Asenapine for the treatment of bipolar disorder

ABSTRACT

Introduction: Bipolar I disorder (BDI) is amongst the most debilitating psychiatric conditions with a great impact on both patients and their families. A class of drugs commonly used in this condition is second-generation antipsychotics (SGAs) including asenapine, one of the latest to be introduced into the clinical practice worldwide to treat manic episodes in BDI.

Areas covered: The aim of this paper is to critically review the literature on the pharmacological characteristics, tolerability, and safety data of asenapine, as well as on its short- and long-term clinical trials in manic episodes as both a monotherapy and as an add-on treatment.

Expert opinion: The available data indicate that asenapine is an effective antimanic agent in both adult and pediatric patients and that it might also improve depressive symptoms and recurrences in BDI patients. Its tolerability profile is good, and its most common side effects are somnolence, light extrapyramidal symptoms, dizziness, weight gain, and oral (but reversible) hypoesthesia. Taken together, the published studies indicate that asenapine might be an effective therapeutic agent in BDI with a broad spectrum of clinical activities. Further double-blind, short- and long-term studies are, however, necessary to clarify its precise role in the treatment of BD.

KEYWORDS:

• Bipolar disorder
• pharmacological treatments
• antipsychotics
• second-generation antipsychotics
• asenapine

Article highlights

• Bipolar disorder of type I (BDI) is one of the most severe psychiatric disorders characterized by episodes of depression and mania that requires a complex pharmacological management.

• Both first-and second-antipsychotics (FGAs and SGAs, respectively) are commonly used for manic episodes. Asenapine is a novel SGA with a broader pharmacologic profile, as compared with other SGAs, encompassing not only the blockade of dopamine 2 (D2) receptors, related to reduction of positive psychotic symptoms, but also interaction with D1, D3, D4, several serotonergic, adrenergic, and histaminergic ones.

• Asenapine was approved by regulatory agencies from different continents for the treatment of manic or mixed episodes associated with BDI.

• The findings deriving from available controlled and uncontrolled trials confirm that asenapine is an effective antimanic agent, with a good tolerability profile.

• A few studies would indicate that asenapine is also effective in mixed states, in bipolar depression, and as add-on treatment to mood stabilizers.

• However, further controlled and long-term studies are necessary to better clarify, and perhaps broaden, the clinical potentials and the specificities of asenapine.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

One referee is a speaker for Allergan who make asenapine. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.

Box 1. Drug Summary Box

Additional information

Funding

This manuscript has not been funded.