Pavlou S N, Interlandi J W, Wakefield G, Rivier J, Vale W, Rabin D
J Androl. 1986 Jul-Aug;7(4):228-33. doi: 10.1002/j.1939-4640.1986.tb00920.x.
LHRH agonist analogs have been investigated as potential male contraceptives. It has been shown that the LHRH agonistic analog [D-Trp6,Pro9-NEt] LHRH (LHRHA) given to men in single doses up to 500 micrograms daily for up to 20 weeks with the coadministration of testosterone enanthate produces reversible oligozoospermia. Individual responses to the treatment, however, were variable. In this study, we gave the same analog to eight normal male volunteers as a continuous infusion of 500 micrograms daily for 16 weeks. Testosterone enanthate, 100 mg, was given by injection every second week. Six of the subjects became oligozoospermic but the other two retained sperm counts that were greater than 20 million/ml, although their treatment continued for 20 weeks. The reasons for this variability of response are not clear. Serum immunoreactive LH values increased during the infusion period whereas testosterone declined. FSH values fell during treatment in all subjects except the two non-responders. The acute pituitary response to LHRHA during the treatment or shortly thereafter (48 h) was completely abolished, and bioactive LH values were suppressed totally. FSH, LH, testosterone and sperm counts returned to normal in all subjects following discontinuation of LHRHA infusion. Continuous infusion of 500 micrograms of LHRHA daily for 16 weeks with 100 mg of testosterone enanthate every 2 weeks induced desensitization of the pituitary, loss of LH bioactivity, and decreases of FSH and testosterone. This mode of administration, however, did not improve sperm density results obtained earlier by single daily injections of the analog. Heterogeneity of sperm density profiles still persists for reasons that are not yet clear.
促黄体生成素释放激素（LHRH）激动剂类似物已作为潜在的男性避孕药进行了研究。研究表明，给男性每日单剂量给予高达500微克的LHRH激动剂类似物[D-色氨酸6，脯氨酸9-乙酯]LHRH（LHRHA），持续20周，并同时给予庚酸睾酮，可产生可逆性少精子症。然而，个体对该治疗的反应存在差异。在本研究中，我们将相同的类似物以每日500微克的持续输注方式给予8名正常男性志愿者，持续16周。每两周注射100毫克庚酸睾酮。6名受试者出现少精子症，但另外两名受试者的精子计数仍大于2000万/毫升，尽管他们的治疗持续了20周。这种反应差异的原因尚不清楚。在输注期间，血清免疫反应性促黄体生成素（LH）值升高，而睾酮水平下降。除两名无反应者外，所有受试者在治疗期间促卵泡生成素（FSH）值均下降。治疗期间或之后不久（48小时），垂体对LHRHA的急性反应完全消失，生物活性LH值被完全抑制。停止LHRHA输注后，所有受试者的FSH、LH、睾酮和精子计数均恢复正常。每日持续输注500微克LHRHA，持续16周，并每2周给予100毫克庚酸睾酮，可导致垂体脱敏、LH生物活性丧失以及FSH和睾酮水平降低。然而，这种给药方式并未改善早期通过每日单次注射该类似物所获得的精子密度结果。精子密度分布的异质性仍然存在，原因尚不清楚。
