Anti-Inflammatory Drug

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Aspirin


Background
Aspirin
Aspirin, or acetylsalicylic acid (ASA) is a salicylate drug, and is generally used as an analgesic (something that relieves pain without producing anaesthesia or loss of consciousness) for minor aches and pains, to reduce fever (an antipyretic), and also as an anti-inflammatory drug. Aspirin works by prohibiting biological substances such as prostaglandins. Many different prostaglandins exist in the human body each serving a plethora of physical functions. Prostaglandins are amongst the chemicals produced by the body’s immune system when it fights off pathogens. These pathogens usually cause inflammation and pain. Following infection, prostaglandins are also produced the hypothalamus, the brain’s centre for controlling body temperature, resulting in a rise in temperature. Inhibiting their production consequently inhibits pain and temperature rise Another type of prostaglandins is found in the blood causes platelets to stick together causing thrombosis. Again aspirin inhibits these prostaglandins. The many kinds of prostaglandin are synthesized by a combination of biochemical pathways. However, all pathways share a common stage facilitated by an enzyme called COX. Aspirin is an enzyme inhibitor. As you can see from figure 2 It suppresses the action of the enzyme COX, stopping the production of prostaglandin, thus disrupting the pathways to pain, inflammation, elevated temperature and the formation of blood clots. Enzymes are biological protein catalysts that speed up chemical reactions without being themselves used up themselves in the reaction. Enzymes are protein catalysts that speed up chemical reactions without being themselves used up in the reactions. An enzyme is a huge molecule with an active site that works like a lock that accepts certain substrate (key) . Enzymes are long, linear chains of amino acids that fold to produce many levels of structure (Primary, tertiary and quaternary) . Each amino acid sequence produces a specific structure.. Individual protein chains may sometimes group together to form a protein complex in this case prostaglandins, which each have their own unique properties.

1763 Edward Stone (a clergyman) read a paper to the Royal Society of London: ‘An account of the success of the Bark of the Willow in the Cure of Agues’. He had collected observations from around the country on the effect of willow bark on the relief of fever due to agues (malaria).

1830s A Scottish physician found that extracts of willow bark relieved symptoms of acute rheumatism.
1840s Organic chemists working with willow bark and flowers of the meadowsweet plant, spirea, isolated and identified the active ingredient as salicin (salix = Latin word for willow).
Salicin
1870 Professor von Nencki of Basle demonstrated that salicin was converted into salicylic acid in the body.
Salicylic acid (2-Hydroxybenzoic acid)
Salicylic acid was then given to patients with fevers and their symptoms were relieved. However, the compound caused severe irritation of the lining of the mouth, gullet and stomach.
1875 Chemists made sodium salicylate and gave that to doctors to try on their patients. It still worked to help reduce pain and fever and did lessen the irritation, but tasted awful!
Sodium salicylate
(Sodium 2-hydroxybenzoate)
In the large doses used for treating rheumatism sodium salicylate frequently caused the patient to vomit.
1890s Felix Hofmann of the Bayer Company in Germany made aspirin which was found to have good medicinal properties, low membrane irritation and a reasonable taste. This followed the publication of news about the temperature reducing properties of acetanilide which immediately spurred a chemist at Bayer’s dye works to make some derivatives:

Aspirin
(2-Ethanoyloxybenzenecarboxylic acid)
He called the new medicine aspirin (‘a’ for acetyl – the systematic name for the compound at the time was acetylsalicylic acid, ‘spir’ for spirea, the meadowsweet...
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