Cyclooxygenase-2 inhibitors: introduction to a new class of drugs
نویسنده
چکیده
he use of nonsteroidal anti-inflammatory drugs (NSAIDs) has progressively increased, due in part to their availability without a prescription. Gastrointestinal-related side effects of the NSAIDs have been implicated in approximately 7600 deaths and 76,000 hospitalizations annually in the USA alone (1). Such statistics have led to the pursuit of new agents to treat pain syndromes. Initially, agents that protected the gastric mucosa were employed. For example, misoprostol, a synthetic prostaglandin analog, was used, but side effects were seen when therapeutically effective dosages were given, so its clinical application was limited. Histamine antagonists also have been tested with varying degrees of success. An acceptable alternative to NSAIDs may be proton-pump inhibitors, but further study is needed with this class of drugs. The most promising development has been the cyclooxygenase (COX)-2 selective agents, but definitive reports in the literature are lacking (2, 3).
منابع مشابه
Designing and Synthesis of Novel Celecoxib Derivatives with Aminosulfonylmethyl and Azidomethyl Substituents as Selective Cyclooxygenase-2 Inhibitors
Introduction: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are used in treating pathologic conditions such as fever, pain and inflammation by inhibiting cyclooxygenase and consequently prostaglandin production. Recently , the discovery of different isoforms of this enzyme, Cyclooxygenase-1 (COX-1) and Cyclooxygense-2 (COX-2), has led to the synthesis and introduction of novel drugs with selec...
متن کاملDesigning and Synthesis of Novel Celecoxib Derivatives with Aminosulfonylmethyl and Azidomethyl Substituents as Selective Cyclooxygenase-2 Inhibitors
Introduction: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are used in treating pathologic conditions such as fever, pain and inflammation by inhibiting cyclooxygenase and consequently prostaglandin production. Recently , the discovery of different isoforms of this enzyme, Cyclooxygenase-1 (COX-1) andCyclooxygense-2 (COX-2), has led to the synthesis and introduction of novel drugs with select...
متن کاملSelective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships
Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...
متن کاملSelective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships
Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...
متن کاملNew cyclooxygenase inhibitors.
INTRODUCTION The discovery of the two isoforms of cyclooxygenase (COX-1 and COX-2) has paved the way for the development of a new class of non-steroidal anti-inflammatory drugs (NSAIDs). The COX-2 inhibitors have shown comparable efficacy to the traditional NSAIDs with less gastrointestinal side effects in major clinical studies. The aims of this paper are to provide a brief historical backgrou...
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