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儿茶酚-O-甲基转移酶抑制剂的安全性和耐受性

Safety and tolerability of COMT inhibitors.

作者信息

Brooks David J

机构信息

MRC Clinical Sciences Centre, Faculty of Medicine, Imperial College London, Hammersmith Hospital, United Kingdom.

出版信息

Neurology. 2004 Jan 13;62(1 Suppl 1):S39-46. doi: 10.1212/wnl.62.1_suppl_1.s39.

DOI:10.1212/wnl.62.1_suppl_1.s39
PMID:14718679
Abstract

Combining levodopa with the catechol-O-methyltransferase (COMT) inhibitor entacapone has been shown to be an effective strategy in the management of Parkinson's disease (PD) patients experiencing motor fluctuations. Safety and tolerability information has come from postmarketing surveillance studies as well as several randomized, placebo-controlled trials with long-term open-label extension phases specifically investigating the safety and tolerability of levodopa plus entacapone. Results show the most common dopaminergic side effects to be dyskinesia and nausea, which result from the increased bioavailability of levodopa and can be readily managed. Non-dopaminergic side effects include diarrhea and harmless urine discoloration. There is no convincing evidence of hepatic injury with entacapone use, and therefore monitoring of liver enzymes is unnecessary. With over 300,000 patient-years of exposure, levodopa combined with entacapone can be considered safe and well tolerated.

摘要

将左旋多巴与儿茶酚-O-甲基转移酶(COMT)抑制剂恩他卡朋联合使用,已被证明是治疗出现运动波动的帕金森病(PD)患者的有效策略。安全性和耐受性信息来自上市后监测研究以及多项随机、安慰剂对照试验,这些试验具有长期开放标签延长期,专门研究左旋多巴加恩他卡朋的安全性和耐受性。结果显示,最常见的多巴胺能副作用是运动障碍和恶心,这是由左旋多巴生物利用度增加导致的,并且很容易处理。非多巴胺能副作用包括腹泻和无害的尿液变色。没有令人信服的证据表明使用恩他卡朋会导致肝损伤,因此无需监测肝酶。在超过300,000患者年的暴露量下,左旋多巴联合恩他卡朋可被认为是安全且耐受性良好的。

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