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艾地苯醌。对其药效学和药代动力学特性以及在年龄相关性认知障碍中的治疗应用的综述。

Idebenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in age-related cognitive disorders.

作者信息

Gillis J C, Benefield P, McTavish D

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1994 Aug;5(2):133-52. doi: 10.2165/00002512-199405020-00007.

Abstract

Idebenone is a benzoquinone compound which has been investigated in elderly patients with dementia. Its precise mechanism(s) of action remains unknown, but in vitro and in vivo studies suggest the drug may diminish nerve cell damage due to ischaemia, correct neurotransmitter defects and/or cerebral metabolism and facilitate memory and learning. In the small number of studies available for evaluation, idebenone was generally superior to placebo and comparable with bifemelane, oxiracetam and nebracetam on the basis of a number of objective and subjective tests and rating scales in patients with mild to moderate cognitive decline. Clinical trial results indicate that patients with mild dementia seem more likely to respond than those with greater functional decline. The degree of benefit conferred by idebenone is often difficult to determine, but in those who respond, improvement is generally mild to moderate. Therapy with idebenone appears well tolerated for up to 2 years, and no changes in vital signs or laboratory values have been seen in clinical trials. In view of the lack of a proven agent to limit or halt the progression of dementia in the elderly, idebenone may warrant consideration in patients with mild cognitive dysfunction on the basis of preliminary evidence of predominantly mild improvement of functional status in some patients and good tolerability. However, further well designed studies, including comparisons with newer and commonly used agents, such as tacrine, are required to better define the role of idebenone in this complex area of treatment.

摘要

艾地苯醌是一种苯醌化合物,已在老年痴呆患者中进行了研究。其确切的作用机制尚不清楚,但体外和体内研究表明,该药物可能减少缺血引起的神经细胞损伤,纠正神经递质缺陷和/或脑代谢,并促进记忆和学习。在少数可供评估的研究中,根据多项客观和主观测试以及评分量表,在轻度至中度认知衰退患者中,艾地苯醌总体上优于安慰剂,且与比呋内酰胺、奥拉西坦和奈非西坦相当。临床试验结果表明,轻度痴呆患者似乎比功能衰退更严重的患者更有可能产生反应。艾地苯醌所带来的益处程度往往难以确定,但在有反应的患者中,改善通常为轻度至中度。艾地苯醌治疗长达2年似乎耐受性良好,临床试验中未观察到生命体征或实验室值的变化。鉴于缺乏已证实的可限制或阻止老年人痴呆进展的药物,基于一些患者功能状态主要有轻度改善的初步证据以及良好的耐受性,艾地苯醌可能值得轻度认知功能障碍患者考虑。然而,需要进一步设计良好的研究,包括与新的常用药物(如他克林)进行比较,以更好地确定艾地苯醌在这一复杂治疗领域中的作用。

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