EFFECTIVE NONSTEROIDAL ANTIINFLAMMATORY DRUGS DEVOID OF GASTROINTESTINAL SIDE-EFFECTS - DO THEY REALLY EXIST

All nonsteroidal anti-inflammatory drugs (NSAIDs) cause gastrointestin al (GI) side effects. One focus of development was to design new drugs with reduced propensity for GI damage. With aspirin as the prototype, research efforts to develop NSAIDs with the efficacy but not the gast roduodenal damaging effects of aspirin have been partially successful. Techniques used to minimize gastric irritant potential include develo ping new drug classes, enteric coatings, nonacidic drugs, and prodrugs . Properties associated with the mucosal damaging effects of NSAIDs (p otent inhibition of prostaglandin synthesis, solubility at low pH, and acid characteristic) are not found in the newer prodrugs such as drox icam and nabumetone. Droxicam was developed as a prodrug of piroxicam with equal efficacy, in addition to improved GI tolerance. Prodrugs ma y offer new molecules with pharmacological profiles and efficacy to to xicity ratios more acceptable to clinicians and patients alike.