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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 被引量:1

Progress in studies on pharmacological action and safety of sodium valproate's metabolites 2-propyl- 2-pentenoic acid
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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.
作者 李龙宽 谢娟
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
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