摘要
儿茶酚-氧位-甲基转移酶(COMT)抑制剂是继左旋多巴(L-dopa)和多巴胺受体激动剂之后推入临床的治疗帕金森病(PD)的一类新药,可抑制外周COMT活性,延长L-dopa的半衰期和药时曲线下面积(AUC),能延长和增加L-dopa的生物利用度,但不影响达峰时间(Tmax)及达峰浓度(Cmax),是长期L-dopa治疗后出现疗效减退和开关现象等并发症时重要的辅助药物。恩他卡朋(entacapone)被认为是较安全的COMT抑制剂。近几年的研究结果显示,在出现运动波动的PD患者中,恩他卡朋可减少L-dopa剂量,延长"开"期,明显缩短"关"期,并改善UPDRS的运动评分,提高生活质量。
Catechol-O-methyltransferase （COMT） inhibitor is a kind of new drug applied in clinic following L-dopa and dopaminergic agonists. COMT inhibitor can inhibit COMT activity in the peripheral, prolong the elimination of L-dopa, increase the area under the concentration-time curve and its bioavailability, but Tmax and Cmax are not affected. COMT inhibitor is an important adjunct to levodopa for the treatment of patients with Parkinson＇ s disease （PD） with motor fluctuations. Entacapone is considered as a safe COMT inhibitor. Based on the studies, entacapone reduces daily dosage of L-dopa, increases the daily ON-time, and reduces the daily OFF-time correspondingly in patients with PD with motor fluctuations. It also improves Unified Parkinson＇s Disease Rating Scale motor scores, improves a variety of quality-of-life measures.
出处
《中国临床神经科学》
2008年第2期183-188,共6页
Chinese Journal of Clinical Neurosciences
