Conforti A, Donini M, Brocco G, Del Soldato P, Benoni G, Cuzzolin L
Institute of Pharmacology, University of Verona, Italy.
Agents Actions. 1993 Nov;40(3-4):176-80. doi: 10.1007/BF01984058.
Diclofenac and its derivative nitrofenac were compared to test their anti-inflammatory efficacy and gastrointestinal toxicity in rats. A similar good anti-inflammatory activity of the two drugs was observed in carrageenan oedema and a marked gastrointestinal toxicity was induced by diclofenac, while nitrofenac failed to produce gastric damage even with very high doses (50 and 100 mg/kg). The lack of the gastric ulcers in rats treated with nitrofenac could be due to the absorption of the drug as an inactive inhibitor of PG synthesis and/or to the fact that probably nitric oxide is released in the intestine and plays an important protective role in maintaining the tissue integrity.
比较双氯芬酸及其衍生物硝芬酸在大鼠体内的抗炎功效和胃肠道毒性。在角叉菜胶性水肿实验中观察到两种药物具有相似的良好抗炎活性,双氯芬酸可诱导明显的胃肠道毒性,而硝芬酸即使使用非常高的剂量(50和100毫克/千克)也不会产生胃损伤。用硝芬酸治疗的大鼠未出现胃溃疡,可能是因为该药物作为PG合成的非活性抑制剂被吸收,和/或可能是因为一氧化氮在肠道中释放并在维持组织完整性方面发挥重要的保护作用。