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The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease

Alzheimer’s disease (AD) is a chronic disabling disease that affects the central nervous system. The main consequences of AD include the decline of cognitive functions and language disorders. One of the causes leading to AD is the decrease of neurotransmitter acetylcholine (ACh) levels in the brain,...

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Autores principales: Vecchio, Immacolata, Sorrentino, Luca, Paoletti, Annamaria, Marra, Rosario, Arbitrio, Mariamena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: SAGE Publications 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8267037/
https://www.ncbi.nlm.nih.gov/pubmed/34285627
http://dx.doi.org/10.1177/11795735211029113
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author Vecchio, Immacolata
Sorrentino, Luca
Paoletti, Annamaria
Marra, Rosario
Arbitrio, Mariamena
author_facet Vecchio, Immacolata
Sorrentino, Luca
Paoletti, Annamaria
Marra, Rosario
Arbitrio, Mariamena
author_sort Vecchio, Immacolata
collection PubMed
description Alzheimer’s disease (AD) is a chronic disabling disease that affects the central nervous system. The main consequences of AD include the decline of cognitive functions and language disorders. One of the causes leading to AD is the decrease of neurotransmitter acetylcholine (ACh) levels in the brain, in part due to a higher activity of acetylcholinesterase (AChE), the enzyme responsible for its degradation. Many acetylcholinesterase inhibitors (AChEIs), both natural and synthetic, have been developed and used through the years to counteract the progression of the disease. The first of such drugs approved for a therapeutic use was tacrine, that binds through a reversible bond to the enzyme. However, tacrine has since been withdrawn because of its adverse effects. Currently, donepezil and galantamine are very promising AChEIs with clinical benefits. Moreover, rivastigmine is considered a pseudo-irreversible compound with anti-AChE action, providing similar effects at the clinical level. The purpose of this review is to provide an overview of what has been published over the last decade on the effectiveness of AChEIs in AD, analysing the most relevant issues under the clinical and methodological profiles and the consequent possible welfare effects for the whole world. Furthermore, novel drugs and possible therapeutic approaches are also discussed.
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spelling pubmed-82670372021-07-19 The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease Vecchio, Immacolata Sorrentino, Luca Paoletti, Annamaria Marra, Rosario Arbitrio, Mariamena J Cent Nerv Syst Dis Review Alzheimer’s disease (AD) is a chronic disabling disease that affects the central nervous system. The main consequences of AD include the decline of cognitive functions and language disorders. One of the causes leading to AD is the decrease of neurotransmitter acetylcholine (ACh) levels in the brain, in part due to a higher activity of acetylcholinesterase (AChE), the enzyme responsible for its degradation. Many acetylcholinesterase inhibitors (AChEIs), both natural and synthetic, have been developed and used through the years to counteract the progression of the disease. The first of such drugs approved for a therapeutic use was tacrine, that binds through a reversible bond to the enzyme. However, tacrine has since been withdrawn because of its adverse effects. Currently, donepezil and galantamine are very promising AChEIs with clinical benefits. Moreover, rivastigmine is considered a pseudo-irreversible compound with anti-AChE action, providing similar effects at the clinical level. The purpose of this review is to provide an overview of what has been published over the last decade on the effectiveness of AChEIs in AD, analysing the most relevant issues under the clinical and methodological profiles and the consequent possible welfare effects for the whole world. Furthermore, novel drugs and possible therapeutic approaches are also discussed. SAGE Publications 2021-07-07 /pmc/articles/PMC8267037/ /pubmed/34285627 http://dx.doi.org/10.1177/11795735211029113 Text en © The Author(s) 2021 https://creativecommons.org/licenses/by-nc/4.0/This article is distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 License (https://creativecommons.org/licenses/by-nc/4.0/) which permits non-commercial use, reproduction and distribution of the work without further permission provided the original work is attributed as specified on the SAGE and Open Access page(https://us.sagepub.com/en-us/nam/open-access-at-sage).
spellingShingle Review
Vecchio, Immacolata
Sorrentino, Luca
Paoletti, Annamaria
Marra, Rosario
Arbitrio, Mariamena
The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title_full The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title_fullStr The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title_full_unstemmed The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title_short The State of The Art on Acetylcholinesterase Inhibitors in the Treatment of Alzheimer’s Disease
title_sort state of the art on acetylcholinesterase inhibitors in the treatment of alzheimer’s disease
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8267037/
https://www.ncbi.nlm.nih.gov/pubmed/34285627
http://dx.doi.org/10.1177/11795735211029113
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