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加兰他敏,一种变构调节烟碱受体的胆碱酯酶抑制剂:对阿尔茨海默病病程的影响。

Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease.

作者信息

Coyle J, Kershaw P

机构信息

Harvard Department of Psychiatry, Belmont, Massacusetts, USA.

出版信息

Biol Psychiatry. 2001 Feb 1;49(3):289-99. doi: 10.1016/s0006-3223(00)01101-x.

DOI:10.1016/s0006-3223(00)01101-x
PMID:11230880
Abstract

Despite the proven efficacy of acetylcholinesterase inhibitors in Alzheimer's disease, there is a need for new and more effective treatments. Galantamine is a novel treatment for Alzheimer's disease that inhibits acetylcholinesterase and modulates nicotinic receptors. In randomized, double-blind, placebo-controlled studies of up to 6 months duration, galantamine significantly improved cognitive function. Galantamine also had beneficial effects on instrumental and basic activities of daily living, and postponed the progression of behavioral symptoms. Patients who completed one of the 6-month, placebo-controlled studies were eligible to enter a 6-month, open-extension study of the 24-mg/day dose of galantamine. At the end of 12 months, cognitive function and activities of daily living were preserved in those patients who had been treated throughout the study with galantamine 24 mg/day. At 12 months, this group of patients had significantly better cognitive functions than patients who had been treated with a placebo for 6 months before receiving galantamine. These studies indicate that galantamine postpones the progression of symptoms in Alzheimer's disease. Since galantamine shows the greatest benefits when treatment is started early, its long-term benefits may result from an effect on the underlying disease process; such an effect might be mediated by galantamine's concomitant action on nicotinic receptors.

摘要

尽管乙酰胆碱酯酶抑制剂在阿尔茨海默病中的疗效已得到证实,但仍需要新的、更有效的治疗方法。加兰他敏是一种用于治疗阿尔茨海默病的新型药物,它能抑制乙酰胆碱酯酶并调节烟碱样受体。在长达6个月的随机、双盲、安慰剂对照研究中,加兰他敏显著改善了认知功能。加兰他敏对日常生活的工具性和基本活动也有有益影响,并延缓了行为症状的进展。完成其中一项为期6个月的安慰剂对照研究的患者有资格进入一项为期6个月、剂量为24毫克/天的加兰他敏开放扩展研究。在12个月结束时,在整个研究过程中接受24毫克/天加兰他敏治疗的患者的认知功能和日常生活活动得以保留。在12个月时,这组患者的认知功能明显优于在接受加兰他敏治疗前曾接受6个月安慰剂治疗的患者。这些研究表明,加兰他敏可延缓阿尔茨海默病症状的进展。由于加兰他敏在早期开始治疗时显示出最大的益处,其长期益处可能源于对潜在疾病进程的影响;这种影响可能是由加兰他敏对烟碱样受体的协同作用介导的。

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Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease.加兰他敏,一种变构调节烟碱受体的胆碱酯酶抑制剂:对阿尔茨海默病病程的影响。
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Galantamine: a randomized, double-blind, dose comparison in patients with Alzheimer's disease.加兰他敏:一项针对阿尔茨海默病患者的随机、双盲、剂量比较研究。
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Drugs. 2000 Nov;60(5):1095-122. doi: 10.2165/00003495-200060050-00008.

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