丙戊酸钠代谢产物2-丙基-2-戊烯酸的药理作用和安全性研究进展  

Progress in studies on pharmacological action and safety of sodium valproate＇s metabolites 2-propyl- 2-pentenoic acid

作　　者：李龙宽 谢娟[1] 

机构地区：[1]贵州省人民医院药剂科,贵阳550002

出　　处：《药物不良反应杂志》2015年第6期436-439,共4页Adverse Drug Reactions Journal

基　　金：贵州省自然科学基金[黔科合J字（2006）2068];贵州省卫生厅基金（gzwkj2010-1-003）

摘　　要：2-丙基-2-戊烯酸（2-ene-VPA）为丙戊酸钠在体内经线粒体β氧化产生的代谢产物，具有抗癫痫活性和镇静作用，同时具有一定的肝毒性和神经毒性。2-ene—VPA在体内的消除较丙戊酸钠慢，血浆蛋白结合率高于丙戊酸钠。2-ene-VPA的肝毒性较丙戊酸钠小，但也可干扰脂肪酸的正常氧化。丙戊酸诱导的高血氨症脑病的发生可能与2-ene-VPA在大脑的蓄积有关。2-ene-VPA的药理作用和安全性仍需更多的临床前研究进行评价。Valproic acid is metabolized via 13-oxidation in the body and produces 2-propyl-2- pentenoic acid （2-ene-VPA） which has antiepileptic activity and sedation but also has certain hepatotoxicity and neurotoxieity. 2-ene-VPA is eliminated slowly than VPA and has a high binding protein as to VPA. Hepatotoxicity of 2-ene-VPA is lesser than VPA but also can interfere with the normal oxidation of fatty acid. The valproie acid-induced hyperammonemie eneephalopathy may refer to the accumulation of 2-ene-VPA in brain. The pharmacological action and safety of 2-ene-VPA need more pre-clinical evaluation.

关 键 词：丙戊酸 代谢解毒 药物 

分 类 号：R96[医药卫生—药理学]