Chrisp P, Goa K L
Adis Drug Information Services, Auckland, New Zealand.
Drugs. 1991 Feb;41(2):254-88. doi: 10.2165/00003495-199141020-00008.
Goserelin is a synthetic analogue of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH); or gonadorelin] which stimulates gonadotrophin and sex hormone release in the short term, and then causes suppression with continued administration. Goserelin is given as a subcutaneous biodegradable depot incorporating 3.6 mg of the drug, which is released continuously at an average rate of 120 micrograms/day over 4 weeks. Monthly goserelin depot therapy produces partial disease remission or stabilisation in about 75% of men with previously untreated prostatic cancer, a rate equivalent to that achieved with orchidectomy or diethylstilbestrol (stilboestrol). The response to goserelin is more rapid than to diethylstilbestrol, and goserelin is better tolerated. About 30 to 45% of premenopausal women with breast cancer responded to goserelin using objective assessment criteria, suggesting comparability to ovariectomy. In benign hormone-dependent conditions, preoperative goserelin aids surgical removal of uterine leiomyoma (fibroids) and reduces blood loss, and 6 months of therapy relieves the signs and symptoms of endometriosis. The elevation in testosterone at the beginning of goserelin therapy can result in disease 'flare' in men with prostate cancer, and sex steroid suppression with continued treatment results in hot flushes and loss of libido in most patients. Thus, goserelin is an effective alternative to surgery or estrogen therapy in prostatic cancer palliation, and possibly to ovariectomy in premenopausal breast cancer. Other gynaecological conditions reliant on the pituitary-gonadal axis also appear amenable to hormone manipulation with goserelin.
戈舍瑞林是促性腺激素释放激素（GnRH）[促黄体生成素释放激素（LHRH）；或戈那瑞林]的合成类似物，它在短期内刺激促性腺激素和性激素释放，然后持续给药会导致抑制作用。戈舍瑞林以皮下可生物降解的长效注射剂形式给药，其中含有3.6毫克药物，该药物在4周内以平均每天120微克的速率持续释放。每月一次的戈舍瑞林长效注射剂治疗可使约75%先前未经治疗的前列腺癌男性患者出现部分疾病缓解或病情稳定，这一缓解率与睾丸切除术或己烯雌酚（乙底酚）治疗相当。戈舍瑞林的反应比己烯雌酚更快，且耐受性更好。根据客观评估标准，约30%至45%的绝经前乳腺癌女性患者对戈舍瑞林有反应，表明其与卵巢切除术效果相当。在良性激素依赖性疾病中，术前使用戈舍瑞林有助于子宫平滑肌瘤（纤维瘤）的手术切除并减少失血，6个月的治疗可缓解子宫内膜异位症的体征和症状。戈舍瑞林治疗开始时睾酮水平升高可导致前列腺癌男性患者出现疾病“flare”，持续治疗导致的性类固醇抑制会使大多数患者出现潮热和性欲减退。因此，戈舍瑞林是前列腺癌姑息治疗中手术或雌激素治疗的有效替代方案，在绝经前乳腺癌治疗中可能是卵巢切除术的替代方案。其他依赖垂体 - 性腺轴的妇科疾病似乎也适合用戈舍瑞林进行激素调控。
