Rajfer J, Handelsman D J, Swerdloff R S, Farrer J H, Sikka S C
Fertil Steril. 1986 Jun;45(6):794-9. doi: 10.1016/s0015-0282(16)49395-7.
For determination of the dose-response relationships of plasma luteinizing hormone (LH) and follicle-stimulating hormone (FSH) to the intranasal administration of gonadotropin-releasing hormone (GnRH), normal adult men were administered doses of 100, 200, 400, and 800 micrograms of GnRH on separate days, and plasma LH and FSH were measured before and after nasal insufflation of GnRH. Plasma LH was increased after a minimum dose of 200 micrograms GnRH. Median peak plasma LH levels occurred 30 minutes after intranasal GnRH and followed a log-dose relationship. When compared with intravenous GnRH, the biopotency of intranasal GnRH at the 200-, 400-, and 800-microgram doses was 1.1%, 2.3%, and 6.2%, respectively. Plasma FSH levels rose significantly only after the highest (800-micrograms) intranasal GnRH dose. From these data, we conclude that in eugonadal adult men the minimal effective dose of intranasal GnRH to elicit a significant pituitary (LH) response is 200 micrograms and that the relative efficacy of intranasal GnRH increases with the dose. In spite of the apparently low biopotency for intranasal GnRH, this route of administration may be considered as an alternative to the parenteral mode of GnRH delivery, and the lower biopotency can be partly overcome by increasing the dose.
为了确定血浆促黄体生成素（LH）和促卵泡生成素（FSH）对鼻内给予促性腺激素释放激素（GnRH）的剂量反应关系，在不同日期给正常成年男性分别给予100、200、400和800微克的GnRH，并在鼻内注入GnRH前后测量血浆LH和FSH。在最低剂量200微克GnRH后，血浆LH升高。血浆LH峰值中位数在鼻内给予GnRH后30分钟出现，并呈对数剂量关系。与静脉注射GnRH相比，200微克、400微克和800微克剂量的鼻内GnRH的生物效价分别为1.1%、2.3%和6.2%。仅在最高（800微克）鼻内GnRH剂量后，血浆FSH水平才显著升高。从这些数据中，我们得出结论，在性腺功能正常的成年男性中，引起显著垂体（LH）反应的鼻内GnRH的最小有效剂量为200微克，且鼻内GnRH的相对效力随剂量增加而增加。尽管鼻内GnRH的生物效价明显较低，但这种给药途径可被视为胃肠外给予GnRH方式的一种替代方法，并且通过增加剂量可部分克服较低的生物效价。
