儿茶酚-O-甲基转移酶抑制剂临床应用进展

Current Clinical Progress of COMT Inhibitor

多巴胺(DA)是脑内重要的神经递质,参与调控椎体外系的运动功能以及人类的精神活动,情绪反应,认知、思想、感觉、理解和推理能力。多巴胺在各条通路的增多或减少可以导致各种疾病。儿茶酚-O-甲基转移酶(COMT)参与代谢降解多巴胺。COMT抑制剂可以减慢DA的代谢,且可以延长左旋多巴(L-dopa)在体内的半衰期,达到治疗由于DA减少的相关疾病。COMT抑制剂主要有托卡朋和恩他卡朋,两者分别在1997年和1998年由FDA首次批准上市。2004年,由卡比多巴、左旋多巴和恩他卡朋组成的复方制剂Sta levo被重新投放市场。本文总结了COMT抑制剂目前在临床上的应用进展,如协助治疗帕金森病,抗抑郁,抗Ⅱ型精神失常和治疗神经痛。

Dopamine （DA） is an important brain neurotransmitter, which involved in the regulation of extrapyramidal motor fun- ction, as well as human mental activity, emotional response, cognition, thinking, feeling, understanding and reasoning ability. The increa- se or decrease of Dopamine in each pathway can lead to various diseases. Catechol-O-methyl transferase （COMT） is involved in the met- abolic degradation of dopamine. COMT inhibitors can reduce the degradation of DA, and also can be extended to levodopa （L-dopa） half-life in vivo, so as to achieve treatment due to reduction of DA related diseases. COMT inhibitors include tolcapone and entacapone, respectively in 1997 and 1998 by FDA first approved listing. Carbidopa, levodopa and entacapone compounded preparation composed as Sta levo was back on the market in 2004. This paper summarizes current clinical progress of COMT inhibitor, such as assisting the treatment of Parkinson＇s disease, anti-depression, anti-schizophrenia and the treatment of neuralgia.