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首页> 外文期刊>CNS drug reviews >Catechol-O-methyltransferase and its inhibitors in Parkinson's disease.
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Catechol-O-methyltransferase and its inhibitors in Parkinson's disease.

机译：儿茶酚-O-甲基转移酶及其抑制剂在帕金森氏病中的作用。

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Parkinson's disease (PD) is a neurological disorder characterized by the degeneration of dopaminergic neurons, with consequent reduction in striatal dopamine levels leading to characteristic motor symptoms. The most effective treatment for this disease continues to be the dopamine replacement therapy with levodopa together with an inhibitor of aromatic amino acid decarboxylase (AADC). The efficacy of this therapy, however, decreases with time and most patients develop fluctuating responses and dyskinesias. The last decade showed that the use of catechol-O-methyltransferase inhibitors as adjuvants to the levodopa/AADC inhibitor therapy, significantly improves the clinical benefits of this therapy. The purpose of this article is to review the current knowledge on the enzyme catechol-O-methyltransferase (COMT) and the role of COMT inhibitors in PD as a new therapeutic approach to PD involving conversion of levodopa to dopamine at the target region in the brain and facilitation of the continuous action of this amine at the receptor sites. A historical overview of the discovery and development of COMT inhibitors is presented with a special emphasis on nebicapone, presently under clinical development, as well as entacapone and tolcapone, which are already approved as adjuncts in the therapy of PD. This article reviews human pharmacokinetic and pharmacodynamic properties of these drugs as well as their clinical efficacy and safety.
机译：帕金森氏病（PD）是一种神经系统疾病，其特征是多巴胺能神经元变性，因此纹状体多巴胺水平降低导致特征性运动症状。对该疾病最有效的治疗仍然是用左旋多巴与芳香族氨基酸脱羧酶抑制剂（AADC）一起进行多巴胺替代治疗。但是，这种疗法的疗效会随着时间而降低，大多数患者会出现波动的反应和运动障碍。最近十年表明，使用儿茶酚-O-甲基转移酶抑制剂作为左旋多巴/ AADC抑制剂治疗的佐剂可显着改善该疗法的临床疗效。本文的目的是回顾关于儿茶酚-O-甲基转移酶（COMT）的最新知识以及COMT抑制剂在PD中作为PD治疗的一种新的治疗方法的作用，该方法涉及在大脑目标区域将左旋多巴转化为多巴胺和促进这种胺在受体部位的连续作用。介绍了有关COMT抑制剂发现和开发的历史概述，其中特别强调了目前正在临床开发中的奈比卡朋，以及已被批准作为PD治疗辅助药物的entacapone和tolcapone。本文综述了这些药物在人体中的药代动力学和药效学特性，以及它们的临床疗效和安全性。

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