Zaki K, Atkinson L E, Segal S J
Arzneimittelforschung. 1978;28(6):1003-8.
17 alpha-Acetoxy-6 alpha-methylprogesterone (medroxy-progesterone acetate, MPA) in doses of 50 mg followed 4 weeks later by an additional 100 mg was i.m. injected in 5 adult normal female monkeys. Serum levels of MPA, progesterone, estradiol-17-beta and LH were determined every other day for a period of 8 weeks then weekly for 8 months. Peak values of serum MPA were detected 2 weeks postinjection followed by a gradual decline to undetectable levels after variable periods ranging from 125 to 225 days. The drug, in the doses used, caused inhibition of LH and estradiol surges and suppression of progesterone for more than 6 months. The return of menstrual cyclicity preceded the return of ovulatory cyclicity. Menstrual cyclicity occurred while the drug was still detectable in the blood. The probable site of action of the drug is discussed.
给5只成年正常雌性猴子肌肉注射剂量为50毫克的17α - 乙酰氧基 - 6α - 甲基孕酮(醋酸甲羟孕酮,MPA),4周后再追加100毫克。每隔一天测定血清中MPA、孕酮、雌二醇 - 17 - β和促黄体生成素(LH)的水平,持续8周,之后8个月每周测定一次。注射后2周检测到血清MPA峰值,随后在125至225天不等的不同时间段后逐渐下降至检测不到的水平。所用剂量的该药物导致LH和雌二醇激增受到抑制,孕酮受到抑制超过6个月。月经周期的恢复先于排卵周期的恢复。在血液中仍可检测到药物时就出现了月经周期。讨论了该药物可能的作用部位。