Clinical Pharmacology, Bayer Pharma AG, Müllerstraße 178, D-13342 Berlin, Germany.
J Clin Pharmacol. 2012 Nov;52(11):1704-13. doi: 10.1177/0091270011423664. Epub 2011 Nov 29.
Dienogest offers pharmacological advantages for the effective treatment of endometriosis and for use in contraception and hormone replacement therapy. This pharmacodynamic study investigated the ovulation-inhibiting effects of dienogest monotherapy in healthy women. Dienogest was administered at 0.5, 1, 2, or 3 mg daily for up to 72 days to women aged 18 to 35 years (n = 102). Ovarian activity was assessed pretreatment and during 2 treatment periods (days 0-36 and days 37-72) by the Hoogland score, based on follicle size and serum estradiol and progesterone levels. Additional hormonal parameters and endometrial thickness were assessed. Hoogland scoring indicated ovulation in all women pretreatment, decreasing to 3 of 21, 1 of 23, 0 of 20, and 0 of 23 women in the 0.5-, 1-, 2-, and 3-mg groups, respectively (per-protocol set). Maximum serum estradiol concentrations were similar to pretreatment levels in the 0.5- or 1-mg group and decreased moderately (within physiologic levels) in the 2- or 3-mg group. Endometrial thickness was reduced by all dienogest doses. Hormonal changes during follow-up indicated resumption of ovulation in most women, shortly after treatment cessation. Dienogest ≥2 mg daily provides moderate suppression of estradiol production and reliable ovulation inhibition, which reverses rapidly after treatment cessation.
地诺孕素在治疗子宫内膜异位症、避孕和激素替代疗法方面具有药理学优势。这项药效学研究调查了地诺孕素单药治疗对健康女性的排卵抑制作用。18 至 35 岁的女性接受为期 72 天的地诺孕素 0.5、1、2 或 3 mg/天治疗（n = 102）。通过卵泡大小和血清雌二醇和孕酮水平的 Hoogland 评分，在治疗前和治疗的 2 个时期（第 0-36 天和第 37-72 天）评估卵巢活动。评估了其他激素参数和子宫内膜厚度。Hoogland 评分表明所有女性在治疗前均排卵，分别降至 0.5、1、2 和 3 mg 组的 21、23、20 和 23 名女性中的 3、1、0 和 0（符合方案集）。最大血清雌二醇浓度与 0.5 或 1 mg 组的治疗前水平相似，而 2 或 3 mg 组的浓度适度下降（在生理水平内）。所有地诺孕素剂量均降低了子宫内膜厚度。随访期间的激素变化表明，大多数女性在治疗停止后不久恢复排卵。每日至少 2 毫克的地诺孕素可适度抑制雌二醇的产生并可靠地抑制排卵，停药后迅速逆转。
