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Risk of adverse advents such as bleeding or gastrointestinal side effects is relatively high with daily aspirin therapy. Even a 81 mg daily aspirin regimen for cardiovascular benefits has been shown to increase risk of long-term bleeding, [27] so the significantly higher aspirin doses used for maintenance therapy are of some concern. [19]
The acutely toxic dose of aspirin is generally considered greater than 150 mg per kg of body mass. [12] Moderate toxicity occurs at doses up to 300 mg/kg, severe toxicity occurs between 300 and 500 mg/kg, and a potentially lethal dose is greater than 500 mg/kg. [13]
Enteric coating on aspirin may be used in manufacturing to prevent release of aspirin into the stomach to reduce gastric harm, but enteric coating does not reduce gastrointestinal bleeding risk. [ 188 ] [ 189 ] Enteric-coated aspirin may not be as effective at reducing blood clot risk.
An enteric coating is a polymer barrier applied to oral medication that prevents its dissolution or disintegration in the gastric environment. [1] This helps by either protecting drugs from the acidity of the stomach, the stomach from the detrimental effects of the drug, or to release the drug after the stomach (usually in the upper tract of the intestine). [2]
Indomethacin, ketoprofen, and piroxicam use appear to lead to the highest rate of gastric adverse effects, while ibuprofen (lower doses) and diclofenac appear to have lower rates. [17] Certain NSAIDs, such as aspirin, have been marketed in enteric-coated formulations that manufacturers claim reduce the incidence of gastrointestinal ADRs ...
Aspirin acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the COX enzyme. [1] This makes aspirin different from other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors; aspirin creates an allosteric change in the structure of the COX enzyme. [2]
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