 5
- A transdermal patch formulation (SECUADO) is also available, delivering 3.8 mg, 5.7 mg, or 7.6 mg of asenapine over 24 hours. 1
- The sublingual route requires patients to avoid food and liquids for at least 10 minutes post-administration to ensure proper absorption. 6
Mechanism of Action
- Asenapine exhibits high affinity antagonism at multiple receptor subtypes, including serotonergic (5-HT2A-C, 5-HT6, 5-HT7), dopaminergic (D2, D3), alpha-adrenergic (α1 and α2), and histaminergic (H1, H2) receptors. 2, 4
- The efficacy in schizophrenia and bipolar disorder is likely mediated through combined D2 and 5-HT2A receptor antagonism. 1
- Notably, asenapine has no appreciable affinity for muscarinic cholinergic receptors, which may reduce anticholinergic side effects. 1, 5
Clinical Efficacy Timeline
- Rapid onset of action is observed, with significant improvements in manic symptoms appearing within 2 days of treatment initiation. 3
- Full therapeutic effects typically emerge within 2-3 weeks for acute manic episodes. 2, 3
- Extension studies demonstrate that efficacy can be maintained over 40-52 weeks of continuous treatment. 3
Common Pitfalls to Avoid
- Do not use asenapine for bipolar depression as monotherapy—it is only approved for manic and mixed episodes, not depressive episodes. 2
- The sublingual tablet must not be swallowed whole, as oral bioavailability is extremely low; it must dissolve under the tongue for proper absorption. 6
- Patients must be counseled to avoid eating or drinking for 10 minutes after sublingual administration to prevent reduced absorption. 6
- The transdermal patch formulation should never be exposed to external heat sources (heating pads, electric blankets), as this increases absorption rate approximately 3.9-fold and may cause overdose. 1