Gudat U, Heinemann L
Klinik für Stoffwechselkrankheiten und Ernährung, Heinrich-Heine-Universität Düsseldorf.
Arzneimittelforschung. 1996 Jun;46(6):606-9.
Sulfonylureas predispose to hypoglycaemia during and after exercise. The hypoglycaemic effect of the novel sulfonylurea glimepiride (G; CAS 93479-97-1) in male healthy volunteers under these conditions. Each subject was exposed to three experimental situations, administration of 3 mg G and rest, administration of 3 mg G and 60 min of bicycle ergometry (E) (work load adjusted to a heart rate of 120 bpm), or placebo (P) and bicycle ergometry as mentioned. Each of these was preceded and followed by 60 min of physical rest. Base line glycaemia was comparable (PE 83 +/- 8 mg/dl, GR 84 +/- 5 mg/dl, GE 86 +/- 7 mg/dl) and fell during GR to 63 +/- 6 mg/dl after 150 min. During GE glycaemia ceased to decline after 30 min exercise, and rose thereafter reaching values comparable to PE after 150 min (80 +/- 8 vs. 82 +/- 7 mg/dl). Serum insulin concentrations rose during exercise following administration of G to 6-7 microU/ml (AUC during the period 60-120 min after administration: GE 371 +/- 81 microU/ml.60 min, GR 414 +/- 77 microU/ml.60 min), and fell during PE to 4 microU/ml (265 +/- 49 microU/ml.60; p < 0.001 vs. GE and GR). During GE serum insulin concentrations fell to 6 microU/ml at the end of exercise and thereafter (AUC during the period 120-180 min after administration: 340 +/- 82 microU/ml.60 min), whereas they remained at 7 microU/ml during GR (399 +/- 109 microU/ml.60 min; p = 0.087 vs. GE). In conclusion, exercise blunts the hypoglycaemic effect of glimepiride in healthy individuals.
磺脲类药物在运动期间及运动后易引发低血糖。研究新型磺脲类药物格列美脲(G;化学物质登记号93479 - 97 - 1)在这些情况下对男性健康志愿者的降血糖作用。每位受试者经历三种实验情况:服用3毫克G并休息、服用3毫克G并进行60分钟的自行车测力计运动(E)(工作负荷调整至心率120次/分钟),或服用安慰剂(P)并进行上述自行车测力计运动。每种情况前后均有60分钟的身体休息。基线血糖水平相当(安慰剂组83±8毫克/分升,格列美脲组84±5毫克/分升,运动加格列美脲组86±7毫克/分升),在格列美脲组中,150分钟后血糖降至63±6毫克/分升。在运动加格列美脲组中,运动30分钟后血糖停止下降,此后上升,150分钟后达到与安慰剂组相当的值(80±8对82±7毫克/分升)。服用G后运动期间血清胰岛素浓度升至6 - 7微单位/毫升(给药后60 - 120分钟期间的曲线下面积:运动加格列美脲组371±81微单位/毫升·60分钟,格列美脲组414±77微单位/毫升·60分钟),在安慰剂组运动期间降至4微单位/毫升(265±49微单位/毫升·60分钟;与运动加格列美脲组和格列美脲组相比,p<0.001)。在运动加格列美脲组中,运动结束时及之后血清胰岛素浓度降至6微单位/毫升(给药后120 - 180分钟期间的曲线下面积:340±82微单位/毫升·60分钟),而在格列美脲组中仍保持在7微单位/毫升(399±109微单位/毫升·60分钟;与运动加格列美脲组相比,p = 0.087)。总之,运动减弱了格列美脲对健康个体的降血糖作用。