Prospects for Reducing Gastrotoxicity of Anti-Inflammatory and Analgesic Therapy While Using Amtolmetin Guacil

The most important problem of non-steroid anti-inflammatory drugs (NSAIDs) is a high risk of ulcerogenicity. It is possible to reduce it by the increase in gastric mucosa concentrations of gastroprotective NO. New NSAIDs Amtolmetin guacil (AMG) was registered in Russia in 2013. It is positioned as an effective medicine with gastroprotective action. AMG stimulates capsaicinoid receptors and accumulates NO in the stomach. However, the data on the effectiveness and safety of AMG are few. During its metabolism highly ulcerogenic Tolmetin is formed. The purpose of our research was to study the anti-inflammatory, analgesic and ulcerogenic effect of AMG after intragastric administration. The research was carried out on white nonlinear mice and rats of both sexes. Our study showed that AMG effectively reduced the severity of carrageenan edema of the rat's paw and reduced the number of acetic cramps in mice. Gastric mucosa of most animals was without pathological changes, single shallow erosions without infiltration were found in 32% of animals after administration during 4 days of AMG to rats at a dose of 200 mg/kg once a day. Diclofenac in the same conditions at a dose of 10 mg/kg caused deep defects in 75% of rats. AMG showed pronounced analgesic and anti-inflammatory effect. Our results also confirmed the advantage of AMG compared to diclofenac in its effect on the gastric mucosa.