Roger M, Chaussain J L, Bost M, Bozzola M, Colle M, Despert F, François R, Freycon F, Garandeau P, Malpuech G
Rev Fr Gynecol Obstet. 1986 May;81(5):297-305.
LH-RH analogs, substituted in position 6 by D-tryptophane, D-serine(tBu), D-leucine or D-alanine induce a strong stimulation of the gonadotrophs, followed by a desensitization of the LH-RH receptors, which leads to a blockade of the gonadotropin secretion and to a hypogonadism. A delayed release preparation of D-Trp-6-LH-RH (Decapeptyl in microcapsules), designed to release the peptide for 28 days after intramuscular injection, was given to 69 girls and 18 boys with precocious puberty. In both, plasma levels of gonadotropins and gonadal steroids were suppressed within 3 weeks, whilst pituitary responses to LH-RH were almost abolished within 7 weeks. A significant improvement of secondary sex characteristics, as well as gonadal size, was obvious within 6 months. Growth velocity was markedly lowered and, more, in most of children, bone maturation was blocked. This study shows that Decapeptyl in microcapsules is more rapidly and more constantly efficient than LH-RH agonists given discontinuously by subcutaneous or intranasal route.
在第6位被D-色氨酸、D-丝氨酸（叔丁基）、D-亮氨酸或D-丙氨酸取代的促黄体生成素释放激素（LH-RH）类似物可强烈刺激促性腺细胞，随后导致LH-RH受体脱敏，进而阻断促性腺激素分泌并导致性腺功能减退。将一种设计为在肌肉注射后28天释放该肽的D-色氨酸-6-LH-RH缓释制剂（微囊化的达必佳）给予69名女孩和18名患有性早熟的男孩。在这两组患者中，促性腺激素和性腺类固醇的血浆水平在3周内受到抑制，而垂体对LH-RH的反应在7周内几乎完全消失。6个月内，第二性征以及性腺大小有明显改善。生长速度明显降低，而且在大多数儿童中，骨成熟被阻断。这项研究表明，微囊化的达必佳比通过皮下或鼻内途径间断给药的LH-RH激动剂起效更快且效果更持久。
