The place of meloxicam in the series of modern non-steroidal anti-inflammatory drugs

Abstract

The article describes the pharmacological characteristics of the first selective COX-2 inhibitormeloxicam, aspects of its mechanism of action, peculiarities of pharmacodynamics and indications, as well as the advantages of the drug compared to the classic and highly selective NSAIDs in termsNon-steroidal anti-inflammatory drugs (NSAIDs) take one of the most important places in clinical practice. The broad spectrum of NSAIDs is stipulated by the unique combination of pharmacological properties, which allow considering them one of the most widely used group of drugs [3]. NSAIDs have been successfully used in the therapy of most rheumatologic diseases. Due to their high clinical efficiency, impact on the main manifestations of the inflammatory process (pain, edema, fever), rapid clinical effect, the absence of reduction of the therapeutic efficiency during prolonged treatment they are used in cases of both inflammatory diseases − rheumatoid arthritis (RA), seronegative spondylarthrosis and in degenerative cases such as osteoarthritis (OA), osteochondrosis, diseases of paraarticular tissues [12,17].However, in spite of the obvious clinical efficiency, the use of NSAIDs has its limitations. The problem matter of the modern rheumatology is development of gastropathies against the background of the therapy by the drugs of this NSAID group; these gastropathies have a negative effect for adherence of patients to the therapy, and make them refuse from further therapy [46]. In some cases NSAID gastropathies may have real hazard for the life of patients [61]. For example, in the USA the death rate caused by the NSAID induced lesions of the gastrointestinal tract equals the death rate caused by the AIDS, and it is higher than the death rate caused by melanoma, bronchial asthma, carcinoma of the uterine cervix or lymphogranulomatosis [10]. In individuals, who take NSAIDs constantly, the frequency of erosive and ulcer changes is compared to the frequency of such pathology development in patients of the gastroenterological profile [69]. It is also generally known that different classes of NSAIDs are hepatotoxic, nephrotoxic and cardiotoxic in different degrees [4].Though the experience of the NSAID application has more than 100 years, the most important aspects of the mechanism of action of using these drugs were found out only in the 70-th of the last century [6]. It has been determined that the most important link of the mechanism of the NSAID action is their ability to inhibit the activity of cycloxygenase (COG) enzyme and thereby to reduce the synthesis of prostaglandins (PG) and other mediators of inflammation. According to the modern conception, COG is a multienzyme complex, including dioxygenase, isomerase, reductase and other components. COG is a hemoprotein located within the endoplasmic reticulum near the sites of arachidonic acid release from membranous phospholipids under the influence of phospholipase enzyme A2. In the presence of molecular oxygen and a number of co-factors COG catalyzes two key reactions in transf...