Asenapine monotherapy in the acute treatment of both schizophrenia and bipolar I disorder
Delia Bishara1, David Taylor1,2
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 5HT2A, 5HT2B, 5HT2C, 5HT6 and 5HT7 serotonergic receptor subtypes, α1A, α2A, α2B and α2C adrenergic and D3 and D4 dopaminergic receptors. As with other atypicals, asenapine exhibits a high 5HT2A: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
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