NSAIDs acetylsalicylic acid

NSAIDs acetylsalicylic acid, antipyrine, paracetamol, ibuprofen, naproxen, phenacetin, piroxicam... 

Acetyls alley lie acid was shown to prevent cirrhosis under certain experimental conditions [125]. Naproxen and indomethacin partially protected against LPS and D-galactosamine-in-duced hepatotoxicity [126] Acetylsalicylic acid and ibuprofen were also protective in endo-toxic shock [127]. Endotoxaemia is one of the complications in cirrhotic patients [128] and is probably caused by an impaired ability of the liver to take up and detoxify gut-derived LPS [116]. The presence of portosystemic shunts in cirrhotic patients may also contribute to this spill-over of LPS into the systemic circulation [129]. NSAIDs, however, are also reported to provoke deleterious effects on renal function in cirrhosis [130], and can therefore not be used in cirrhotic patients. Cell-specific delivery of NSAIDs to SECs and/or KCs may make application of these drugs in cirrhosis feasible by circumventing the renal side-effects. 

Acetylsalicylic acid and related non-steroidal anti-inflammatory drugs (NSAIDs) selectively inhibit the cyclooxygenase activity of prostaglandin synthase [2] and consequently the synthesis of most eicosanoids. This explains their analgesic, antipyretic, and antirheumatic effects. Frequent side effects of NSAIDs also result from inhibition of eicosanoid synthesis. For example, they impair hemostasis because the synthesis of thromboxanes by thrombocytes is inhibited. In the stomach, NSAIDs increase HCl secretion and at the same time inhibit the formation of protective mucus. Long-term NSAID use can therefore damage the gastric mucosa. 

Recommended antipyretics are paracetamol, acetylsalicylic acid and short acting NSAIDs to adults. Children under the age of 18 should not be treated with acetylsalicylic acid due to an increased risk of Reye s syndrome in viral infections. 

Most of the nonsteroidal anti-inflammatory drugs (NSAIDs) are carboxylic acids. Aspirin (8.69) (acetylsalicylic acid, ASA) has been used since the turn of the last century to reduce pain and fever, but the parent compound, salicylic acid, has been known and used since antiquity, owing to its common occurrence as a glycoside in willow bark. Acetylation merely decreases its irritating effect. Among the numerous other salicylates known and used, flufenisal (8.70) has a longer duration of activity and fewer side effects than aspirin. Mefenamic acid (8.71) and flufenamic acid (8.72) are derivatives of anthranilic acid, while ibuprofen (8.73) and naproxen (8.74) are derivatives of phenylacetic and naphthylacetic acids, respectively. 

There are two major classes of pain medications, nonopioids and opioids. The nonopioids used to treat mild pain include agents such as acetaminophen, both steroid and nonsteroidal antiinflammatory drugs (NSAIDs), and acetylsalicylic acid. Anticonvulsants suppress neuronal firing and are also helpful in neuropathic pain. Antiinflammatory agents (e.g., NSAIDs or corticosteroids) may be particularly helpful when bony involvement occurs and are often used for low-intensity pain. Steroids decrease inflammatory edema and are useful in cases of nerve and spinal cord compression, lymphedema, visceral pain caused by organ enlargement, and bone pain. Finally, short-term corticosteroid therapy may also produce euphoria (thus ameliorating less severe depressions) as well as reverse anorexia. 

Prostanoid mediators derived from arachidonic acid and sites of drug action. ASA, acetylsalicylic acid (aspirin) LT, leukotriene NSAID, nonsteroidal... 

Almost all non-opioid analgesics are non-steroidal anti-inflammatory drugs (NSAIDs) and have varying degrees of analgesic, anti-inflammatory and antipyretic activity. Acetylsalicylic acid (Aspirin ), used to relieve mild to moderate pain and certain types of severe pain, is the archetypal NSAID and is probably the best known and most used therapeutic drug worldwide. 

Analgesic efficacy and clinical use Dextropropoxyphene (Grover, 1988) is a moderately potent opioid analgesic often combined with paracetamol or acetylsalicylic acid or other NSAIDs (Collins et al., 2000). As the hydrochloride or napsylate it is used orally for the treatment of mild, moderate, or severe pain (Beaver, 1984). 

Nonsteroidal Antiinflammatory Drugs. Nonsteroidal antiinflammatory drugs (NSAIDs) include, among the numerous agents of this class, aspirin (acetylsalicylic acid), the arylacetic acids indomethacin and sulindac, and the arylpropionic acids, tS)-<8) and (/ )-(9) ibuprofen, (S)-(10) and (/ )-(11), flurbiprofen naproxen, and fenoprofen. See also Analgesics, Antipyretics, and Antiinflammatory Agents and Salicylic Acid and Related Compounds. 

