治疗发作性睡病新药——组胺H_3受体拮抗剂和反向激动剂哌托生特

A new drug therapy in narcolepsy——histamine H_3-receptor antagonist/inverse agonist pitolisant

哌托生特为一种口服有效的组胺H3受体拮抗剂和反向激动剂,由法国Bioproject公司开发,于2016年3月31日获欧盟批准用于治疗成人伴或不伴猝倒的发作性睡病。临床试验证实与安慰剂相比哌托生特能够明显降低发作性睡病患者白日过度睡眠,也能够明显降低猝倒发生率。哌托生特最常见的不良反应为失眠、头痛、恶心、焦虑、兴奋、头晕及抑郁等。

Pitolisant is an orally available histamine H3 receptor antagonist/inverse agonist that is under development by Bioproject. Pitolisant was approved in the EU on 31 March 2016 for the treatment of narcolepsy with or without cataplexy in adults. In the clinic trials, pitolisant significantly decreased excessive daytime sleepiness versus placebo in adults with narcolepsy with or without cataplexy. Pitolisant also significantly decreased cataplexy rate versus placebo in these patients. The most frequent adverse drug reactions reported with Ditolisant were insomnia, headache nausea, anxiety, irritability, dizziness, depression and so on.