Makarov V A, Kiril'chuk L P, Kalganova G I, Astakhova V G, Sakhnenko N V
Farmakol Toksikol. 1978 May-Jun;41(3):319-23.
In in vivo experiments with rats anapriline (1 mg/kg) greatly reduced the level of gastrically introduced norsulfazol (200 mg/kg) in the blood, liver, kidneys, stomach, small and large intestine both in healthy rats as well as in those with experimental gastritis provoked by acetylsalicylic acid twice introduced into the stomach. Under the influence of anapriline the acetylization of norsulfazol in the liver would become 4.7 times less intensive. Dihydroergotamin (10 mg/kg) did not influence the absorption, distribution and acetylization of norsulfazol. Reserpine (10 mg/kg) brought down the amount of free norsulfazol in the gastro-intestinal tract and reduced the quantity of acetylized norsulfazol in the blood, stomach, small and large intestines. The acetylization changes in the kidneys were not significant. In the springtime the intensity of the norsulfazol acetylization increases by more than twice. The described results bear witness to the participation of beta-adrenoreceptors in the transport and metabolism of norsulfazol.
在对大鼠进行的体内实验中，心得安（1毫克/千克）显著降低了无论是健康大鼠还是经胃内两次注入乙酰水杨酸引发实验性胃炎的大鼠，胃内注入的诺氟沙星（200毫克/千克）在血液、肝脏、肾脏、胃、小肠和大肠中的水平。在心得安的影响下，诺氟沙星在肝脏中的乙酰化强度降低4.7倍。双氢麦角胺（10毫克/千克）不影响诺氟沙星的吸收、分布和乙酰化。利血平（10毫克/千克）降低了胃肠道中游离诺氟沙星的量，并减少了血液、胃、小肠和大肠中乙酰化诺氟沙星的量。肾脏中的乙酰化变化不显著。在春季，诺氟沙星乙酰化强度增加两倍多。所述结果证明β-肾上腺素受体参与了诺氟沙星的转运和代谢。
