Analgésicos inibidores específicos da ciclooxigenase-2: avan?os terapêuticos

摘要

BACKGROUND AND OBJECTIVES: Nonsteroidal Anti-inflammatory Drugs (NSAIDs) are among the most widely prescribed drugs, including for Anesthesiology. This review aimed at discussing some current cycloxygenase biochemical aspects, which have provided the basis for the development of new analgesic and anti-inflammatory drugs. CONTENTS: These drugs primarily act by inhibiting cycloxygenase (COX), which is the key-enzyme catalyzing the conversion of arachidonic acid into prostaglandins and thromboxane. At least two COX isoforms have already been identified: COX-1, which is constitutively expressed in most tissues, and the inducible enzyme COX-2, which is primarily found in inflammatory cells and tissues. The discovery of COX-2 has enabled the development of more selective drugs to decrease inflammation without affecting COX-1 that protects stomach and kidneys and giving origin to a new generation of anti-inflammatory compounds called specific COX-2 inhibitors. CONCLUSIONS: Although there is significantly lower gastrointestinal toxicity in patients treated with selective COX-2 inhibitors, other severe adverse effects have been observed, including renal failure and cardiovascular effects, such as myocardial infarction acute and thrombosis. Despite these potential side effects, these new drugs are being tested in different clinical conditions, especially in cancer prevention and Alzheimer's disease.