Choi C J, Shin D B, Kim S W, Yang I M, Kim J W, Kim Y S, Choi Y K
Korean J Intern Med. 1987 Jul;2(2):176-83. doi: 10.3904/kjim.1987.2.2.176.
Somatostatin is a potent inhibitor of the growth hormone (GH) secretion. However, the short half-life as well as the rebound phenomenon have rendered it impractical for therapeutic use. SMS 201-995, a long acting somatostatin analogue, has been shown to have a long acting inhibitor effect on GH secretion. To observe its suppressive effect on GH secretion and to determine whether it has a diabetogenic effect and whether it can suppress the paradoxical response of GH, we administered 50 μg of SMS 201-995 subcutaneously to five acromegalic patients before breakfast. Serum GH was reduced 85% from the basal concentration four hours after the administration of SMS 201-995 and remained below the basal level for up to eight hours without a rebound phenomenon. The pattern of glucose intolerance was observed in 4 out of 5 patients but not in the normal controls; it seemed to be caused by exessive GH. Also SMS 201-995 did not suppress postprandial insulin and glucagon secretion. In addition, we observed that SMS 201-995 suppressed the paradoxical release of GH to TRH in two of three patients who showed a paradoxical response. Unexpectedly one patient who had no paradoxical response before the administration of SMS 201-995 showed a paradoxical response. In conclusion, we suggest that more than 50 μg of SMS 201-995 should be given at least 3 times a day for adequate adjunctive therapy of acromegaly. The SMS 201-995 has no diabetogenic effect.
生长抑素是生长激素(GH)分泌的强效抑制剂。然而,其半衰期短以及存在反弹现象,使其在治疗应用中不切实际。SMS 201-995是一种长效生长抑素类似物,已被证明对GH分泌具有长效抑制作用。为观察其对GH分泌的抑制作用,并确定其是否具有致糖尿病作用以及是否能抑制GH的反常反应,我们在早餐前给5例肢端肥大症患者皮下注射了50μg的SMS 201-995。注射SMS 201-995后4小时,血清GH从基础浓度降低了85%,并在长达8小时内保持低于基础水平,无反弹现象。5例患者中有4例观察到葡萄糖耐量异常模式,但正常对照组未观察到;这似乎是由过量的GH引起的。此外,SMS 201-995并未抑制餐后胰岛素和胰高血糖素的分泌。另外,我们观察到,在3例出现反常反应的患者中,有2例SMS 201-995抑制了GH对促甲状腺激素释放激素(TRH)的反常释放。出乎意料的是,1例在注射SMS 201-995前无反常反应的患者出现了反常反应。总之,我们建议,为了对肢端肥大症进行充分的辅助治疗,每天应至少3次给予超过50μg的SMS 201-995。SMS 201-995没有致糖尿病作用。