摘要
米非司酮(RU486,Mifepristone,Mifegyne)是19-去甲睾酮的衍生物。在受体水平对抗孕激素和糖皮质激素。其药理学及药代动力学特点为:(1)吸收快,服药1h达到高峰;(2)半衰期长(25～30h);(3)无蓄积作用;(4)稳态血药浓度高。米非司酮的血清动力学受血清转运蛋白α12酸糖蛋白(AAG)调节,由于组织结合饱和度,故具有0.55L/(kg·d)的低代谢率、低分布容量、口服剂量超过100mg药物血清浓度却有一样的特点。它具有终止早孕、抗着床、诱导月经及促进宫颈成熟等作用。另外国外学者报道,应用米非司酮引起子宫内膜的萎缩,其机理是:(1)米非司酮可以通过PR途径,引起非竞争性对抗雌激素作用;(2)增加雄激素水平及雄激素受体水平,引起非竞争性对抗雌激素作用;(3)米非司酮使子宫螺旋动脉萎缩,引起子宫内膜供血不足;(4)米非司酮对子宫内膜有抗氧化作用;(5)米非司酮能够诱导细胞凋亡。故米非司酮越来越广泛地应用于妇产科领域,并发挥不可低估的作用。
Summary of Mifepristone （RU486, Mifepristone, Mifegyne） is 19-nortestosterone derivatives. In receptor antagonism, progesterone and glucocorticoids. Its pharmacological and pharmacokinetic characteristics： （1） absorbs quickly, taking drugs and 1h peak; （2） a long half-life （25-30h）; （3） no accumulation function; （4） the steady-state plasma concentrations are high. Mifepristone dynamics of serum is blood serum transporter α 12 acid glycoprotein （AAG） Regulation, because the Organization combined with saturation, with 0.55L/（kg · d） low metabolic rates, low distribution capacity, oral dose over 100mg drug serum concentration has the same characteristics . It has RLY, implantation, induced menstrual and promote the role of cervical ripening, etc. Also foreign scholars report, mifepristone caused the atrophy of the endometrium, the mechanism is （1） mifepristone can PR channels, caused by non-competitive confrontation estrogen effect; （2） increased Androgen levels and androgen receptor, causing the non-competitive confrontation estrogen effect; （3） in the uterus spiral arteries atrophy, cause endometrial insufficiency; （4） of mifepristone to have antioxidant effects; （5） of mifepristone can induce cell apoptosis. Hence the mifepristone and more widely used in Gynecology and obstetrics, and not underestimate the role.
出处
《当代医学》
2011年第9期33-34,共2页
Contemporary Medicine
