Tanović A, Alfaro V
Facultat de Biologia, Universitat de Barcelona, Avda. Diagonal 645, E-08028 Barcelona, Spain.
Rev Neurol. 2006;42(10):607-16.
To review the therapeutic efficacy of memantine, an uncompetitive antagonist of N-methyl-D-aspartate (NMDA)-glutamate receptor.
Alzheimer's disease (AD) is the most common neurodegenerative disorder and cause of dementia with ageing worldwide. The main AD symptoms are a gradual loss of cognitive function and a functional impairment. Glutamatergic excitatory neurotransmission, an important process in learning and memory, is severely disrupted in AD, probably due to the oxidative stress associated with the beta-amyloid peptide (1-42) increase. The glutamate-related excitotoxicity, mainly mediated by NMDA subtype of the glutamate receptors, is a common clue of pathogenesis for neurodegenerative disorders.
Memantine, a moderate-affinity, voltage-dependent, uncompetitive antagonist of NMDA receptor, shows neuroprotective effects in patients with moderate-to-severe AD. Memantine is a drug with neuroprotective and cognition-enhanced properties, which can be combined with other treatments for AD. Thus, memantine does not stop or reverse AD, but its moderating effect in protecting the brain from the toxic levels of calcium, allows normal signaling among brain neurons. The efficacy and safety profile of memantine have been reported in several clinical trials for treatment of AD and vascular dementia.
回顾美金刚（一种N-甲基-D-天冬氨酸（NMDA）-谷氨酸受体非竞争性拮抗剂）的治疗效果。
阿尔茨海默病（AD）是全球范围内最常见的神经退行性疾病及老年痴呆的病因。AD的主要症状是认知功能逐渐丧失和功能障碍。谷氨酸能兴奋性神经传递是学习和记忆中的一个重要过程，在AD中受到严重破坏，可能是由于与β-淀粉样肽（1-42）增加相关的氧化应激。主要由谷氨酸受体的NMDA亚型介导的谷氨酸相关兴奋性毒性是神经退行性疾病发病机制的一个常见线索。
美金刚是一种NMDA受体的中等亲和力、电压依赖性、非竞争性拮抗剂，对中重度AD患者具有神经保护作用。美金刚是一种具有神经保护和认知增强特性的药物，可与AD的其他治疗方法联合使用。因此，美金刚并不能阻止或逆转AD，但它在保护大脑免受钙毒性水平影响方面的调节作用，使大脑神经元之间能够进行正常信号传递。美金刚的疗效和安全性已在多项治疗AD和血管性痴呆的临床试验中得到报道。
