The name “Aspirin” is a brand name for one of the most popular low-cost medicines. Despite a low cost, and almost 125 years of usage, it still has about 2.5 billion USD of market share, which is expected to grow. “A” in aspirin comes from its chemical compound – Acetylsalicylic acid (ASA) and “spir” from Spiraea ulmaria – a meadowsweet plant that contains salicin, which is source for ASA.
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This product was developed by a German chemist Felix Hoffmann, who was working for a pharma company Bayer. This discovery made on 10th August 1897, led to its commercialization two years later on 6th March 1899. The brand “Asprin” became so popular that in 1933, it became a noun in Oxford dictionary, a rare feat indeed for a drug-brand.
Ancient connections
While ASA was new, salicylic acid was ancient. Ancient Egyptians, Babylonians, and Greeks used bark of willow tree as a remedy for pain and fever. In Europe ancient healers and birth attendants often used Willow bark tea, to reduce pain during delivery. By the beginning of 19th century, physicians in England were using willow bark powder as a remedy for fevers and joint pains.
In 1828, Johann Büchner who was working at University of Munich isolated an active substance from willow tree. He named it salicin (Latin word for willow). A year later, Henri Leroux, a French pharmacist isolated a pure crystalline form of Salicin or Salicylic acid, and in 1853 Charles Gerhardt figured out how to artificially produce this compound.
A new compound – ASA
As the drug became popular, its adverse effects of vomiting, stomach bleed and ulcerations became apparent. Bayer – a chemical dye making company had an aspiration to take up pharmaceuticals. It asked its chemist Felix Hoffmann to improve the compound. Hoffmann could alter Salicylic acid, and added an Acetyl moiety. Thus, ASA was born – that could be ingested, and absorbed with a fewer adverse effects. This was in 1897, and the compound was ready to be tested and used.
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Who bears the credit ?
Hoffmann provided this compound to Heinrich Dreser, head of the pharmacology laboratory for testing. In fact he has submitted not only acetyl, but also propionyl, butyryl, valeryl, and benzoyl variants of salicylic acid. It is a mystery, why Dreser started testing only in 1898, and how he selected the acetyl compound from the many variants. It is likely that Hoffmann and coworkers had already tested ASA by 1897. Regardless, on 6 March 1899 Bayer registered Aspirin, and published its first report in Die Heilkunde and Therapeutische Monatshefte.
It is debated, that more than Hoffmann and Dreser, another chemist Arthur Eichengrün had synthesized ASA. Eichengrün was a Jew and made this claim only in 1946 after the Nazi’s were defeated in second world war. By this time Aspirin was hugely popular. and it was a leading drug used across the world for pain, fever, joint pains and inflammation.
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Popular usages in its first 70 years
While part of the popularity was the effect, and part marketing. Bayer Initially launched Aspirin as a powder, and the company would send packets of the drug to doctors, encouraging them to publish about the drug’s effects. Soon in in 1900 it was packaged as a tablet, and the name “Bayer” was etched on each tablet. This was sold as “genuine” Aspirin, as opposed to local versions that were available in some countries.
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The drug was patented in US and Britain, and and after 1915, it could be purchased without a prescription. German Bayer, shifted its operations to its US plant to continue producing Aspirin during and in between the wars. Aspirin became a drug of choice during the 1918 flu epidemic. It was only in 1946, that we discovered paracetamol, which gradually took over Aspirin.
Mechanisms and more usages
Aspirin’s antiplateet action was first observed in 1967 by Harvey Weiss and Louis Aledort. In 1971, John Robert Vane, a British pharmacologist, and his graduate student Priscilla Piper were exploring substances that are released during inflammation. They discovered prostaglandin – a hormone that effects blood vessels, and leads to a pain response. He found that Aspirin inhibits prostaglandin synthesis. In 1976, scientists also discovered cyclooxygenases (COXs) – enzyme that helps in prostaglandin synthesis. Aspitin inhibits COX, and hence its pain response. For Vane’s pioneering work he, along with Sune K. Bergström and Bengt I. Samuelsson, received the Nobel Prize in Physiology or Medicine in 1982.
Beyond pain, Aspirin has a role in prevention of coronary artery disease, cancers, and stroke. Many studies published between 1974 and 2000 have confirmed these effects. These preventive effects occur at a much lower dose (75 or 150mg per day) as compared to pain relief effect at higher dosages (325 to 1200 mg/day). Thus, Aspirin today is a life saving drug and more than 70 million pounds of this drug are produced every year.
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125 years and counting
The drug is still so important to Bayer, that in the 1999 company created another world record. On March 6, exactly 100 years after registration of Aspirin, Bayer set a Guinness world record by transforming its 122 meter tall headquarters building in Leverkusen into the largest Aspirin box. The building is wrapped with more than 22,500 square meters of fabric to celebrate it’s 100th birthday.
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From pain relief to prevention of heart attacks, stroke and cancer, Aspirin is truely a wonder drug. It may surely be aspiring for more, and only time will stand testimony to this future. The drug in its purified form has truly worked wonders in its 125 year history, and much longer as a willow-tree bark.