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The role of citicoline in cognitive impairment: pharmacological characteristics, possible advantages, and doubts for an old drug with new perspectives

Authors Gareri P, Castagna A, Cotroneo AM, Putignano S, De Sarro G, Bruni AC

Received 4 May 2015

Accepted for publication 1 July 2015

Published 3 September 2015 Volume 2015:10 Pages 1421—1429

DOI https://doi.org/10.2147/CIA.S87886

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Richard Walker

Pietro Gareri,1 Alberto Castagna,1 Antonino Maria Cotroneo,2 Salvatore Putignano,3 Giovambattista De Sarro,4 Amalia Cecilia Bruni1

1
Centro Regionale di Neurogenetica, ASP Catanzaro, Lamezia Terme, Catanzaro, 2ASL2 Turin, Turin, 3Elderly Assistance Unit, Naples, 4Department of Health Sciences, School of Medicine, University Magna Græcia of Catanzaro, Catanzaro, Italy

Background: Citicoline is able to potentiate neuroplasticity and is a natural precursor of phospholipid synthesis, or rather serves as a choline source in the metabolic pathways for biosynthesis of acetylcholine. Several studies have shown that it can have beneficial effects both in degenerative and in vascular cognitive decline. The aim of the present study was to review the pharmacokinetics and pharmacodynamics of this drug and its role in cognitive impairment according to the present medical literature.
Methods: A MEDLINE® search was made using the following key words: citicoline, pharmacokinetics, pharmacodynamics, elderly, cognitive impairment, vascular dementia, and Alzheimer’s disease. Recent studies on the possible role of citicoline in increasing sirtuin 1 (SIRT1) expression were assessed. Some personal studies were also considered, such as the VITA study and the IDEALE study.
Results: Administered by both oral and intravenous routes, citicoline is converted into two major circulating metabolites, cytidine and choline. It is metabolized in the gut wall and liver. Pharmacokinetic studies suggested that it is well absorbed and highly bioavailable with oral dosing. A number of studies have clearly shown the possible role of citicoline in cognitive impairment of diverse etiology. It can also modulate the activity/expression of some protein kinases involved in neuronal death and increases SIRT1 expression in the central nervous system. The VITA study and the IDEALE study suggested that both parenteral and oral citicoline are effective and safe. Other studies have clearly demonstrated citicoline’s effects on several cognitive domains. Conversely, some studies did not point out any evidence of efficacy of this drug.
Conclusion: Citicoline appears to be a promising agent to improve cognitive impairment, especially of vascular origin. In fact, so far it appears as a drug with the ability to promote “safe” neuroprotection, capable of enhancing endogenous protective. Large clinical trials are needed to confirm its benefits.

Keywords: citicoline, cognitive impairment, elderly, neurodegeneration, neuroprotective effects, sirtuins

Corrigendum for this paper has been published

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