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阿尼西坦。其药效学和药代动力学特性概述,以及其在老年认知障碍治疗潜力的综述。

Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders.

作者信息

Lee C R, Benfield P

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1994 Mar;4(3):257-73. doi: 10.2165/00002512-199404030-00007.

DOI:10.2165/00002512-199404030-00007
PMID:8199398
Abstract

Aniracetam is a member of the nootropic class of drugs, which have possible cognition enhancing effects. It appears to positively modulate metabotropic glutamate receptors and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-sensitive glutamate receptors, and may facilitate cholinergic transmission, effects which are possibly related to its mechanism of action. Results from trials in elderly patients with mild to moderate cognitive impairment due to senile dementia of the Alzheimer type suggest that aniracetam may be of benefit, with further trials required to confirm its efficacy profile and to define more precisely those patients most likely to respond to treatment. Aniracetam 1500 mg/day was significantly more effective than placebo in all tests at 4 and 6 months, and in a further 6-month trial was more effective than piracetam 2400 mg/day in 8 of 18 tests. Preliminary evidence in the treatment of patients with cognitive impairment of cerebrovascular origin suggests aniracetam may also be of benefit in this condition. Whilst incidence rates of adverse effects are not yet available, data from trials suggest aniracetam is well tolerated. In particular, aniracetam does not appear to cause increases in liver enzyme levels. The evaluation of drugs for patients with senile cognitive disorders is a difficult area and therapeutic options are currently limited. Preliminary evidence of the potential benefits and good tolerability profile of aniracetam support continued evaluation of its use in patients with mild to moderate senile dementia of the Alzheimer type.

摘要

阿尼西坦是促智药类药物的一种,这类药物可能具有增强认知的作用。它似乎能正向调节代谢型谷氨酸受体和α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)敏感的谷氨酸受体,并可能促进胆碱能传递,这些作用可能与其作用机制有关。对患有阿尔茨海默型老年性痴呆导致的轻度至中度认知障碍的老年患者进行的试验结果表明,阿尼西坦可能有益,但需要进一步试验来确认其疗效特征,并更精确地确定最可能对治疗有反应的患者。在4个月和6个月时,阿尼西坦1500毫克/天在所有测试中均显著优于安慰剂,在另一项为期6个月的试验中,在18项测试中的8项中,其效果优于2400毫克/天的吡拉西坦。对脑血管源性认知障碍患者进行治疗的初步证据表明,阿尼西坦在这种情况下可能也有益。虽然不良反应的发生率尚无数据,但试验数据表明阿尼西坦耐受性良好。特别是,阿尼西坦似乎不会导致肝酶水平升高。对老年认知障碍患者的药物评估是一个困难的领域,目前治疗选择有限。阿尼西坦潜在益处和良好耐受性的初步证据支持继续评估其在患有轻度至中度阿尔茨海默型老年性痴呆患者中的应用。

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Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study.阿尼西坦单药或联合胆碱酯酶抑制剂治疗认知障碍患者的临床疗效:一项比较开放研究。
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Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors.吡拉西坦定义了一个新的变构调节剂结合位点,用于调节α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体。
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[A test model for cerebrally-active drugs as demonstrated by the example of the new substance aniracetam].[以新物质阿尼西坦为例的脑活性药物测试模型]
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