Asenapine monotherapy in the acute treatment of both schizophrenia and bipolar I disorder

Review

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Authors: Delia Bishara, David Taylor

Published Date September 2009 Volume 2009:5 Pages 483 - 490

DOI: http://dx.doi.org/10.2147/NDT.S5742

Delia Bishara¹, David Taylor^1,2

¹Pharmacy Department, South London and Maudsley NHS Foundation Trust, Denmark Hill, London, UK; ²Division of Pharmaceutical Sciences, King’s College, London, UK

Abstract: Asenapine is a new atypical antipsychotic agent currently under development for the treatment of schizophrenia and bipolar disorder. It has high affinity for various receptors including antagonism at 5HT_2A, 5HT_2B, 5HT_2C, 5HT₆ and 5HT₇ serotonergic receptor subtypes, α_1A, α_2A, α_2B and α_2C adrenergic and D₃ and D₄ dopaminergic receptors. As with other atypicals, asenapine exhibits a high 5HT_2A:D₂ affinity ratio. Although similar to clozapine in its multitarget profile, it shows no appreciable affinity for muscarinic receptors. Asenapine has shown efficacy in alleviating both positive and negative symptoms of schizophrenia compared with placebo. Although promising, further studies are required in order to determine whether it has advantages over placebo and other antipsychotics in alleviating cognitive impairment associated with schizophrenia. It has also shown long-term efficacy comparable with olanzapine in bipolar I disorder. Asenapine is generally well tolerated and appears to be metabolically neutral. It has low propensity to cause weight gain and prolactin elevation. There were no concerns in the studies about its effects on the cardiovascular system and QTc prolongation. The incidence of extrapyramidal symptoms with asenapine however has been found to be higher than that with olanzapine. It may be a useful alternative to aripiprazole in schizophrenia and bipolar disorder in patients who are at high risk of metabolic abnormalities.

Keywords: asenapine, schizophrenia, bipolar I disorder, antipsychotics