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Transdermal Asenapine in Schizophrenia: A Systematic Review

Authors Carrithers B, El-Mallakh RS

Received 20 May 2020

Accepted for publication 26 June 2020

Published 25 August 2020 Volume 2020:14 Pages 1541—1551

DOI https://doi.org/10.2147/PPA.S235104

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Johnny Chen


Brennan Carrithers, Rif S El-Mallakh

Department of Psychiatry and Behavioral Sciences, University of Louisville School of Medicine, Louisville, Kentucky 40202, USA

Correspondence: Rif S El-Mallakh
Department of Psychiatry and Behavioral Sciences, University of Louisville School of Medicine, 401 East Chestnut Street, Suite 610, Louisville, Kentucky 40202, USA
Tel +1 502 588 – 4450
Fax +1 502 588 - 9539
Email rselma01@louisville.edu

Background: Asenapine is a novel antipsychotic that has demonstrated efficacy in controlling psychosis in schizophrenia and mania in bipolar illness. It must be administered as a sublingual formulation because it is nearly completely metabolized in the first pass through the liver. Recently, a transdermal formulation of asenapine has been approved for schizophrenia by the Food and Drug Administration.
Methods: A systematic review of transdermal asenapine was done utilizing the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) model.
Discussion: There are several formulations of transdermal asenapine but only Secuado® has been approved for clinical use. Total bioavailability is 35%. Peak plasma concentration (Cmax) is 4 ng/mL and occurs within 1 hr (Tmax); elimination half-life (t1/2) is 24 hrs (range 13.4 to 39.2 h). Asenapine is highly bound (95%) to albumin and α1-acid glycoprotein. It has a unique receptor profile in which it functions as an antagonist at multiple receptors with affinity that is higher than D2 (Ki = 1.3) including D3, D4, 5HT2A, 5HT2C, 5HT2B, 5HT7, 5HT6, H1, and α 2. This profile suggests that asenapine may be of particular value off label for bipolar depression, anxiety, and aggression. Transdermal asenapine was only tested in one randomized, placebo-controlled study of acute psychosis in schizophrenia. It was superior to placebo at week 6 with nearly one-third of patients experiencing > 30% improvement in total PANSS score which translates in a number needed to treat (NNT) of 9.

Keywords: asenapine, schizophrenia, transdermal, topical, antipsychotic

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