帕金森病药物

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帕金森病药物

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31644162 (在PubMed
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文摘

帕金森病是一种进行性神经病学方面的疾病,其特征是缓慢和缺乏运动迟缓,肌肉僵硬,静止震颤,无序的姿势。发病通常是6号还是7号十年生命的运动不能进展缓慢,严重的震动,身体残疾和死亡在10至25年的最初症状。帕金森病是常见的,影响大约1%的美国人60岁以上。帕金森病的原因是未知的,但被dopamine-containing神经元的损失在脑干的黑质致密部和失去正常的多巴胺能神经传递。治疗帕金森病的不断发展,导致改善生活质量和生存。最初的代理用于帕金森病抗胆碱能药物包括苯海索(Artane Trihexy: 1949),苯托品(Cogentin: 1954)和biperiden (Akineton: 1959);他们在帕金森症的作用机制尚不完全清楚。与增加多巴胺的作用的理解帕金森症的病理生理学,代理,直接或间接地影响多巴胺传输已经开发,导致显著改善帕金森病症状的管理。左旋多巴(左旋多巴:1970)是一种多巴胺和代谢前体是帕金森病最有效的代理。它通常是结合卡比多巴(Sinemet: 1975),这就增加了左旋多巴的药物水平和半衰期抑制氨基酸脱羧酶代谢左旋多巴外围。 Dopaminergic receptor agonists are also beneficial in Parkinson disease and are often combined with levodopa/carbidopa. Dopamine receptor agonists currently available include bromocriptine (1978: Parlodel), pergolide (Permax: 1988), apomorphine (Apokyn: 2004) and more selective agonists for the D2 class of dopamine receptors - ropinirole (Requip: 1997), pramipexole (Mirapex: 1997) and rotigotine (Neupro which is formulated in a transdermal patch: 2007). More recently, inhibitors of catechol-O-methyltransferase (COMT) have been developed that block the major enzyme responsible for the metabolism of dopamine; these agents include tolcapone (Tasmar: 1998) and entacapone (Comtan: 2003). Dopamine is also metabolized by the monamine oxidases and selegiline (Atapryl: 2006) and rasagiline (Azilect: 2007) which are specific inhibitors of monamine oxidase (MAO) type B, and are used as an adjunctive therapy with levodopa in therapy of Parkinson disease. Amantadine (Symmetrel: 1987) also has activity in Parkinson disease, perhaps through stimulation of release of dopamine in the substantial nigra. It is discussed separately as an anti-influenza agent. Other agents used in the management of Parkinson disease are used to treat specific complications such as psychosis (pimavanserin: Nuplazid, 2016) and postural hypotension (droxidopa: Vectibix, 2014). Most of the drugs used to treat Parkinson disease have little potential for hepatotoxicity and are rare causes of clinically apparent acute liver injury, the exception being tolcapone. The full references on hepatotoxicity and safety of the drugs for Parkinson disease are given in the discussion of the individual agents listed below.

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药物