Anti-inflammatory and antiplatelet effects of amtolmetin guacyl, a new gastroprotective non-steroidal anti-inflammatory drug.

Abstract

Amtolmetin guacyl (CAS 873344-06-7, MED 15) is a non-steroidal anti-inflammatory drug (NSAID) which has shown gastroprotective effects attributable to capsaicin receptor stimulation through the presence of a vanillic moiety in its molecular structure. The present paper further defines the anti-inflammatory activity of the product in an exudative rat model and in an arthritic rat model. The results obtained from both studies demonstrate anti-inflammatory effects comparable to those of the traditional NSAIDs in use. This study also demonstrated that amtolmetin guacyl possesses high antiaggregatory activity comparable to acetylsalicylic acid (CAS 50-78-2), when expressed as inhibition of blood thromboxane synthesis; the in vitro antiaggregatory activity was decidedly superior to that expressed by either acetylsalicylic acid or tolmetin (CAS 26171-23-3) (a traditional NSAID and metabolite of amtolmetin guacyl). The characteristics of gastroprotection along with control of inflammation and platelet aggregation render amtolmetin guacyl recommendable in the treatment of inflammatory and thromboembolic conditions where long-term therapy is required.