Centro Ricerche Cliniche, Telemedicina e Telefarmacia Università di Camerino, Via Madonna delle Carceri 9, 62032 Camerino (MC) Italy.
Curr Alzheimer Res. 2013 Dec;10(10):1070-9. doi: 10.2174/15672050113106660173.
Cholinergic precursors have represented the first approach to counter cognitive impairment occurring in adultonset dementia disorders. These compounds were early leaved because their clinical efficacy was not clearly demonstrated. This is probably not true for some choline-containing phospholipids including choline alphoscerate. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. An ongoing trial indicates that association between the acetylcholinesterase inhibitor donepezil and choline alphoscerate is accompanied by an improvement in several cognitive tests superior to that induced by donepezil alone. It is suggested that this association may represent a therapeutic option to prolong beneficial effects of cholinergic therapies in Alzheimer's disease patients with concomitant ischemic cerebrovascular disorders. In summary, choline alphoscerate has significant effects on cognitive function with a good safety profile and tolerability. Although limited both in terms of size of the samples investigated and of the length of treatment, preclinical and clinical results presented suggest that cognitive enhancing capabilities of choline alphoscerate merit of being further investigated in appropriate trials.
胆碱能前体代表了治疗成年发病的痴呆障碍认知障碍的第一种方法。这些化合物很早就被淘汰了,因为它们的临床疗效没有得到明确证明。但对于一些含有胆碱的磷脂,包括胆碱磷酸酯,情况可能并非如此。胆碱磷酸酯可增加大鼠海马乙酰胆碱的释放,促进实验动物的学习和记忆,改善大脑转导机制,并减少与学习和记忆相关的大鼠脑区的年龄相关结构变化。该化合物在胆碱能神经传递改变和脑血管损伤的模型中发挥神经保护作用。在临床研究中,胆碱磷酸酯改善了痴呆症患者的记忆和注意力障碍以及情感和躯体症状。一项正在进行的试验表明,乙酰胆碱酯酶抑制剂多奈哌齐与胆碱磷酸酯的联合使用可改善多种认知测试,优于单独使用多奈哌齐的效果。有人认为,这种联合治疗可能是一种治疗选择,可以延长伴有缺血性脑血管疾病的阿尔茨海默病患者的胆碱能治疗的有益效果。总之,胆碱磷酸酯对认知功能有显著影响,具有良好的安全性和耐受性。尽管在研究样本量和治疗时间方面都存在局限性,但目前的临床前和临床结果表明,胆碱磷酸酯的认知增强能力值得在适当的试验中进一步研究。