University of Southampton, Memory Assessment and Research Centre, Moorgreen Hospital, Southampton, SO30 3JB, UK.
Expert Rev Neurother. 2001 Nov;1(2):153-9. doi: 10.1586/14737175.1.2.153.
Galantamine (Reminyl) is a tertiary alkaloid, originally isolated from the Caucasian snowdrop and several Amaryllidaceae plants. It has been used for over 40 years in anesthetics to reverse the effects of curarization. In vitro and in vivo studies have confirmed that galantamine is an orally-active, reversible, competitive inhibitor of brain cholinesterase, which is 50 times more selective for acetylcholinesterase, compared with butyrylcholinesterase. Galantamine has also been shown to allosterically potentiate sub-maximal nicotinic responses to acetylcholine. This direct effect on pre- and postsynaptic nicotinic receptors may represent a second mechanism of action for enhancing cholinergic function, but as yet it is unclear as to whether that has any clinical significance. Galantamine has been licensed for use in the symptomatic treatment of Alzheimer's disease patients, after proving its efficacy in a number of well-designed clinical trials. It has to be administered twice daily and has shown good tolerability, which typically for drugs of this class, is improved by slow titration. The most common side effects are: nausea, vomiting, diarrhea and anorexia. Galantamine appears to be an effective treatment for Alzheimer's disease comparable with the other acetylcholinesterase inhibitors in improving cognition and function with growing evidence for its effects on behavior and caregiver burden.
加兰他敏(Reminyl)是一种 tertiary 生物碱,最初从高加索雪花莲和几种石蒜科植物中分离出来。它已在麻醉中使用超过 40 年,以逆转箭毒的作用。体外和体内研究证实,加兰他敏是一种口服、可逆、竞争性的脑乙酰胆碱酯酶抑制剂,与丁酰胆碱酯酶相比,对乙酰胆碱酯酶的选择性高 50 倍。加兰他敏还被证明可以变构增强乙酰胆碱对烟碱受体的亚最大反应。这种对前突触和后突触烟碱受体的直接作用可能代表增强胆碱能功能的第二种作用机制,但目前尚不清楚这是否具有任何临床意义。加兰他敏已被许可用于治疗阿尔茨海默病患者的症状,因为它在多项精心设计的临床试验中证明了其疗效。它必须每天服用两次,并且表现出良好的耐受性,这对于此类药物来说通常通过缓慢滴定来改善。最常见的副作用是:恶心、呕吐、腹泻和厌食。加兰他敏似乎是一种有效的阿尔茨海默病治疗药物,与其他乙酰胆碱酯酶抑制剂一样,可改善认知和功能,并且其对行为和护理人员负担的影响也越来越多。