Asenapine: a synthesis of efficacy data in bipolar mania and schizophrenia.

INTRODUCTION: This article briefly reviews the efficacy, as well as safety and tolerability, data pertaining to asenapine in bipolar mania and schizophrenia. Postulated mechanism of action is also reviewed.
METHODS: A PubMed search was conducted using the search term asenapine. All displayed articles were reviewed; we selected for review studies that were part of the regulatory registration package to the FDA as part of the bipolar disorder and schizophrenia indication. We also included a review of articles reporting on asenapine's preclinical profile.
RESULTS: Asenapine is a recently introduced atypical antipsychotic approved by the FDA for bipolar mania and mixed states with or without psychotic features, as well as for the treatment and prevention of psychotic relapses in schizophrenia. Preliminary evidence suggests that asenapine mitigates depressive symptoms in bipolar mania and offers superior efficacy to olanzapine or risperidone in the negative symptoms of schizophrenia. The pharmacodynamic profile of asenapine provides a rationale for hypothesizing efficacy in the treatment of cognitive deficits in mood and psychotic disorders. Asenapine is associated with sedation and/or somnolence; it has a lower propensity to weight gain and metabolic disruption than olanzapine. Extrapyramidal side effects (EPS) are associated with asenapine and may be dose-dependent. Asenapine is not associated with sustained hyperprolactinemia or cardiovascular toxicity. Dysgeusia and oral hypoesthesia/paresthesia is associated with asenapine, but is rarely a cause for treatment discontinuation.
CONCLUSIONS: Asenapine is the only atypical antipsychotic available exclusively as a sublingual, fast-dissolved formulation. Electrophysiological, behavioral, pharmacological, and radioligand studies are predictive of antidepressant, mood-stabilizing, as well as antipsychotic, effects.