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促性腺激素释放激素及其类似物的治疗用途

[Therapeutic use of gonadotropin-releasing hormone and its analogs].

作者信息

Carol W

机构信息

Klinik für Frauenheilkunde und Geburtshilfe, Bereichs Medizin der Friedrich-Schiller-Universität Jena.

出版信息

Zentralbl Gynakol. 1988;110(12):757-65.

PMID:3063027
Abstract

The discovery of the structure of Gn-RH in 1971 has opened new ways of investigation and treatment. The anterior pituitary gland requires episodic Gn-RH stimulation in order to secrete the gonadotropins in a physiologic manner. Deficiency of Gn-RH leads in both sexes to functional disturbances which in females may produce chronic anovulation and amenorrhea. Replacement therapy with the administration of Gn-RH in a pulsatile rhythm corrects the deficiency of endogenous Gn-RH secretion and stimulates via gonadotropins the function of peripheral target organs. If given continuously, Gn-RH leads to desensitization of pituitary Gn-RH receptors and inhibition of LH and FSH secretion. Potent and long-acting agonistic Gn-RH analogs have been synthesized which are capable of producing a selective "medical castration". Indications and preliminary results of the administration of Gn-RH and its long-acting agonists in humans are reviewed.

摘要

1971年促性腺激素释放激素(Gn-RH)结构的发现开启了新的研究和治疗途径。腺垂体需要间歇性的Gn-RH刺激才能以生理方式分泌促性腺激素。Gn-RH缺乏在男女两性中都会导致功能紊乱,在女性中可能会引起慢性无排卵和闭经。以脉冲节律给予Gn-RH进行替代疗法可纠正内源性Gn-RH分泌不足,并通过促性腺激素刺激外周靶器官的功能。如果持续给予Gn-RH,会导致垂体Gn-RH受体脱敏并抑制促黄体生成素(LH)和促卵泡生成素(FSH)的分泌。已合成了强效且长效的激动性Gn-RH类似物,它们能够产生选择性“药物去势”。本文综述了Gn-RH及其长效激动剂在人体中的应用指征和初步结果。

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