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对乙酰氨基酚对吲哚美辛在大鼠胃中侵蚀活性的影响。

The influence of paracetamol on the erosive activity of indomethacin in the rat stomach.

作者信息

van Kolfschoten A A, Zandberg P, Jager L P, van Noordwijk J

出版信息

Agents Actions. 1982 Apr;12(1-2):247-53. doi: 10.1007/BF01965155.

Abstract

Indomethacin induced erosions in the glandular part of the rat stomach in a dose-dependent manner. Gastric erosions became apparent about 15 min after administration of indomethacin and the damage was maximal at about 4 h. The erosive activity of indomethacin administered subcutaneously was similar to that after oral administration, confirming the data of other authors. The erosive activity of subcutaneously applied aspirin, however, was far less than that of oral administered aspirin and it was not dose dependent. In a dose-dependent manner, paracetamol reduced the incidence of gastric erosions induced with indomethacin; this effect was independent of the route of administration of either drug. Paracetamol was also effective when given 0.5 or 1 h before indomethacin. Orally administered paracetamol also reduced the incidence of gastric erosions induced with aspirin but after subcutaneous administration, paracetamol had no protective effect. The differences between the erosive activities of indomethacin and aspirin are discussed with emphasis on the differentiating influence of paracetamol on the incidence of gastric erosions. Direct contact with the mucosa is apparently more important for the erosive activity of aspirin than for that of indomethacin. Possible mechanisms by which paracetamol exerts its protective activity are proposed.

摘要

吲哚美辛以剂量依赖的方式诱导大鼠胃腺部出现糜烂。给予吲哚美辛后约15分钟,胃糜烂变得明显,损伤在约4小时时达到最大程度。皮下注射吲哚美辛的糜烂活性与口服给药后的相似,证实了其他作者的数据。然而,皮下应用阿司匹林的糜烂活性远低于口服阿司匹林,且不具有剂量依赖性。对乙酰氨基酚以剂量依赖的方式降低了吲哚美辛诱导的胃糜烂发生率;这种作用与两种药物的给药途径无关。在吲哚美辛给药前0.5或1小时给予对乙酰氨基酚也有效。口服对乙酰氨基酚也降低了阿司匹林诱导的胃糜烂发生率,但皮下给药后,对乙酰氨基酚没有保护作用。讨论了吲哚美辛和阿司匹林糜烂活性的差异,重点在于对乙酰氨基酚对胃糜烂发生率的不同影响。对于阿司匹林的糜烂活性而言,与黏膜的直接接触显然比对吲哚美辛更为重要。提出了对乙酰氨基酚发挥其保护活性的可能机制。

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