Nonsteroidal antiinflammatory drugs Actions

There are several hundred reported NF-kB inhibitors (see www.nf-kb.org for a complete and updated list). These inhibitors include natural products, chemicals, metabolites, and synthetic compounds. A large majority of these products, in particular commonly used antiinflammatory drugs such as corticosteroids and the nonsteroidal antiinflammatory drugs (NSADDs) aspirin, sulindac, ibuprofen and sulphasalazine, have the ability to partially inhibit NF-kB activity in cell culture. However, the precise mechanism of action and the specific molecular targets of most of these inhibitors remain unclear. 

V.c.1.1. Cyclo-oxygenase inhibition. Inhibition of cyclo-oxygenase reduces the level of circulating prostaglandins and neurogenic inflammation. This is the mechanism of action of nonsteroidal antiinflammatory drugs (NSAID) and aspirin. The mode of action of paracetamol is less clear (inhibition of prostaglandins in the nociceptors of the posterior horn of the spinal cord and action on the supraspinal structures implicated in nociception). 

Serhan, C.N., Clish, C.B., Brannon, J. et al., Novel functional sets of lipid-derived mediators with antiinflammatory actions generated from omega-3 fatty acids via cyclooxygenase 2-nonsteroidal antiinflammatory drugs and transcellular processing. J. Exp. Med., 192, 1197, 2000. 

Abramson SB, Weissmann G. The mechanisms of action of nonsteroidal antiinflammatory drugs. Arthritis Rheum 1989 32(l) l-9. 

McCormack K 1994 The spinal actions of nonsteroidal antiinflammatory drugs and the dissociation between their anti-inflammatory and analgesic effects. Drugs Supplement 5 2 45... 

Stabler I, Kapui Z, Ambrus J L1994 Study on the mechanisms of action of sodium meclofenamic acid (meclomen) a double inhibitor" of the arachidonic acid cascade. Journal of Medicine 25 371-382 Stillman M, Schlesinger P 1990 Nonsteroidal antiinflammatory drugs nephrotoxicity. Archives of Internal Medicine 150 268-270... 

The inhibitors of COX enzymes are called nonsteroidal antiinflammatory drugs (NSAIDs) that are prescribed to relieve pain and fever. They stop prostaglandin and thromboxane production. Acetylsalicylic acid (aspirin) was used for this for many years and it was eventually discovered to acetylate a serine residue involved in the dioxygenase action of cyclooxygenases. A second class of NSAIDs, typified by ibuprofen (commonly called Advil or Motrin), inhibits catalysis by attaching irreversibly to cyclooxygenases. Aspirin and ibuprofen inhibit all prostaglandin and thromboxane synthesis. 

The coxibs, including celecoxib (Celebrex), are a recently developed class of nonsteroidal antiinflammatory drugs (NSAIDs). The coxibs show antiinflammatory actions without affecting platelet function. These effects of the coxibs are best attributed to selective inhibition of which of the following ... 

The analgetic potency of these compounds varies considerably. However, they do share several properties. They are all acidic and exhibit clinically useful antiinflammatory properties. In addition, they share a common mechanism of action, as will be discussed. The nonsalicylate drugs in Table 5-2 are now collectively referred to as nonsteroidal antiinflammatory drugs (NSAIDs). The salicylates should actually share this designation. 

Three treatments are available for patients with acute gouty arthritis. Colchicine is less favored now than in the past because its onset of action is slow and it invariably causes diarrhea. Nonsteroidal antiinflammatory drugs, which are currently favored, are rapidly effective but may have serious side effects. Corticosteroids, administered either intraarticularly or parenterally, are used increasingly in patients with monarticular gout, especially if oral drug therapy is not feasible. 

Although mesalamine is a salicylate, its therapeutic effect does not appear to be related to cyclooxygenase inhibition indeed, traditional nonsteroidal antiinflammatory drugs actually may exacerbate IBD. Many potential sites of action have been demonstrated in vitro for either sulfasalazine or mesalamine inhibition of the production of IL-1 and TNF-a, inhibition of the lipoxygenase pathway, scavenging of free radicals and oxidants, and inhibition of NF-Kp, a transcription factor pivotal to production of inflammatory mediators. Specific mechanisms of action of these drugs have not been identified. 

The client with rheumatoid arthritis is taking etodolac (Lodine), a nonsteroidal antiinflammatory drug (NSAID). The client is complaining of a headache. Which action should the nurse implement ... 

First, oleanolic acid (43) could induce the release of the prostaglandin I2 (PGI2) of bioactive prostanoid having smooth muscle relaxation action and platelet aggregation restraint action by the human coronary SMC (Smooth Muscle Cell). This effect was inhibited by a coxib-based nonsteroidal antiinflammatory drug celecoxib of a selective Cox-2 inhibitor that relieves pain and inflammation without harming the digestive tract. 

Among the treatment options, topical decongestants, topical and oral antihistamines, mast cell stabilizers, dual-action/multiaction drugs, and certain nonsteroidal antiinflammatory agents have proven useful for alleviating the signs and symptoms associated with ocular allergic reactions. Homeopathic preparations have also become of interest to the ophthalmic community, and their scientific... 

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