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Transdermal Asenapine in Schizophrenia: A Systematic Review
Brennan Carrithers1, Rif S El-Mallakh1
1Department of Psychiatry and Behavioral Sciences, University of Louisville School of Medicine, Louisville, Kentucky 40202, USA.
Transdermal asenapine, approved for schizophrenia, offers a novel delivery method for this antipsychotic. Clinical trials show it is superior to placebo in treating acute psychosis, with a number needed to treat of 9.
Area of Science:
- Pharmacology
- Psychiatry
- Drug Delivery Systems
Background:
- Asenapine is an antipsychotic effective for schizophrenia and bipolar mania.
- Sublingual administration is necessary due to high first-pass liver metabolism.
- A transdermal formulation has recently gained FDA approval for schizophrenia.
Purpose of the Study:
- To systematically review the transdermal formulation of asenapine.
- To evaluate its pharmacokinetic properties and receptor binding profile.
- To assess its efficacy in treating acute psychosis in schizophrenia.
Main Methods:
- Systematic review conducted using the PRISMA model.
- Analysis of pharmacokinetic data including bioavailability, Cmax, Tmax, and half-life.
- Review of a randomized, placebo-controlled study for efficacy assessment.
Main Results:
- Secuado® is the only approved transdermal formulation with 35% bioavailability.
- Asenapine exhibits a unique receptor antagonist profile with high affinity for multiple receptors.
- The transdermal formulation demonstrated superiority over placebo in a schizophrenia psychosis study (NNT=9).
Conclusions:
- Transdermal asenapine, specifically Secuado®, provides an alternative administration route.
- Its receptor profile suggests potential off-label uses for bipolar depression, anxiety, and aggression.
- The efficacy in acute schizophrenia psychosis is supported by clinical trial data.
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