Johann Wolfgang Goethe-University of Frankfurt, Deptartment of Psychiatry, Psychosomatics and Psychotherapy, Heinrich-Hoffmann-Strasse 10, Frankfurt, Germany.
Expert Opin Drug Metab Toxicol. 2010 Mar;6(3):345-54. doi: 10.1517/17425251003592137.
Alzheimer's disease (AD) is the most frequent, age-related neurodegenerative disorder and is characterized by progressive deterioration of cognition and global functioning. The relevance of the cholinergic system for memory, cognition and activities of daily life has been recognized decades ago, and research has demonstrated an early involvement and affection of central cholinergic pathways in the course of AD.
Here, we review a body of placebo-controlled studies as well as meta-analyses on the cholinesterase (ChE) inhibitor galantamine, one of only four drugs currently approved for anti-dementia therapy in AD.
The scope of this article is to concisely review the rationale of cholinergic treatment in AD, the chemistry and pharmacology of galantamine and to give a detailed overview of its clinical efficacy, safety, tolerability and potential usability for indications beyond AD.
Galantamine can improve and stabilize cognitive performance, activities of daily living and behavioral symptoms over the course of 6 months and its efficacy and tolerability are comparable with those of other ChE inhibitors (rivastigmine and donepezil). As long as no other drug therapies with comparable or better clinical efficacy emerge, galantamine will remain one of the standard first-line medications for mild-to-moderate AD.
阿尔茨海默病(AD)是最常见的、与年龄相关的神经退行性疾病,其特征是认知和整体功能的进行性恶化。几十年来,人们已经认识到胆碱能系统对记忆、认知和日常生活活动的重要性,研究表明,在 AD 的发展过程中,中枢胆碱能通路很早就会受到影响。
在这里,我们回顾了一系列安慰剂对照研究以及荟萃分析,这些研究的对象是胆碱酯酶(ChE)抑制剂加兰他敏,它是目前仅有的四种被批准用于 AD 抗痴呆治疗的药物之一。
本文的范围是简要回顾 AD 中胆碱能治疗的原理、加兰他敏的化学和药理学,并详细概述其在 6 个月内的临床疗效、安全性、耐受性以及在 AD 以外适应症的潜在可用性。
加兰他敏可以改善和稳定认知表现、日常生活活动和行为症状,其疗效和耐受性可与其他 ChE 抑制剂(利伐斯的明和多奈哌齐)相媲美。只要没有出现其他具有类似或更好临床疗效的药物治疗方法,加兰他敏仍将是轻度至中度 AD 的标准一线药物之一。