PDF(Pubmed)
Abstract：
Current medical treatment options for endometriosis associated pains are inadequate. Evidence on effects of nonsteroidal anti-inflammatory drugs is scarce. Around one third of patients are not responsive to oral contraceptives or progestins due to progesterone resistance. Gonadotropin-releasing hormone (GnRH) agonists can only be used for a short duration because of associated side effects. Oral GnRH antagonists, including elagolix, relugolix, and linzagolix allow oral administration, induce dose dependent reduction of estradiol levels, do not cause initial flare up of endometriosis symptoms, and allow the fast return of ovarian function and menstruation after discontinuation. Elagolix at a low dose of 150 mg once daily, or the higher dose of 200 mg twice daily, significantly increased the proportion of women achieving clinically meaningful decline of dysmenorrhea, noncyclic pelvic pain, and dyspareunia. Relugolix at an oral dose of 40 mg/day results in improvement in different forms of endometriosis related pelvic pain, with an efficacy and side effect profile similar to that of GnRH agonists. Adding 1 mg of estradiol and 0.5 mg of norethindrone to 40 mg of relugolix (relugolix combination therapy) allows extension of treatment to 24 weeks with maintained efficacy and an improved side effect profile. Linzagolix, in a dose of 75 mg/day, can be used alone to treat endometriosis associated pain. For severe pelvic pain and dyspareunia, linzagolix can be used in a high dose of 200 mg/day with hormonal add-back therapy to preserve bone health.
摘要：
目前子宫内膜异位症相关疼痛的药物治疗选择是不充分的。关于非甾体类抗炎药作用的证据很少。大约三分之一的患者由于孕酮抵抗而对口服避孕药或孕激素没有反应。由于相关的副作用,促性腺激素释放激素(GnRH)激动剂只能短期使用。口服GnRH拮抗剂,包括elagolix,relugolix,linzagolix允许口服,诱导雌二醇水平的剂量依赖性降低，不要引起子宫内膜异位症症状的初始发作，并在停药后允许卵巢功能和月经的快速恢复。Elagolix在150毫克的低剂量每日一次，或每日两次200毫克的较高剂量，显着增加女性达到临床上有意义的痛经下降的比例，非周期性盆腔疼痛，和性交困难.口服剂量为40毫克/天的Relugolix可改善不同形式的子宫内膜异位症相关的盆腔疼痛，与GnRH激动剂相似的疗效和副作用。在40mgrelugolix（relugolix联合疗法）中添加1mg雌二醇和0.5mgnoretindrone，可以将治疗延长至24周，并保持疗效并改善副作用。Linzagolix,剂量为75毫克/天，可单独用于治疗子宫内膜异位症相关性疼痛。对于严重的盆腔疼痛和性交困难，linzagolix可以以200毫克/天的高剂量使用激素补充疗法来保持骨骼健康。
