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[美金刚:从原研药到仿制药]

[Memantine: from the original brand to generics].

作者信息

Titova N V

机构信息

Pirogov Russian National Research Medical University, Moscow, Russia.

出版信息

Zh Nevrol Psikhiatr Im S S Korsakova. 2017;117(10):136-143. doi: 10.17116/jnevro2017117101136-143.

Abstract

Memantine is the first clinically available glutamate antagonist, with an antagonist action at the N-methyl-D-aspartate receptors in the brain, for correction of cognitive and behavioral functions in neurodegenerative disorders. Glutamate mediated excitotoxic neuronal damage has been implicated in Alzheimer's disease (AD) and other parkinsonism-related dementias and, therefore, memantine represents a novel mode of action to counteract the glutamate-mediated excitotoxicity. In moderate to severe AD, 20 mg of memantine shows a positive effect on cognition, mood, behavior and the ability to perform activities of daily living. Long-term studies show good tolerability of memantine with an acceptable side-effect profile. In recent years, there have been a proliferation of a number of companies producing generic memantine with different trade names. In Russia, the first memantine generic drug noojerone was approved in 2010 and its use has since been supported by a growing evidence base of efficacy in real-life clinical practice. Postmarketing studies show that noojerone provides long-term and effective therapy in patients with moderate and severe Alzheimer's dementia. This observation is supported by the clinically significant therapeutic effect of noojerone on cognitive and daily functioning, behavioral and psychotic symptoms of dementia and a reduction of the burden on caregivers. This generic version of memantine is affordable and, therefore, reduces financial burden on patients and improves compliance with treatment.

摘要

美金刚是首个可临床使用的谷氨酸拮抗剂,它作用于大脑中的N-甲基-D-天冬氨酸受体,用于纠正神经退行性疾病中的认知和行为功能。谷氨酸介导的兴奋性毒性神经元损伤与阿尔茨海默病(AD)及其他帕金森病相关痴呆有关,因此,美金刚代表了一种对抗谷氨酸介导的兴奋性毒性的新作用方式。在中度至重度AD中,20毫克美金刚对认知、情绪、行为及日常生活活动能力均有积极作用。长期研究表明美金刚耐受性良好,副作用可接受。近年来,众多生产不同商品名美金刚仿制药的公司不断涌现。在俄罗斯,首个美金刚仿制药“诺吉乐”于2010年获批,此后在实际临床实践中,其疗效的证据基础不断扩大,支持了该药的使用。上市后研究表明,“诺吉乐”为中度和重度阿尔茨海默病痴呆患者提供了长期有效的治疗。“诺吉乐”对认知和日常功能、痴呆的行为及精神症状具有临床显著治疗效果,并减轻了照料者负担,这一观察结果支持了上述观点。这种美金刚仿制药价格实惠,因此减轻了患者的经济负担,提高了治疗依从性。

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