Shoupe D, Mishell D R, Lahteenmaki P, Heikinheimo O, Birgerson L, Madkour H, Spitz I M
Department of Obstetrics and Gynecology, University of Southern California, Los Angeles.
Am J Obstet Gynecol. 1987 Dec;157(6):1415-20. doi: 10.1016/s0002-9378(87)80235-1.
The response to a single oral dose of the antiprogesterone RU 486 was studied in the midluteal phase in 26 normal women. Each subject received a dose between 50 and 800 mg RU 486 on days 6 to 8 after the luteinizing hormone surge and blood samples were taken over the following 48 hours. Another group of five patients received a single oral dose of 200 mg RU 486 and blood sampling was extended for 14 days. Menses were induced in all women but one within 3 days after RU 486 administration. Two distinct patient populations emerged. In nine of the subjects, there was a single bleeding episode and the treatment cycle was significantly shorter (p less than 0.05) than the following cycle. In 16 of these 25 patients a second bleeding episode occurred 19.0 +/- 0.8 days after the luteinizing hormone surge. The total treatment cycle was significantly prolonged (p less than 0.05) when compared with the following cycle. In the group with a single bleeding episode, there was a significant decline in follicle-stimulating hormone, estradiol, and progesterone over the 48-hour sampling period, but there was no change in these values in the group with two bleeding episodes. These two groups could not be separated on the basis of RU 486 dose or serum levels. After the four higher doses, there was a dose-dependent rise in serum prolactin. There were no alterations in mean cortisol values with the three lower doses, but there was a significant increase at 24 and 48 hours after the higher doses. Serum levels of RU 486 were maximal between 1 and 4 hours and the half-life of serum RU 486 was determined to be 24 hours.
对26名正常女性在黄体中期口服单剂量抗孕激素RU 486的反应进行了研究。每位受试者在促黄体生成素激增后的第6至8天接受50至800毫克RU 486的剂量，并在接下来的48小时内采集血样。另一组5名患者接受200毫克RU 486的单次口服剂量，血样采集延长至14天。除一名女性外，所有女性在服用RU 486后3天内均出现月经来潮。出现了两个不同的患者群体。在9名受试者中，有一次出血事件，治疗周期明显短于下一个周期（p<0.05）。在这25名患者中的16名中，促黄体生成素激增后19.0±0.8天出现第二次出血事件。与下一个周期相比，总治疗周期明显延长（p<0.05）。在有一次出血事件的组中，在48小时的采样期内促卵泡激素、雌二醇和孕酮显著下降，但在有两次出血事件的组中这些值没有变化。这两组在RU 486剂量或血清水平上无法区分。在四个较高剂量后，血清催乳素呈剂量依赖性升高。三个较低剂量时平均皮质醇值无变化，但较高剂量后24小时和48小时显著升高。血清RU 486水平在1至4小时达到最大值，血清RU 486的半衰期确定为24小时。
