Nonsteroidal anti-inflammation drugs

In addition to their beneficial effects, some medications may actually cause cellular injury and disease. An example of this phenomenon involves nonsteroidal anti-inflammatory drugs (NSAIDS). These drugs include aspirin (a derivative of salicylic acid), ibuprofen (arylpropionic acid, Advil ), and acetaminophen (para-aminophenol derivative, Tylenol ). Because of their beneficial pharmacological effects, consumption of these agents has increased significantly in recent years. NSAIDS have the ability to treat fever, pain, acute inflammation, and chronic inflammatory diseases such as arthritis. They are also used prophylactically to prevent heart disease, stroke, and colon cancer. 

COX-2 Inhibitor Celecoxib (Celebrex, Pfizer) inhibits the enzyme COX-2, which is involved in pain and inflammation, but it has no effect on the COX-1 enzyme, which helps to maintain stomach lining. It is prescribed for the relief of pain and symptoms of osteoarthritis and rheumatoid arthritis. Previously, nonsteroidal anti-inflammatory drugs (NSAIDs) were used. NSAIDs inhibit both COX-1 and COX-2 enzymes and cause stomach bleeding (see Case Study 2). 

Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used to treat the signs and symptoms of inflammation, particularly arthritic pain. - It is mainly through the inhibition of cyclooxygenases (COXs), key enzymes in prostaglandin (PG) biosynthesis from arachidonic acid, that NSAIDs exert their anti-inflammatory effect. 

As was already mentioned, piroxicam also is a nonsteroidal, anti-inflammatory drug. It is used in inflammatory and degenerative diseases of the musculoskeletal system that are accompanied by painful symptoms. It is used for rheumatic heart disease, nonspecific infectious polyarthritis, gouty arthritis, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, arthrosis, back pain, nenralgia, myalgia, and other diseases associated with inflammation. Synonyms for piroxicam are feldene, dexicam, roxenan, and others. 

Interestingly, nonsteroidal anti-inflammatory drugs, such as ketoprofen 25 (Scheme 17), which are used to treat a wide range of ailments, such as inflammation, pain, and fever, also undergo photodecarboxylation. Unfortunately, many of these drugs have been shown to have cutaneous side effects, which are caused by their photodecomposition. Various research groups have demonstrated that irradiation of ketoprofen 25 yields 26 under anaerobic conditions, whereas in oxygen-saturated... 

Figure 8.9 Prostaglandins and leukotrienes are potent eicosanoid lipid mediators, derived from phospholipase-released arachidonic acids, that are involved in numerous homeostatic biological functions and inflammation. They are generated by cyclooxygenase isozymes and 5-lipoxygenase, respectively, and their biosynthesis and pharmacological actions are inhibited by clinically relevant nonsteroidal anti-inflammatory drugs.

Reduction of inflammation with nonsteroidal anti-inflammatory drugs (NSAIDs) often results in relief of pain for significant periods. Furthermore, most of the nonopioid analgesics (aspirin, etc) have anti-inflammatory effects, so they are appropriate for the treatment of both acute and chronic inflammatory conditions. 

Clinical use Niflumic acid (Auclair et al., 1989) is a nonsteroidal anti-inflammatory drug used for the treatment of inflammation and pain in musculoskeletal and joint disorders such as rheumatoid arthritis as well as traumatic and postoperative pain. Niflumic acid is used in oral, rectal or topical preparations (up to 750 mg/day). 

Morini, G., Grandi, D., Krause, M., Schunack, W., 1997. Gastric mucosal injury by nonsteroidal anti-inflammatory drugs is reduced by (R)-a-methylhistamine and its prodrugs in the rat. Inflamm. Res. 46 (Suppl. 1), S101-S102. 

During the acute phase of a viral infection of the thyroid gland, there is destruction of thyroid parenchyma with transient release of stored thyroid hormones. A similar state may occur in patients with Hashimoto s thyroiditis. These episodes of transient thyrotoxicosis have been termed "spontaneously resolving hyperthyroidism." Supportive therapy is usually all that is necessary, such as propranolol for tachycardia and aspirin or nonsteroidal anti-inflammatory drugs to control local pain and fever. Corticosteroids may be necessary in severe cases to control the inflammation. 

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