Protective effect by anti-spasmodic activity of tiquizium bromide on NSAIDs-induced gastric injury in rats

• Published in: Japanese Journal of Pharmacology 1999, Vol.79 (suppl.1), p.207-207
• Main Authors: Tokunaga, Hirotaka, Yamauchi, Toshie, Mizutani, Fujie, Saito, Takaharu, Iwanaga, Yuji, Morikawa, Kouji, Nagata, Osamu, Kato, Hideo
• Format: Article
• Language: English
• ISSN: 0021-5198; 1347-3506
• DOI: 10.1016/S0021-5198(19)34840-1

NSAIDs produce gastric injury by the results of PGs deficiency and acid secretion. On the other hand, gastric hypercontraction mediated by cholinergic neurons might play an important role in the pathogenesis of indomethacin (IND)-induced gastric lesion. Aim： To compare the protective effect of tiquizium bromide (TQB), an anti-muscarinic agent, on NSAIDs-induced gastric injury with that of omeprazole (OPZ) and to confirm the spasmolyticity of TQB to IND-induced gastric hypermotility. Method： Ul-cerogenicity was estimated 7 hrs after oral co-administration of IND, diclofenac Na (DIC) or ibuprofen (IP) with TQB or OPZ in rats. Gastric motility was measured using a balloon inserted into the stomach in unanesthetized rats. Results： IND (12.5-50 mg/kg), DIC (25-100 mg/kg) and IP (25-200 mg/kg) produced mucosal injury. TQB (5-40 mg/ kg) dose-dependently prevented mucosal injury induced by IND (25 mg/kg), DIC (50 mg/kg) and IP (200 mg/kg). OPZ (5-20 mg/kg) also prevented mucosal injury induced by IND and DIC, but not by IP. IND (25 mg/kg,s.c.), DIC (100 mg/kg,s.c.) and IP (100 mg/kg,s.c.) increased gastric motility, and TQB (30mg/kg,i.d.), which didn't inhibit gastric acid secretion, reduced gastric hypermotility by IND. Conclusion： These data suggest that TQB may protect stomach from gastric injury induced by NSAIDs, in part, through the anti-spasmodic activity and that TQB will be suitable for co-therapy to prevent NSAIDs gastropathy.