Effectiveness of nootropic drugs with cholinergic activity in treatment of cognitive deficit: a review

Abstract

Nootropics represent probably the first “smart drugs” used for the treatment of cognitive deficits. The aim of this paper is to verify, by a systematic analysis of the literature, the effectiveness of nootropics in this indication. The analysis was limited to nootropics with cholinergic activity, in view of the role played by acetylcholine in learning and memory. Acetylcholine was the first neurotransmitter identified in the history of neuroscience and is the main neurotransmitter of the peripheral, autonomic, and enteric nervous systems. We conducted a systematic review of the literature for the 5-year period 2006–2011. From the data reported in the literature, it emerges that nootropics may be an effective alternative for strengthening and enhancing cognitive performance in patients with a range of pathologies. Although nootropics, and specifically the cholinergic precursors, already have a long history behind them, according to recent renewal of interest, they still seem to have a significant therapeutic role. Drugs with regulatory indications for symptomatic treatment of Alzheimer’s disease, such as cholinesterase inhibitors and memantine, often have transient effects in dementia disorders. Nootropics with a cholinergic profile and documented clinical effectiveness in combination with cognate drugs such as cholinesterase inhibitors or alone in patients who are not suitable for these inhibitors should be taken into account and evaluated further.

The Nootropic Drug Α-Glyceryl-Phosphoryl-Ethanolamine Exerts Neuroprotective Effects in Human Hippocampal Cells

“…Furthermore, GPE significantly enriched Ach content, in a concentration dependent manner, supporting the nootropic properties of the compound. To note, improved learning and memory has been widely associated with an enhancement in cholinergic neurotransmission in the hippocampus [14,[26][27][28]. Our data suggested an augmentation of Ach that could be beneficial for memory consolidation in neurons.…”

“…In particular, reduced levels of PC and/or PUFAs in brain cells have been associated to a decrease in membrane excitability and neurotransmitter release [4,5] that lead to insufficient synaptic transmission and finally to memory impairment. Consistently, the administration of drugs able to restore membrane composition and functionality can ameliorate memory performances [14]. Among these compounds, GPE has emerged in preserving the well-being of astrocytes and neural stem cells [1,4,[15][16][17].…”

“…In this respect, explicit memory has been demonstrated to be enhanced by phosphatidylcholine (PC) administration via the release of choline [1,13] which is a constituent of the cellular membrane and an acetylcholine (Ach) precursor [1]. In particular, the Ach precursor, choline alfoscerate, and the PC biosynthesis intermediary, citicoline, have been proven to enhance memory and cognitive function in humans and even in Alzheimer's patients [14]. Finally, lifespan of yeast and human-derived cell cultures has been prolonged by phosphatidylethanolamine (PE) and its precursor ethanolamine [1,15].…”

Syndrome of High Academic Loads in School-Aged Children and Adolescents

“…Являясь источником холина и фосфолипидов, лецитин принимает участие в синтезе ацетилхолина, строении нейрональных мембран и миелина. Исследователи выдвигают гипотезы и предполагают, что лецитин улучшает когнитивные функции [59,60]. Доклинические исследования показали, что лецитин достоверно повышает уровень важного для когнитивных функций нейромедиатора ацетихолина [61].…”

The many faces of vascular cognitive impairment

“…This was followed by a series of cerebral circulation enhancers with primarily vasodilating action. Unfortunately, these drugs were quite inefficient and led to a period of neurocentric research with the discovery of nootropic substances, which showed a certain level of efficacy to slow cognitive decline in vascular dementia (Colucci et al 2012). Animal models and brain imaging techniques allowed the discovery of several risk factors and mechanisms involved in the development of vascular cognitive impairment.…”