Entacapone: catechol-O-methyltransferase抑制剂对帕金森病的辅助治疗。

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纳吉布J

Entacapone: catechol-O-methyltransferase抑制剂对帕金森病的辅助治疗。

其他。2001年6月,23 (6):802 - 32;讨论771年。

PubMed ID
11440283 (在PubMed
]
文摘

背景:当使用左旋多巴治疗帕金森病,药物在周围神经系统的退化与动作障碍和运动的波动有关。这种退化是由catechol-O-methyltransferase (COMT的),一种酶参与代谢的儿茶酚胺和苯邻二酚的化合物。抑制COMT的活动延长左旋多巴的作用,减少波动的反应。Entacapone的选择性抑制剂COMT的活动主要是在周围神经系统,与在中枢神经系统的影响不大。目的:本文综述了药理性质和临床实用性entacapone治疗帕金森病。方法:最近的研究,摘要和评论发表在英文文献被确定通过搜索MEDLINE(1966 - 2000年9月),国际制药(1970 - 2000年9月),摘要和PharmaProjects(2000年9月版),和网站的帕金森病会议从1996年必威国际app到2000年9月举行。有关人类研究提供进一步的信息entacapone的药理性质和临床实用性。结果:Entacapone迅速吸收,最大浓度的时间约为1小时。消除其血浆半衰期在beta阶段是0.4到0.7小时和2.4小时在γ阶段,它有35%的绝对生物利用度口服后,二次初步的间隙。Entacapone 98%的蛋白质绑定; thus, it is not distributed widely in tissues and is almost completely metabolized before excretion (0.1%-0.2% of dose unchanged in urine). The drug inhibits erythrocyte-soluble COMT activity in a dose-dependent fashion (48% after a 400-mg dose, 82% after an 800-mg dose). The inhibitory effect is reversible, with recovery of soluble COMT activity within 4 to 8 hours. In levodopa-treated patients with Parkinson's disease who experience motor fluctuations, clinical trials have demonstrated entacapone's effectiveness in increasing "on" time (the period during which medications relieve the symptoms of Parkinson's disease) by up to 1.2 hours, decreasing "off" time (the period during which symptoms increase) by 0.9 to 1.3 hours, and producing overall total improvement in scores on the Unified Parkinson's Disease Rating Scale. The recommended dosage of entacapone is 200 mg administered orally with each dose of levodopa/carbidopa, up to 8 doses per day. The drug is generally well tolerated, with most adverse effects attributed to levodopa-related dopaminergic effects, including dyskinesias and nausea. CONCLUSIONS: In clinical trials, adjuvant treatment with entacapone appeared to be an effective and well-tolerated therapeutic strategy in patients with Parkinson's disease who experience fluctuations in the response to levodopa therapy. The increased elimination half-life of levodopa with concomitant entacapone results in greater and more sustained plasma levodopa levels, with more constant dopaminergic stimulation in the brain and greater amelioration of parkinsonian symptoms.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
Entacapone 儿茶酚O-methyltransferase 蛋白质 人类
是的
抑制剂
 细节