Nonsteroidal anti‐inflammatory drugs (NSAIDs) constitute a very important category of drugs that has therapeutic applications exploited since centuries. NSAIDs are a key composition for pharmacological management of acute and chronic pain. These drugs have enthralling evolution from the classic molecule called aspirin to the recently available coxibs, used for treatment of inflammatory conditions such as rheumatoid arthritis (RA) and osteoarthritis (OA). Almost all the drugs available in this category are associated with physiological side effects ranging from gastrointestinal to heart‐ and liver‐related diseases. As a result, the development and search for an ultimate magic drug molecule to treat inflammation continues to be an important face till date. The mechanism of action of NSAIDs relies mainly on inhibition of production of proinflammatory compounds by the action of cyclooxygenase (COX) enzymes. NSAIDs differ in their potency, duration of action and cause of gastric ulcer depending on their relative selectivity of COX enzymes (COX‐1/2). As recent developments, COX‐2‐selective inhibitors are being designed in search of safer and effective pain killer molecules, as COX‐1 inhibitors are associated with undesired side effects. In spite of the tremendous efforts being made since the past decade, the development of an effective and safe NSIAD to treat inflammatory conditions still presents key challenges.
Key Concepts
NSAIDs are most commonly used chemicals in the form of drugs.
Almost all NSIADs have adverse physiological effect on prolonged usage.
Novel category of NSAIDs to inhibit COX‐2 isoform is being developed.
Novel targets are needed to be explored for designing of safer drugs to control pain and inflammation.
More specific drugs are needed in order to avoid toxic effects.