Asenapine: an atypical antipsychotic with atypical formulations

Abstract

Asenapine is a second-generation (atypical) antipsychotic medication not available in a pill that can be swallowed; rather, it is commercialized in sublingual and transdermal formulations. This is a consequence of extensive first-pass metabolism if ingested. The sublingual formulation is approved in many jurisdictions for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder and is available generically. The efficacy profile is well characterized in a number of clinical trials, including an off-label use for the management of agitation. Obstacles to its use include food and drink restrictions, twice-daily dosing and adverse effects such as dysgeusia (distorted, altered, or unpleasant taste) and oral hypoesthesia (numbness). Transdermal asenapine was approved by the US Food and Drug Administration in 2019 for the treatment of schizophrenia in adults. Efficacy was established in a registrational study examining acutely ill inpatients with schizophrenia. The patch needs to changed once daily. Obstacles to its use include the potential for skin reactions such as erythema and pruritis, and being a branded product, it is more costly than other options. This is a narrative review of the chemistry and pharmacokinetics/pharmacodynamics of asenapine, as well as summarizing the efficacy and tolerability of both sublingual and transdermal asenapine, and its possible place in treatment.

Acceptability of transdermal antipsychotic patches by patients who refuse oral medication and their effectiveness in preventing recurrence of delirium: a retrospective observational study

“…Transdermal antipsychotics have the potential to enhance treatment adherence, so the US Food and Drug Administration approved transdermal asenapine in 2019 for the treatment of schizophrenia in adults ( Musselman et al , 2021 ). Its possible place in real-world practice has been sought.…”

Risk of Drug-induced Movement Disorders with Newer Antipsychotic Agents

“…Data from this phase III DBRCT using sublingual asenapine showed akathisia and overall DIMD rates as high as 7.7% and 10%, respectively, during a 12–16-week open label period (n = 549) and 1.6% and 2.4%, respectively, during the 26-week double-blind phase (n = 253) relative to 0.8% in the placebo group [ 139 ]. Other studies (n = 80–532) in both schizophrenia and bipolar mania or mixed episodes showed similar rates of these AEs and minimal changes in motor rating scales [ 138 ]. No reports were found of tardive syndromes are associated with transdermal asenapine.…”

“…Patches are applied daily with equal hepatic and renal metabolism [ 137 ]. It antagonizes multiple receptors including 5-HT 2A/2B/2C/6/7 , D1/D2/D3Rs, and α 1 /α 2a/b/c adrenergic receptors with dose-dependent D2R occupancy [ 138 ].…”

Bipolar depression: a review of treatment options

“…Although generally similar, the side effect profiles of these SGAs do vary. For example, compared with other SGAs, asenapine poses relatively less risk of parkinsonism, dystonia and anticholinergic effects but relatively more weight gain and glucose abnormalities 39. Risperidone poses a higher risk of hyperprolactinaemia but relatively fewer anticholinergic side effects 40.…”

“…For example, compared with other SGAs, asenapine poses relatively less risk of parkinsonism, dystonia and anticholinergic effects but relatively more weight gain and glucose abnormalities. 39 Risperidone poses a higher risk of hyperprolactinaemia but relatively fewer anticholinergic side effects. 40 Clozapine carries a higher risk of weight gain, glucose abnormalities, hyperlipidaemia, anticholinergic side effects, sedation, agranulocytosis and electrocardiographic abnormalities, including QT interval prolongation.…”