McLachlan R I, Healy D L, Burger H G
Br J Obstet Gynaecol. 1986 May;93(5):431-54.
LHRH agonists are synthetic peptide analogues of hypothalamic luteinizing hormone releasing hormone (LHRH) with superior potency and longer duration of gonadotrophin release. Paradoxically, repeated administration causes pituitary desensitization with diminished gonadotrophin and oestradiol secretion. A state of hypogonadotrophic hypogonadism is reversibly induced; plasma oestrogen can be reduced to castrate levels. LHRH agonists reliably induce anovulation but are unlikely to replace existing contraceptive methods in most normal women. By contrast these agents offer, for the first time, the prospect of inducing a reversible pseudomenopause essentially free of side-effects. LHRH analogues promise to have a profound impact upon the management of a diverse range of oestrogen-dependent gynaecological diseases both benign and malignant. In particular, they may shortly become the gynaecological treatment of choice in endometriosis, as well as becoming part of the management of common gynaecological disorders such as dysfunctional uterine bleeding and uterine fibroids.
促性腺激素释放激素(LHRH)激动剂是下丘脑促黄体生成素释放激素(LHRH)的合成肽类似物,具有更强的效力和更长的促性腺激素释放持续时间。矛盾的是,重复给药会导致垂体脱敏,使促性腺激素和雌二醇分泌减少。可逆性地诱导出性腺功能减退性性腺功能低下状态;血浆雌激素可降至去势水平。LHRH激动剂能可靠地诱导无排卵,但在大多数正常女性中不太可能取代现有的避孕方法。相比之下,这些药物首次提供了诱导基本无副作用的可逆性假绝经的前景。LHRH类似物有望对多种雌激素依赖性妇科良性和恶性疾病的治疗产生深远影响。特别是,它们可能很快成为子宫内膜异位症的首选妇科治疗方法,也将成为功能失调性子宫出血和子宫肌瘤等常见妇科疾病治疗的一部分。