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Transdermal donepezil on the treatment of Alzheimer's disease

Authors PIERA S, Cerasa, MARINELLI L, Di Stefano A

Received 18 June 2012

Accepted for publication 27 July 2012

Published 20 August 2012 Volume 2012:8 Pages 361—368

DOI https://doi.org/10.2147/NDT.S16089

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2


Piera Sozio, Laura S Cerasa, Lisa Marinelli, Antonio Di Stefano

Department of Pharmacy, University of "G. d'Annunzio," Vai dei Vestini, Chieti, Italy

Abstract: Alzheimer's disease (AD) is the most common type of senile dementia, characterized by cognitive deficits related to degeneration of cholinergic neurons. The first anti-Alzheimer drugs approved by the Food and Drug Administration were the cholinesterase inhibitors (ChEIs), which are capable of improving cholinergic neurotransmission by inhibiting acetylcholinesterase. The most common ChEIs used to treat cognitive symptoms in mild to moderate AD are rivastigmine, galantamine, and donepezil. In particular, the lattermost drug has been widely used to treat AD patients worldwide because it is significantly less hepatotoxic and better tolerated than its predecessor, tetrahydroaminoacridine. It also demonstrates high selectivity towards acetylcholinesterase inhibition and has a long duration of action. The formulations available for donepezil are immediate release (5 or 10 mg), sustained release (23 mg), and orally disintegrating (5 or 10 mg) tablets, all of which are intended for oral-route administration. Since the oral donepezil therapy is associated with adverse events in the gastrointestinal system and in plasma fluctuations, an alternative route of administration, such as the transdermal one, has been recently attempted. The goal of this paper is to provide a critical overview of AD therapy with donepezil, focusing particularly on the advantages of the transdermal over the oral route of administration.

Keywords: Alzheimer's disease, donepezil, transdermal, patch

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