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
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
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
This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.Download Article [PDF] View Full Text [HTML][Machine readable]