Stahl S M
Clinical Neuroscience Research Center in San Diego and the Department of Psychiatry at the University of California San Diego, USA.
J Clin Psychiatry. 2000 Oct;61(10):710-1. doi: 10.4088/jcp.v61n1001.
Three new cholinesterase inhibitors, donepezil, rivastigmine, and galantamine, all inhibit the enzyme AChE. Rivastigmine also inhibits BuChE, which could lead to additional benefits in late-stage Alzheimer's disease, but also cause more GI side effects at initiation of therapy. Galantamine is also an allosteric modulator of nicotinic receptors, which could lead to additional efficacy for attention and for behaviors mediated by neurotransmitters other than ACh. We are now entering an exciting era where the options for treating the devastating illness Alzheimer's disease are multiplying and creating a foundation upon which new therapies with new mechanisms of action can be built.
三种新型胆碱酯酶抑制剂,多奈哌齐、卡巴拉汀和加兰他敏,均能抑制乙酰胆碱酯酶(AChE)。卡巴拉汀还能抑制丁酰胆碱酯酶(BuChE),这可能在晚期阿尔茨海默病中带来额外益处,但在治疗开始时也会引发更多胃肠道副作用。加兰他敏还是烟碱受体的变构调节剂,这可能在注意力以及由乙酰胆碱以外的神经递质介导的行为方面带来额外疗效。我们现在正进入一个令人兴奋的时代,治疗毁灭性疾病阿尔茨海默病的选择正在增多,并为基于新作用机制的新疗法奠定基础。