加兰他敏在阿尔茨海默病中的应用综述。

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Scott LJ, Goa KL报道

加兰他敏在阿尔茨海默病中的应用综述。

药品。2000年11月;60(5):1095-122。

PubMed ID

11129124 (PubMed视图

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摘要

目前，乙酰胆碱酯酶(AChE)抑制剂是治疗阿尔茨海默病(AD)最有前途的一类药物。加兰他敏是一种可逆的、竞争性的三级生物碱AChE抑制剂。该药对乙酰胆碱酯酶而不是丁酰胆碱酯酶有选择性。除了抑制AChE外，加兰他敏还与烟碱乙酰胆碱受体发生变构相互作用，增强激动剂对这些受体的作用。在设计良好、持续3 - 6个月的大型试验(n = 285 - 978例轻度至中度AD患者)中，16或24 mg/天加兰他敏的接受者相对于安慰剂接受者在认知和整体症状方面取得了显著改善。加兰他敏还改善了这些患者的日常生活活动，并显著降低了日常生活活动对护理人员协助的需求。此外，加兰他敏接受者在行为症状方面比安慰剂接受者取得了显著更好的结果。在一项长期研究(12个月)中，加兰他敏24毫克/天减缓了疾病症状的进展，并维持了轻度至中度AD患者的认知功能和日常生活活动。加兰他敏通常耐受性良好，大多数不良事件的强度为轻度至中度和短暂性。可以预见，不良事件本质上是胆碱能性的，通常与胃肠系统有关。 These effects were reduced in patients receiving the recommended dose escalation regimen. Galantamine had no clinically relevant effects on vital signs, haematological or biochemical laboratory parameters and, importantly, there were no reports of hepatotoxicity. The incidence of serious adverse events was similar between galantamine (8 to 32 mg/day) and placebo groups (6 to 16% of patients across all treatment groups). CONCLUSIONS: Galantamine is an effective well tolerated symptomatic treatment for AD which improves cognition, function and activities of daily living in the short term (up to 6 months) in patients with mild to moderate AD. In addition, it delays the development of behavioural disturbances and psychiatric symptoms, and reduces caregiver burden (as measured by caregiver time). In the long term (up to 1 year), galantamine maintains cognition and activities of daily living. Adverse events associated with galantamine are mainly cholinergic, usually mild to moderate in intensity and transient. Galantamine has been evaluated in several large well-designed studies and, given the relative lack of established treatment options, it may be considered as one of the first-line pharmacological treatments in patients with mild to moderate AD.

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