Nonsteroidal anti-inflammatory drugs agents

Drugs (nonsteroidal anti-inflammatory, antineopiastic agents, aicohoi) Denatured proteins (amino acid analogs)... 

Simple analgesics such as acetaminophen and nonsteroidal anti-inflammatory drugs (NSAIDs) are first-line agents for treating OA (Table 55-2). 

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. 

Many nonsteroidal anti-inflammatory drugs (NSAIDs) are substituted 2-arylpropionic acids. Most NSAIDs also have a chiral carbon next to the carboxylate and are administered as a racemic mixture of the two enantiomers. In general, the (S)-enantiomcr is responsible for most of the antiinflammatory activity of these agents. It was found that the (/ -enantiomer is converted to the (S)-enantiomer but the reverse does not occur (23). As with amino acid conjugation, the pathway involves reaction with ATP to form an AMP ester, which is, in turn, converted to a Co-A ester, and it is the Co-A ester that undergoes chiral inversion (Fig. 7.14). Substrates include ibuprofen, naproxen, and fenoprofen. 

The compound 5-[5-(4-chlorophenyl)furan-2-yl]-2,3,4,5-tetrahydrofuran-2-one (F-1044, 7.85) is a nonsteroidal anti-inflammatory agent possibly acting via a ring-opened hydroxybutyric acid metabolite. To examine this hypothesis, F-1044 was submitted to extensive in vivo testing, which revealed potent activities and a unique pharmacological profile markedly different from that of acidic nonsteroidal anti-inflammatory drugs [169], These results have been interpreted to mean that part or most of the observed effects of F-... 

Anti-neoplastic activity of UDCA was demonstrated first in the context of ulcerative colitis-associated colorectal carcinogenesis. Subsequently, encouraging (but not definitive) results have been obtained in clinical trials of UDCA for prevention of sporadic colorectal adenoma recurrence, which should prompt further evaluation of UDCA for polyp prevention, particularly given its excellent safety profile compared with other candidate chemoprevention agents such as the nonsteroidal anti-inflammatory drugs. 

Significant research has centered on the preparation and investigation of oxicam derivatives as pharmaceutical agents. This interest was fueled by the successes of the nonsteroidal anti-inflammatory drugs (NSAIDs) piroxicam (Feldene ) 21, meloxicam (Mobic ) 22, and tenoxicam 23 (Figure 24). 

The combination of MAOIs with meperidine, and perhaps with other phenylpiperidine analgesics, also has been implicated in fatal reactions attributed to the serotonin syndrome. Aspirin, nonsteroidal anti-inflammatory drugs, and acetaminophen should be used for mild to moderate pain. Of the narcotic agents, codeine and morphine are safe in combination with MAOIs, although doses may need to be lower than usual. 

Nonsteroidal anti-inflammatory drugs [P] Inhibition of platelet function, gastric erosions some agents increase hypoprothrombinemic response (unlikely with diclofenac, ibuprofen, or naproxen). 

Nonsteroidal anti-inflammatory drugs are widely used in veterinary practice and are, therefore, of growing interest to the residue control of animal-derived food. Veterinarians are seeing an increased use of anti-inflammatory agents, administered with or without antibiotics, for treatment of mastitis because of the increase in efficiency of these agents over antibiotics alone. 

Garcia Rodriguez LA, Hernandez-Diaz S. The risk of upper gastrointestinal complications associated with nonsteroidal anti-inflammatory drugs, glucocorticoids, acetaminophen, and combinations of these agents. Arthritis Res 2001 3(2) 98-101. 

The primary adverse effect of intravenous cidofovir is a dose-dependent nephrotoxicity. Concurrent administration of other potentially nephrotoxic agents (eg, amphotericin B, aminoglycosides, nonsteroidal anti-inflammatory drugs, pentamidine, foscarnet) should be avoided. Prior administration of foscarnet may increase the risk of nephrotoxicity. Other potential side effects include uveitis, decreased intraocular pressure, and probenecid-related hypersensitivity reactions. Neutropenia and metabolic acidosis are rare. The drug caused mammary adenocarcinomas in rats and is embryotoxic. 

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