Haupt E, Küllmer K A, Schöffling K
Klin Wochenschr. 1977 Jul 15;55(14):695-703. doi: 10.1007/BF01478836.
Pharmacodynamic studies were performed with two new blood glucose lowering sulfonamides of high potency: gliquidone and gliflumide. The aim was to obtain equipotent doses on the basis of a maximum 30% blood glucose decrease in healthy normals (Ed 30) in order to compare the new compounds with the well known effects of tolbutamide and glibenclamide. Our investigations demonstrated a dose dependent blood glucose decrease with each sulfonylurea corresponding with the insulin levels after intravenous application. Gliquidone revealed a "tolbutamide-typed" dynamic both on insulin secretion and on blood glucose decrease whereas gliflumide showed a "glibenclamide-typed" reaction. The delayed and more prolonged insulin decrease, well known for glibenclamide, was even more distinct following gliflumide. Differences of insulin secretion after sulfonulureas can be observed only under intravenous conditions. Following oral application an only small increase of insulin can be noted when measured in peripheral blood.
对两种新型高效降血糖磺酰胺类药物格列喹酮和格列氟脲进行了药效学研究。目的是在健康正常人中基于最大30%的血糖降低(有效剂量30,Ed30)获得等效剂量,以便将新化合物与甲苯磺丁脲和格列本脲的已知作用进行比较。我们的研究表明,每种磺脲类药物静脉应用后血糖下降呈剂量依赖性,且与胰岛素水平相对应。格列喹酮在胰岛素分泌和血糖下降方面均表现出“甲苯磺丁脲型”动态,而格列氟脲则表现出“格列本脲型”反应。格列氟脲用药后,格列本脲所熟知的胰岛素下降延迟且持续时间更长的情况更为明显。磺脲类药物后胰岛素分泌的差异仅在静脉给药条件下才能观察到。口服给药后,在外周血中检测时只能观察到胰岛素有少量增加。