Robinson Dean M, Keating Gillian M
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2006;66(11):1515-34. doi: 10.2165/00003495-200666110-00015.
Memantine (Ebixa, Axura, Namenda, Akatinol) is a moderate-affinity, uncompetitive, voltage-dependent, NMDA-receptor antagonist with fast on/off kinetics that inhibits excessive calcium influx induced by chronic overstimulation of the NMDA receptor. Memantine is approved in the US and the EU for the treatment of patients with moderate to severe dementia of the Alzheimer's type. In well designed clinical trials, oral memantine, as monotherapy or in addition to a stable dose of acetylcholinesterase inhibitors, was well tolerated during the treatment of mild to severe Alzheimer's disease for up to 52 weeks. Memantine generally modified the progressive symptomatic decline in global status, cognition, function and behaviour exhibited by patients with moderate to severe Alzheimer's disease in four 12- to 28-week trials. In patients with mild to moderate Alzheimer's disease, data from three 24-week trials are equivocal, although meta-analyses indicate beneficial effects on global status and cognition. Memantine is an effective pharmacotherapeutic agent, and currently the only approved option, for the treatment of moderate to severe Alzheimer's disease.
美金刚(易倍申、Axura、Namenda、Akatinol)是一种具有中等亲和力、非竞争性、电压依赖性的N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,其开关动力学迅速,可抑制NMDA受体长期过度刺激所诱导的过量钙内流。美金刚在美国和欧盟被批准用于治疗中度至重度阿尔茨海默病类型的痴呆患者。在精心设计的临床试验中,口服美金刚作为单一疗法或与稳定剂量的乙酰胆碱酯酶抑制剂联合使用时,在治疗轻度至重度阿尔茨海默病长达52周的过程中耐受性良好。在四项为期12至28周的试验中,美金刚总体上改善了中度至重度阿尔茨海默病患者在整体状况、认知、功能和行为方面逐渐出现的症状性衰退。在轻度至中度阿尔茨海默病患者中,三项为期24周试验的数据并不明确,尽管荟萃分析表明其对整体状况和认知有有益影响。美金刚是治疗中度至重度阿尔茨海默病的一种有效药物治疗剂,且是目前唯一被批准的选择。