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征集健康育龄妇女9例于连续若干周期的黄体晚期单次口服米非司酮,剂量分别依次为25mg、100mg、400mg和600mg,并于服药前以及服药后4、8、12、24、48、72、96和120h采血,以测定血清ACTH和皮质醇。另征集健康育龄妇女15例,随机分成三组(组Ⅰ~Ⅲ),分别在黄体早、中、晚期给于米非司酮25mgq12h×6,在d1~d7期间每天采血以测定血清ACTH、皮质醇和米非司酮水平。结果显示米非司酮25mg和100mg单次口服对ACTH、皮质醇水平及其昼夜分泌节律并无明显影响,可是一次口服高剂量(400mg和600mg)后,ACTH和皮质醇上午分泌水平增加,昼夜变化幅度明显减少。米非司酮多次用药(25mqq12h×6)期间,每天上午ACTH和皮质醇几乎无明显变化,黄体期早、中、晚期服药的对象,其血药浓度、ACTH与皮质醇水平均无明显差异。本研究提示对于非妊娠妇女,米非司酮以剂量-依赖的方式显示其抗糖皮质激素活性,只有一次口服大剂量米非司酮才会明显影响其ACTH与皮质醇的昼夜分泌节律。黄体期不同的生殖激素状态对口服米非司酮后的药物吸收及其抗糖皮质激素活性无明显影响。
A total of 9 healthy women of childbearing age were enrolled in this study. Mifepristone was orally given in a single dose of 25 mg, 100 mg, 400 mg, and 600 mg in successive luteal phase for several consecutive cycles. Before and 4, 8, 12, 24, 48, Blood samples were taken at 72, 96 and 120 h to determine serum ACTH and cortisol. Fifteen healthy women of childbearing age were collected and randomly divided into three groups (group Ⅰ ~ Ⅲ). The patients were given mifepristone 25mgq 12h × 6 respectively in the early, middle and late stages of corpus luteum. Blood samples were collected every day from d1 to d7 to determine serum ACTH, cortex Alcohol and mifepristone levels. The results showed that mifepristone 25mg and 100mg single oral administration of ACTH, cortisol levels and circadian rhythm did not have a significant effect, but a high dose of oral (400mg and 600mg), ACTH and cortisol morning secretion increased day and night The change range is obviously reduced. Mifepristone multiple administration (25mqq12h × 6) during the morning ACTH and cortisol almost no significant change in the early, middle and late luteal phase of the object, the plasma concentration, ACTH and cortisol levels were no significant difference . This study suggests that mifepristone shows anti-glucocorticoid activity in a dose-dependent manner in nonpregnant women. Only a single oral high dose of mifepristone significantly affects the diurnal secretion of ACTH and cortisol. Luteal phase of different reproductive hormone status after oral administration of mifepristone drug absorption and anti-glucocorticoid activity had no significant effect.