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儿茶酚氧位甲基转移酶(COMT)抑制剂是一种全新的帕金森病治疗选择。COMT抑制剂具有延长左旋多巴(L-dopa)疗效的作用,本文总结了COMT抑制剂tolcapone和entacapone临床试验的结果。 COMT抑制剂tolcapone和entacapone都是氮甲酚胺型化合物,两者都是强效的外周COMT抑制剂并且可安全应用于人。加入一种COMT抑制剂时,L-dopa的药物代谢学也发生了改变,多次服用后,血浆中的L-dopa水平很少波动,这使L-dopa水平更稳定而不必增加L-dops/卡比多巴缓释剂的剂量。
Catechol oxygen methyltransferase (COMT) inhibitor is a new treatment option for Parkinson’s disease. COMT inhibitors have the effect of prolonging the efficacy of L-dopa. This paper summarizes the results of the clinical trials of tolcapone and entacapone, a COMT inhibitor. Both COMT inhibitors, tolcapone and entacapone, are azocresol-type compounds, both of which are potent peripheral COMT inhibitors and are safe for human use. Pharmacokinetics of L-dopa have also changed when a COMT inhibitor is added, and plasma levels of L-dopa fluctuate less frequently after multiple injections, making L-dopa more stable without increasing L-dops / Carbidopa slow release dose.