Shuba N.M.

Summary. Objectives. To review the literature and provide an update on the mechanisms of action and therapeutic uses of nonsteroidal anti-inflammatory drugs (NSAIDs). Methods. We performed PubMed database searches for relevant studies in the literature. Searches encompassed mechanisms of action NSAIDs and clinical applications in medical conditions. Results. This article is devoted to the analysis of the search of optimal anti-­inflammatory and analgesic medicines (from NSAIDs) to cyclooxygenase (COX)-2 specific). NSAIDs, which act via inhibition of the COX isozymes, were disco­vered more than 100 years ago. They remain a key component of the pharmacological management of acute and chronic pain. It is also shown that NSAIDs safety determines not only by the degree of their COX-2-selectivity. A better understanding of the inhibitory activity and COX-1/COX-2 selectivity of an NSAID at therapeutic doses, based on pharmacokinetic and pharmacodynamic properties (eg, inhibitory dose, absorption, plasma versus tissue distribution, and elimination), and the impact on drug tolerability and safety can guide the selection of appropriate NSAIDs for pain management. There are NSAIDs that have a number of additional, non-COX-dependent effects, which play significant role in treatment of a variety of nosologies more than only COX inhibition. Each patient’s clinical background, including gastrointestinal and cardiovascular risk factors, should be taken into account when selecting appropriate NSAIDs. Conclusion. Today, diclofenac is the gold standard of the­rapy for patients with pain in inflammatory diseases of the musculoskeletal system, the use of which ensures high treatment efficiency along with an acceptable safety profile. Recent studies add more and more arguments in favor of the use of diclofenac both from the standpoint of the effectiveness of treatment and in the context of its complex effect on arachidonic acid metabolism enzymes and a new risk management strategy for adverse reactions. Further understanding of the mechanisms of action underlying the therapeutic efficacy will lead to its potential use in a variety of conditions.

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