Rainsford K D
Agents Actions Suppl. 1977(1):59-70.
A multifactorial basis has been shown to exist in the development of gastric damage induced by aspirin and related N.S.A.I. drugs. Aspirin-induced gastric damage is characterized by a variety of physical and biochemical changes induced in the gastric mucosa which occur at different stages after administration of the drug. Aspirin only causes gastric ulceration and massive haemorrhage in the stomach when the stomach has been sensitized by the prior exposure to moderate stress conditions (which may resemble anxiety or psychologic stress). A model of ulcer development in which aspirin or other N.S.A.I. drugs are given to rats or pigs exposed to brief periods of stress has been described. Using this more sensitive assay procedures can be explored for reducing the gastric damaging effects of N.S.A.I. drugs. One such procedure involves chemical modification of the carboxylic acid moiety of aspirin.
已证明阿司匹林及相关非甾体抗炎药(NSAI)所致胃损伤的发生存在多因素基础。阿司匹林所致胃损伤的特征是胃黏膜出现多种物理和生化变化,这些变化在药物给药后的不同阶段发生。只有在胃先前暴露于中度应激条件(可能类似于焦虑或心理应激)而致敏后,阿司匹林才会导致胃溃疡和胃大量出血。已经描述了一种溃疡发展模型,即给暴露于短暂应激期的大鼠或猪服用阿司匹林或其他非甾体抗炎药。利用这种更敏感的检测方法,可以探索降低非甾体抗炎药胃损伤作用的方法。一种这样的方法涉及对阿司匹林羧酸部分进行化学修饰。