Nillius S J
Wien Klin Wochenschr. 1985 Dec 6;97(23):865-73.
Potent and long-acting stimulatory analogues to the hypothalamic gonadotrophin-releasing hormone (GnRH) were originally developed for profertility purposes. Paradoxically they proved to possess anti-fertility properties. Their anti-gonadal properties are at present being utilized for therapeutic purposes, e.g. contraception, treatment of central precocious puberty and sex steroid-dependent benign and malignant diseases of the reproductive organs, predominantly metastatic prostatic cancer. This review will be limited to the potential use of superactive GnRH agonists for contraception in women and men. Inhibit ion of ovulation by continuous GnRH agonist administration has been studied most extensively and will be dealt with in more detail. Other approaches to interfere with corpus luteum function (induction of in adequate luteal function, luteolysis or early abortion) have so far proved less successful. In males, complete azoospermia has not been consistently achieved by chronic high dose GnRH superagonist therapy alone. Testosterone supplementation is mandatory to avoid the unacceptable side effects associated with GnRH superagonist therapy, namely loss of libido and potency. Thus, to date, inhibition of ovulation by repeated intranasal GnRH agonist administration seems to have the greatest potential as a future contraceptive method. In long-term clinical trials, this new lead to birth control has already proved to provide safe, reliable and reversible contraception in women.
下丘脑促性腺激素释放激素（GnRH）的强效长效刺激类似物最初是为促进生育而研发的。矛盾的是，它们被证明具有抗生育特性。目前其抗性腺特性正被用于治疗目的，例如避孕、中枢性性早熟的治疗以及生殖器官的性激素依赖性良性和恶性疾病，主要是转移性前列腺癌。本综述将局限于超活性GnRH激动剂在男性和女性避孕方面的潜在用途。通过持续给予GnRH激动剂抑制排卵的研究最为广泛，将进行更详细的讨论。迄今为止，其他干扰黄体功能的方法（诱导黄体功能不足、黄体溶解或早期流产）已证明不太成功。在男性中，单独使用慢性高剂量GnRH超激动剂疗法尚未始终如一地实现完全无精子症。必须补充睾酮以避免与GnRH超激动剂疗法相关的不可接受的副作用，即性欲和性能力丧失。因此，迄今为止，通过反复鼻内给予GnRH激动剂抑制排卵似乎作为未来的避孕方法具有最大的潜力。在长期临床试验中，这种新的避孕方法已证明能为女性提供安全、可靠且可逆的避孕效果。
