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Aspirin


Aspirin is a member of a group of medicines collectively referred to as Non-Steroidal Anti-Inflammatory Drugs (NSAIDs). Various remedies similar to aspirin, originally derived from the organic compound salicylic acid that accumulates in the willow tree, have been used for centuries. The Sumerians and the Egyptians knew of the pain-relieving properties of willow leaves, or salix. The Greek physician Hippocrates of Cos, who lived from 460 to 377 B.C. and is often referred to as the father of modern medicine, prescribed chewing willow leaves to women in labour as a method of reducing pain. As well as the Greeks, the Native Americans and the Hottentots of South Africa were also aware of the therapeutic properties of willow in cases of fever, inflammation, and pain. This knowledge was not utilised in modern Europe until the Nineteenth Century.

The main problem with salicylic acid, apart from its unpleasant taste, was that it was harsh on the stomach. Patients often experienced extreme side effects, including stomach irritation, gastric discomfort and nausea. In 1853 the French chemist Charles Frederic Gerhardt addressed this problem by synthesizing acetylsalicylic acid, which is a chemical salt that neutralised the salicylic acid, by buffering it with sodium salicylate and acetyl chloride. Gerhardt called this 'acetosalicyclic anhydride' but his discovery was not marketed and was to linger in obscurity for a number of years. In the meantime, Hermann Kolbe, a chemistry professor at Marburg University in north-west Germany, succeeded in making synthetic salicylic acid in 1859, clearing the way for its large scale distribution.

The breakthrough came in the 1897 when Felix Hoffman, an employee of the Friedrich Bayer and Company in Germany, drew on Gerhardt's formula in an effort to find a treatment for his father's arthritis. He found an easier way to make acetylsalicylic acid and in the process created the world's first truly synthetic drug, one that was not merely a copy of a naturally occurring compound. This was synthesized acetylsalicyclic acid (ASA) which the Bayer company marketed as a powder under the name Aspirin in 1899. The 'A' came from acetyl chloride, the 'spir' was derived from the spiraea ulmaria plant that provided the salicylic acid, and the 'in' was merely a common suffix used for medicines. Aspirin was sold in tablet form by Bayer for the first time in 1915.

Aspirin was so popular that, after the defeat of Germany in the First World War, the Bayer company was forced to give up its aspirin trademark as part of the war reparations enacted by the Treaty of Versailles. All of this popularity had been achieved without a detailed understanding of how it actually worked. It was not until British pharmacologist Sir John Vane conducted clinical trials on aspirin at London's Royal College of Surgeons in 1971 that this knowledge was gained. He discovered that aspirin suppresses the production of hormone-like substances known as prostoglandins, which are found in most tissues in the body.

Prostoglandins perform a variety of regulatory functions within the body, including controlling smooth muscle tissue contraction, regulating temperature, blood vessel elasticity, as well as mediating pain and inflammation. Inflammation is actually an attempt by the body to protect the damaged area by bathing the tissue in fluids from the blood until it can heal.

Pain is part of the body's warning system, drawing attention to damage or dysfunction, through a system of special nerve endings situated throughout the body. When injury or inflammation occurs, the damaged cells release unsaturated fatty acids which form prostaglandins. Prostaglandins are made using an enzyme called cyclo-oxygenase (COX) and serve as pain activators, amplifying the degree of pain experienced. Aspirin sticks to the cyclo-oxygenase and restricts the production of prostaglandins. Aspirin's acetylsalicylic acid works by inhibiting the synthesis of prostaglandins in the body, thereby reducing the amount of pain stimuli that is transmitted to the brain. This does not, however, fix the damage that initially triggers the pain in the first place.

Prostoglandins also control the build up of platelets, the minute disc-like cytoplasmic body found in blood plasma, that create the clots that can result in heart attacks and strokes. This enables aspirin to work as an antithrombotic medication by blocking the production of thromboxane by the platelets, one of the chemicals that cause platelet agglutination. This ability becomes reduced as low doses of aspirin inhibit the release of prostaglandin.

Aspirin has many therapeutic qualities. It is an analgesic that can reduce pain as well as an anti-inflammatory that can alleviate swelling. Aspirin is also an antipyretic compound that lowers body temperature and reduces fever through the dissipation of heat through effects on the hypothalamus. The body turns aspirin into salicyclic acid which is then transferred through the body to the liver and the kidneys, until it is passed out of the body in the urine.

Aspirin is used in the treatment of a wide variety of ailments including headache, acute migraine, fever (pyrexia), muscular pain, dental pain, sore throat, rheumatic fever, rheumatoid arthritis, joint inflammation, swelling, and the prevention of blood clots and thrombosis. Aspirin is also believed to reduce the risk of heart disease, strokes, and some forms of cancer, including colon and bowel cancer.

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