The best representative of an NSAID is aspirin (acetylsalicylic acid Fig. 15-1). Newer NSAIDs are usually compared to aspirin in terms of efficacy and safety. Acetaminophen is another agent that is similar to aspirin and other NSAIDs in its ability to decrease pain and fever. Acetaminophen, however, is not considered an NSAID because it lacks anti-inflammatory and anticoagulant properties. For a discussion of the comparative effects of aspirin, newer NSAIDs, and acetaminophen, see Comparison of Aspirin with Other NSAIDs. ... 

A major aim of enteric coating is protection of drugs that are sensitive or unstable at acidic pH. This is particularly important for drugs such as enzymes and proteins, because these macromolecules are rapidly hydrolyzed and inactivated in acidic medium. Antibiotics, especially macrolide antibiotics like erythromycin, are also rapidly degraded by gastric juices. Others, such as acidic drugs like NSAID s (e.g., diclofenac, valproic acid, or acetylsalicylic acid) need to be enteric coated to prevent local irritation of the stomach mucosa. 

Rheumatoid arthritis is a disease that involves inflammation in joints and causes severe pain and immobility. The worldwide scenario indicates that the elderly population suffers the most from this disease. The drugs of choice for treatment of this condition are nonsteroidal antiinflammatory drugs (NSAIDs), which include acetylsalicylic acid, diclofenac sodium, piroxicam, nimesulide, celecoxib, and refecoxib. Therapeutic doses, adverse effects, and precautions are given in the foifowing pages. 

Theis JGW. Acetylsalicylic acid (ASA) and nonsteroidal anti-inflammatory drugs (NSAIDs) during pregnancy are they safe Can Fam Physician 1996 42 2347-2349. 

Ketorolac tromethamine is contraindicated in patients while wearing soft contact lenses. Caution should be used with patients who have previously exhibited sensitivity to acetylsalicylic acid,phenylacetic acid derivatives, and other NSAIDs because a potential exists for cross-sensitivity. 

Mode of action. Acetylsalicylic acid is unique among NSAIDs in that it also irreversibly inhibits COX by acylating the active site of the enzyme, so preventing the formation of products including thromboxane, prostacyclin and other prostaglandins, imtil more COX is synthesised. Acetylsalicylic acid is rapidly hydrolysed to salicylic acid in the plasma. Salicylic acid also has an anti-inflammatory action but additionally exerts important effects on respiration, intermediary metabolism and acid-base balance, and it is highly irritant to the stomach. 

Alcohol, acetylsalicylic acid and NSAIDs should be avoided. There is no advantage to be gained from not consuming certain foods (such as spices) or from the long-term intake of H2 blockers. 

Aspirin or acetylsalicylic acid, an ester of acetic acid, is the oldest known NSAID and the prototype of the salicylate drugs (Collier 1971, Rogstad Yndestad 1981). In addition to inhibition of COX, salicylates inhibit the formation and release of kinins, stabilize lysosomes and uncouple oxidative phosphorylation (Boothe 1995). In horses, the half-life of aspirin is very short. For example, in ponies, the elimination half-life of aspirin administered i.v. at a dose rate of 19 mg/kg was determined to be approximately 7min (Lees et al 1987a). 

The most common NSAID is aspirin, or acetylsalicylic acid, whose use goes back to the late 1800s. It had been known from before the time of Hippocrates in 400 bc that fevers could be lowered by chewing the bark of willow trees. The active agent in willow bark was found in 1827 to be an aromatic compound called salicin, which could be converted by reaction with water into sal- oxidized to give salicylic acid. Salicylic acid... 

Subsequently there was enormous use of sodium salicyate as an ANALGESIC, ANTIPYRETIC and ANTIINFLAMMATORY (though a gastric irritant). This, in turn, prompted the synthesis of acetylsalicylic acid (aspirin), and subsequently the salicylate series of NSAID ANALGESICS, which later proved to work through being CYCLOOXYGENASE INHIBITORS. 

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. 

All compounds of the test dataset are nonsteroidal anti-inflammatory drugs (NSAIDs) and are thus relatively similar in terms of their pharmacological properties (Fig. 18). The compounds are 1, acetylsalicylic acid 2, diclofenac 3, flufe-namic acid 4, flubiprofen 5, ibuprofen 6, indometacin 7, ketoprofen 8, meclofe-namic acid 9, mefenamic acid 10, naproxen 11, piroxicam 12, sulindac sulfide (active metabolite of sulindac) 13, tenoxicam 14, meloxicam 15, cgp 28238 16, DuP-697 17, L-745-337 18, 6-methoxy-2-naphthylacetic acid (active metabolite of nabumeton) 19, NS-389 20, SC 58125. 

Most NSAIDs are nonselective inhibitors of cyclooxygenases, acting on both COX 1 and COX 2 isoforms to decrease formation of PGs and thromboxanes. This action is a primary (but not sole) contributor to the pharmacologic actions of NSAIDs. These actions include analgesic, antipyretic, anti-inflammatory, and antiplatelet effects. Acetylsalicylic acid (ASA) is the prototype of the group, which includes more than 20 individual drugs. 

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