Salicylate anti-inflammatory effects

The salicylates include aspirin (acetylsalicylic acid) and related drugp, such as magnesium salicylate and sodium salicylate. The salicylates have analgesic (relieves pain), antipyretic (reduces elevated body temperature), and anti-inflammatory effects. All the salicylates are similar in pharmacologic activity however, aspirin has a greater anti-inflammatory effect than the other salicylates. Specific salicylates are listed in the Summary Drug Table Nonnarcotic Analgesics Salicylates and Nonsalicylates. 

Aspirin is acetylsalicylic acid and is used as an antiplatelet agent and for pain relief. Its use for anti-inflammatory effects is limited by the occurrence of side-effects, which include tinnitus and deafness, both features of salicylate poisoning. 

Pharmacology BSS appears to have antisecretory and antimicrobial effects in vitro and may have some anti-inflammatory effects. The salicylate moiety provides the antisecretory effect, while the bismuth moiety may exert direct antimicrobial effects against bacterial and viral enteropathogens. 

Aspirin is employed for mild to moderate pain of varied origin but is not effective for severe visceral pain. Aspirin and other NSAIDs have been combined with opioid analgesics for treatment of cancer pain, where their anti-inflammatory effects act synergistically with the opioids to enhance analgesia. High-dose salicylates are effective for treatment of rheumatic fever, rheumatoid arthritis, and other inflammatory joint conditions. 

Mechanism of action The antipyretic and anti-inflammatory effects of the salicylates are due primarily to the blockade of prostaglandin synthesis at the thermoregulatory centers in the hypothalamus and at peripheral target sites. Furthermore, by decreasing prostaglandin synthesis, the salicylates also prevent the sensitization of pain receptors to both mechanical and chemical stimuli. Aspirin may also depress pain stimuli at subcortical sites (that is, the thalamus and hypothalamus). 

This is a non-narcotic, non-salicylate analgesic with few anti-inflammatory effects that acts by inhibiting prostaglandin synthesis in the CNS (hence being antipyretic and analgesic). It is metabolized by CYP1A2. 

Therapeutic Concentration. In plasma, salicylic acid usually in the range 20 to 100 pg/ml for analgesia and 150 to 300 pg/ml for anti-inflammatory effect. 

Aspirin is often given in a buffered form. The addition of small amounts of antacids decreases GI irritation and increases the dissolution and absorption rate of the aspirin. Nonacetylated salicylates, including salsalate, sodium salicylate, choline salicylate, magnesium salicylate, and various salicylate combinations, are usually more expensive but can be effective. Although these aspirin substitutes provide less anti-inflammatory effects than aspirin, they exhibit minimal antiplatelet properties and have fewer GI side effects.They can therefore be useful for patients who cannot tolerate aspirin or other NSAIDs. 

Answer C. Ocular toxicity is characteristic of chloroquine and hydroxychloroquine. Corneal deposits are reversible, but retinal pigmentation can ultimately lead to blindness. Patients will complain about GI distress, visual dysfunction, ringing in the ears (note that tinnitus aiso occurs in salicylism), and itchy skin. Hydroxychloroquine also promotes oxidative stress that can lead to hemolysis in G6PD deficiency. DMARDs include gold salts (e.g., auranofin), methotrexate, and etanercept, but thioridazine is a phenothiazine used as an antipsychotic it lacks anti-inflammatory effect, but does cause retinal pigmentation. 

The therapeutic activities of acetylsalicylic acid and sodium salicylate do not appear to have been compared directly in controlled trials, although it is generally considered that the former is superiori " . However, Wood , on the basis of relief of stiffness, believes that their anti-inflammatory effects are equal. Wood has also pointed out the difficulties of deter-... 

Indomethacin has pmminent anti-inflammatory and analgesic-antipyretic properties similar to those of the salicylates. Indomethacin is a more potent inhibitor of COX than is aspirin, but patient intolerance generally limits its use to short-term dosing. Indomethacin has analgesic properties distinct from its anti-inflammatory effects, and there is evidence for central and peripheral actions. 

A. Classification and Prototypes Aspirin (acetylsaUcylic acid) is the prototype of the salicylates. The other older nonselective NSAIDs (ibuprofen, indomethacin, many others) vary primarily in their potency, analgesic and anti-inflammatory effectiveness, and duration of action. Ibu-... 

Diffusion of salicylate salts from skin into synovial fluid has only been studied in the knee, where the concentrations are too low for significant anti-inflammatory effect. Direct diffusion from skin into the synovial fluid appears insignificant, although these agents may still be effective for soft tissue rheumatism, which is frequently superficial. 

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. 

Q88 Anti-inflammatory doses of aspirin may cause tinnitus and deafness. These side-effects are symptoms of salicylate intoxication. 

The antipyretic and analgesic actions of aspirin are believed to occur in a certain area of the brain. It is also thought by some that the salicylates exert their analgesia by their effect on water balance. Aspirin is anti-inflammatory because it inhibits the biosynthesis of chemicals called prostaglandins. The irritation of the stomach lining caused by aspirin can be alleviated with the use of mild bases such as sodium bicarbonate, aluminum glycinate, sodium citrate, aluminum hydroxide, or magnesium trisilicate (a common trademark for this type of aspirin is Bufferin ). 

Pharmacology Salicylates have analgesic, antipyretic, anti-inflammatory, and antirheumatic effects. Salicylates lower elevated body temperature through vasodilation of peripheral vessels, thus enhancing dissipation of excess heat. The anti-inflammatory and analgesic activity may be mediated through inhibition of the prostaglandin synthetase enzyme complex. 

Pharmacology Olsalazine sodium is a sodium salt of a salicylate compound that is effectively bioconverted to 5-aminosalicylic acid (mesalamine 5-ASA), which has anti-inflammatory activity in ulcerative colitis. Approximately 98% to 99% of an oral dose will reach the colon, where each molecule is rapidly converted into 2 molecules of 5-ASA by colonic bacteria. The liberated 5-ASA is absorbed slowly, resulting in very high local concentrations in the colon. 

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