Non-steroidal anti-inflammatory drugs are widely used in the treatment of acute and chronic inflammation and pain, because they work by inhibiting cyclooxygenase (COX) and blocking the conversion of arachidonic acid into prostaglandins, so they are also known as cyclooxygenase inhibitors. Human application of cyclooxygenase inhibitors has more than 150 years of history, cyclooxygenase inhibitors have become an important indispensable drug in people’s daily life, is the world’s most widely used, the application of one of the largest varieties of medicine, about 34 million people in the world every day in the use of non-steroidal anti-inflammatory drugs, for anti-inflammatory, anti-rheumatic, pain relief and anti-coagulant treatment, in China is second only to anti-infective drugs It is the second largest class of drugs used in China after anti-infective drugs. The development of cyclooxygenase inhibitors began in 1899, the appearance of aspirin from Bayer in Germany marked the beginning of the era of modern anti-inflammatory treatment, and in the following half century, it has been the main drug for anti-inflammatory treatment. 1950s, the emergence of POTAXON, the 1960s marketed indomethacin, since the 1970s launched ibuprofen, diclofenac, piroxicam, 80s, sulforaphane, nabumetone, etc., all of which are used in anti-inflammatory treatment. Nabumetone, etc., all of which are used in clinical applications because of their better efficacy. However, they still have more adverse effects, especially damage to the gastrointestinal, liver, kidney and bone marrow. Scientists continue to explore the mechanism of action of NSAIDs in order to develop NSAIDs with better efficacy and less side effects. 1971, experts explained the mechanism of action of NSAIDs with the theory of cyclooxygenase, prostaglandins are inflammatory mediators and are related to pain production, and inhibition of COX produces anti-inflammatory and analgesic effects. 1991, it was found that cyclooxygenase exists in COX-1 and COX-1 is a structural enzyme, which is an elemental enzyme required to maintain human physiology; COX-2 is an inducible enzyme, which is mainly present at the site of inflammation and is involved in the synthesis of inflammatory prostaglandins. Adverse effects produced by cyclooxygenase inhibitors such as gastrointestinal irritation and kidney damage are also due to the elimination of physiological prostaglandins that protect the stomach and kidneys. Cyclooxygenase inhibitors are classified as non-selective COX-2 inhibitors and selective COX-2 inhibitors according to the degree of COX-2 inhibition. Studies have shown that the stronger the selectivity of the drug for COX-2 inhibition, the weaker the side effect of inducing gastric ulcer, while non-selective COX-2 inhibitors such as aspirin and indomethacin, which cause more serious gastric ulcer, have a weaker effect on COX-2 inhibition, but on the contrary, have a strong effect on COX-1 inhibition. The development of selective COX-2 inhibitors has not only opened up new avenues of anti-inflammatory and analgesic treatment, but such drugs have also shown therapeutic effects in antitumor, preventing preterm birth, and delaying the progression of progeria lesions. Compared to conventional NSAIDs, the incidence of gastrointestinal adverse reactions to celecoxib, rofecoxib, and other celecoxib drugs, which are selective COX-2 inhibitors, is significantly lower, but a 3-year study entitled “Prevention of adenomatous polyps with rofecoxib” suggests that in patients taking rofecoxib after 18 months, the incidence of myocardial disease associated with rofecoxib use is significantly lower. The results forced Merck Sharp & Dohme to recall rofecoxib worldwide. An FDA advisory panel reevaluated COX-2 inhibitors and concluded unanimously that the entire class of COX-2 inhibitors had an increased potential for cardiovascular disease and that such drugs needed to be labeled with cardiovascular side effect warnings. Studies now show that COX-1 and COX-2 cannot be judged simply as “good” or “bad”; COX-1 is not all good and COX-2 is not all bad. A study found that naproxen, a traditional NSAID, could also increase the risk of cardiovascular disease, and the FDA also recommended caution with naproxen. While the gastrointestinal safety of cyclooxygenase inhibitors has been a century-old challenge, cardiovascular safety has only been recognized with the introduction of selective NSAIDs. Both traditional non-selective COX-2 inhibitors and selective COX-2 inhibitors have varying degrees of side effects, and the chances of serious side effects are greatly increased especially in people with high-risk factors who take cyclooxygenase inhibitors should choose the right cyclooxygenase inhibitor to bring out the efficacy of cyclooxygenase inhibitors and prevent and treat the damage caused by cyclooxygenase inhibitors in humans.