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.
出处
《药物不良反应杂志》
CSCD
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)
关键词
丙戊酸
代谢解毒
药物
Valproic acid
Metabolic detoxication, drug