屈昔多巴的临床应用进展

The Clinical Application Progress of Droxidopa

屈昔多巴是一种人工合成的去甲肾上腺素前体药物,当交感神经系统受损时,屈昔多巴在L-芳香族氨基酸脱羧酶的作用下,在外周和中枢神经通过脱羧作用转化为去甲肾上腺素,从而使神经系统去甲肾上腺素水平升高。1989年,日本便将屈昔多巴运用在神经源性体位性低血压的治疗中,但是其未在欧洲或美国使用,直到2014年美国FDA批准屈昔多巴治疗有症状的直立性低血压,其次是原发性自主神经病变、多巴胺-β-羟化酶缺乏症或非糖尿病自主神经病变。2012年1月,中国重庆圣华曦药业股份有限公司3.1类新药屈昔多巴胶囊(商品名:善为)获批上市,是屈昔多巴在国内的首次应用。屈昔多巴在治疗体位性低血压、步态障碍以及透析性低血压的疗效确切,安全性良好。文中就屈昔多巴的药动学特性、作用机制、临床效果以及耐受性研究进行综述。

Droxidopa, a synthesis of norepinephrine precursor drugs, metabolized to norepinephrine by LAAAD in peripheral and central nervous when the sympathetic nervous system was damaged. In 1989, droxidopa was applied in neurogenic orthostatic hypotension（n OH） in Japan while not in Europe or USA. Until 2014, the FDA approved its treatment in symptomatic orthostatic hypotension, primary autonomic neuropathy, DBDH and non-diabetic autonomic neuropathy. Droxidopa capsules named Shanwei which were produced by Shenghuaxi Pharm. Co., Ltd. were approved by CFDA in January 2012 and it was the first application of droxidopa in China. Its pharmacokinetics, mechanism, clinical effect and tolerability were reviewed. In general, it is effective and safe in orthostatic hypotension, gait disorder and dialytic hypotension, and further study is needed.