Brogden R N, Buckley M M, Ward A
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1990 Mar;39(3):399-437. doi: 10.2165/00003495-199039030-00007.
The gonadotrophin releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH); gonadorelin] agonist buserelin is a promising new agent in the treatment of a variety of disorders in gynaecology and andrology, paediatrics and oncology. While a single dose of buserelin stimulates the release of pituitary gonadotrophins, multiple doses produce reversible pituitary desensitisation, and this specific blockade of gonadotrophin support to the gonads provides the basis for the drug's efficacy in conditions dependent on sex hormone secretion. Thus, buserelin provides comparable efficacy to orchidectomy or high dose estrogens in the treatment of hormone-sensitive prostate cancer and exhibits a lower incidence of adverse effects. During the early phase of treatment it may be particularly useful in combination with antiandrogens. Buserelin also appears promising in hormone-sensitive premenopausal breast cancer. Extensive studies have proven the value of buserelin in endometriosis, where it produces a transient remission with gradual recurrence of the disease on cessation of treatment. Surgical intervention is necessary in severe disease after buserelin-induced involution of the lesions. In patients with uterine leiomyoma, preliminary data suggest that buserelin may be beneficial in rendering surgery more conservative by reducing fibroid size, although it appears unlikely to preclude surgical intervention. The use of buserelin to induce a state of reversible hypogonadotrophism before administration of exogenous gonadotrophins is a promising strategy in the treatment of infertility associated with polycystic ovary syndrome and other conditions of infertility with underlying ovarian dysfunction; such a strategy also clearly enhances the efficiency of in vitro fertilisation programmes. Initial studies suggest its potential usefulness as a female contraceptive when administered intermittently in conjunction with a progestogen. Buserelin represents a first-line treatment of central precocious puberty. In endometriosis the adverse effect profile of buserelin is generally favourable, with hypoestrogenic effects such as hot flushes and vaginal dryness, and decreased libido, predominating. There is no apparent detrimental effect on lipid metabolism. The potential for adverse hypoestrogenic effects on bone mineral content with long term administration remains to be clarified. Thus, the GnRH agonist buserelin represents an advance in the treatment of a variety of gynaecological and andrological as well as paediatric and oncological conditions, infertility and other sex-hormone dependent conditions, with a low incidence of adverse treatment effects.
促性腺激素释放激素（GnRH）[促黄体生成素释放激素（LHRH）；戈那瑞林]激动剂布舍瑞林是治疗妇科、男科、儿科及肿瘤学多种疾病的一种有前景的新药。虽然单剂量布舍瑞林会刺激垂体促性腺激素的释放，但多剂量会导致可逆性垂体脱敏，而这种对性腺促性腺激素支持的特异性阻断为该药物在依赖性激素分泌的疾病中的疗效提供了基础。因此，在治疗激素敏感性前列腺癌方面，布舍瑞林与睾丸切除术或高剂量雌激素具有相当的疗效，且不良反应发生率较低。在治疗早期，它与抗雄激素联合使用可能特别有用。布舍瑞林在激素敏感性绝经前乳腺癌中似乎也很有前景。广泛的研究已证明布舍瑞林在子宫内膜异位症中的价值，它能使疾病暂时缓解，但在治疗停止后疾病会逐渐复发。在布舍瑞林使病变 involution 后，严重疾病仍需手术干预。对于子宫肌瘤患者，初步数据表明布舍瑞林可能有助于通过缩小肌瘤大小使手术更保守，尽管似乎不太可能避免手术干预。在给予外源性促性腺激素之前，使用布舍瑞林诱导可逆性性腺功能减退状态是治疗与多囊卵巢综合征及其他伴有潜在卵巢功能障碍的不孕相关疾病的一种有前景的策略；这种策略也明显提高了体外受精程序的效率。初步研究表明，当与孕激素间歇联合使用时，它作为女性避孕药有潜在用途。布舍瑞林是中枢性性早熟的一线治疗药物。在子宫内膜异位症中，布舍瑞林的不良反应通常较好，主要是低雌激素效应，如潮热、阴道干燥和性欲减退。对脂质代谢没有明显的有害影响。长期给药对骨矿物质含量的潜在不良低雌激素效应仍有待阐明。因此，GnRH 激动剂布舍瑞林代表了在治疗各种妇科、男科、儿科及肿瘤学疾病、不孕及其他性激素依赖疾病方面的一项进展，且治疗不良反应发生率较低。
