Villarroya Mercedes, García Antonio G, Marco-Contelles José, López Manuela G
Universidad Autónoma de Madrid, Instituto Teófilo Hernando and Departamento de Farmacología, Facultad de Medicina, C/Arzobispo Morcillo, 4; 28029-Madrid, Spain.
Expert Opin Investig Drugs. 2007 Dec;16(12):1987-98. doi: 10.1517/13543784.16.12.1987.
Alzheimer's disease (AD) is associated with a gradual loss of attention and memory that has been related to impairment of brain cholinergic neurotransmission, particularly a deficit of cholinergic neurons. The first therapeutic target that has demonstrated therapeutic efficacy on cognition, behaviour and functional daily activities has been the inhibition of acetylcholinesterase. The acetylcholinesterase inhibitors used to treat AD patients at present are donepezil, rivastigmine and galantamine. This review summarises the current state of the art concerning the pharmacology of galantamine, focusing on the most important details of its possibilities as an acetylcholinesterase inhibitor, an allosteric potentiator of neuronal nicotinic receptors for acetylcholine, a modulator of neurotransmitter release, and an agent causing neuroprotection through an antiapoptotic action. In so doing, galantamine will be discussed in the context of the treatment of dementia, both of AD type and of mixed vascular-Alzheimer type.
阿尔茨海默病（AD）与注意力和记忆力的逐渐丧失有关，这与脑胆碱能神经传递受损有关，尤其是胆碱能神经元的缺乏。第一个已证明对认知、行为和日常功能活动具有治疗效果的治疗靶点是抑制乙酰胆碱酯酶。目前用于治疗AD患者的乙酰胆碱酯酶抑制剂有 donepezil、rivastigmine 和 galantamine。本综述总结了加兰他敏药理学的当前研究现状，重点关注其作为乙酰胆碱酯酶抑制剂、乙酰胆碱神经元烟碱受体的变构增强剂、神经递质释放调节剂以及通过抗凋亡作用发挥神经保护作用的可能性的最重要细节。在此过程中，将在AD型和血管性 - 阿尔茨海默混合型痴呆的治疗背景下讨论加兰他敏。
