Gartner A H
J Am Dent Assoc. 1976 Jul;93(1):111-7. doi: 10.14219/jada.archive.1976.0591.
Aspirin-induced gastritis and gastrointestinal hemorrhage were reviewed and discussed on the basis of currently available literature. Acute hemorrhagic gastritis occurs in from 50% to 70% of all patients taking aspirin, is not directly related to dose size, and can be severe enough to cause death in a few cases. No tolerance appears to ever develop. The mechanism that causes this bleeding is not definite, but the back diffusion of H+ ions accross the gastric barrier seems to bear primary responsibility, with physical erosion, prolonged platelet bleeding, and the effect of low pH values also being possible explanations. There appears to be less acid present in the stomach when bleeding occurs, but this is a masking effect of the aspirin that causes increased absorption of the H+ ions. Factors important in determining pharmaceutical formulation are method of administration, particle size of the aspirin, duration of contact between the drug and the mucosa, presence of buffers in the drug to raise the gastric pH, dissolution rate of the drug in the stomach, and ionization characteristics of the drug itself. Gastrointestinal blood loss caused by aspirin can be minimized by administering the drug in one of these forms:--a dilute solution of acetylsalicylate;--an intravenously injected solution;--a very rapidly dissolving and rapidly absorbed tablet;--a solution with sufficiently large amounts of antacid added;--a fine-grain, highly buffered aspirin tablet;--an enteric-coated tablet that does not dissolve in the stomach; or--an aspirin substitute such as acetaminophen.
基于现有文献,对阿司匹林诱发的胃炎和胃肠道出血进行了综述与讨论。在所有服用阿司匹林的患者中,50%至70%会发生急性出血性胃炎,这与剂量大小无直接关系,在少数情况下可能严重到足以导致死亡。似乎从未产生耐受性。导致这种出血的机制尚不确定,但H⁺离子跨胃黏膜屏障的反向扩散似乎起主要作用,物理侵蚀、血小板出血时间延长以及低pH值的影响也可能是解释原因。出血发生时胃内的酸似乎较少,但这是阿司匹林的一种掩盖效应,会导致H⁺离子吸收增加。在确定药物剂型时重要的因素包括给药方法、阿司匹林的颗粒大小、药物与黏膜的接触时间、药物中用于提高胃pH值的缓冲剂的存在、药物在胃中的溶解速率以及药物本身的离子化特性。通过以下形式之一给药可将阿司匹林引起的胃肠道失血降至最低:——乙酰水杨酸稀溶液;——静脉注射溶液;——非常快速溶解和吸收的片剂;——添加了足够量抗酸剂的溶液;——细颗粒、高度缓冲的阿司匹林片剂;——不在胃中溶解的肠溶包衣片剂;或者——对乙酰氨基酚等阿司匹林替代品。