Selective Cyclooxygenase Inhibitors: Current Status
Ravindran Nandakishore, Prasanna R. Yalavarthi, Yengala R. Kiran and Malepati Rajapranathi
Affiliation: Department of Pharmaceutics, Sree Vidyanikethan College of Pharmacy, Andhra Pradesh 517102, India.
For ages aspirin has established its value as an analgesic, anti-inflammatory drug, but in 1938, it was found to
be a causative factor of gastric inflammation (ulcer). Later discovered non-steroidal anti-inflammatory drugs (NSAIDs)
were found effective as aspirin but failed to overcome the goal of safer aspirin. As the method of prostaglandin inhibition
through COX is a common mechanism to both the wanted and unwanted effects of aspirin and non-aspirin NSAIDs, the
COX enzyme becomes a target for drug designers for the development of the “safe aspirin”. In the late 1990s, a new class
of drug molecules collectively known as selective inhibitors of cyclooxygenase-2(Coxibs) was developed for the treatment
of pain and inflammation. Coxibs developed were as efficacious as the common NSAIDs, but they are devoid of major
side effect, the gastrointestinal bleeding. This review presents an overview on all the discovered COX-2 inhibitors,
their physiological role, side effects and reasons of their withdrawal.
Keywords: Coxib, cyclooxygenase, gastric bleeding, prostaglandin.
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