Aspirin and a pharmaceutical milestone

On August 10, 1897, German chemist Felix Hoffman synthesised aspirin, paving the way for it to become a household name. Over a century later, aspirin might have been dislodged from its position as the most popular painkiller, but it continues to be in use despite controversies surrounding it. A.S.Ganesh takes a look at Hoffman and his war against pain...

August 08, 2021 12:27 am | Updated November 10, 2021 12:15 pm IST

Aspirin remains one of the most popular drugs in the world.

Aspirin remains one of the most popular drugs in the world.

As sentient beings, human beings constantly strive to be happy and avoid suffering. While an ideal world where everyone is happy and free from suffering might be a utopian dream, we have definitely come a long way at alleviating pain. German chemist Felix Hoffman’s aspirin had a telling role as a painkiller and continues to be relevant till this day as it has been clinically proven to work for many conditions.

Aspirin’s ancestor, if we can use such a terminology, dates back thousands of years. For as far back as the Sumerian Third Dynasty of Ur around 2000 BC, people were using the bark of the willow tree and extracts from the plant spiraea for relief from headaches, fevers, and inflammations.

Salicin identified

Around 2500 years ago, Greek philosopher Hippocrates had observed the usefulness of powdered willow bark as a painkiller and documented his findings. It was, however, only early in the 19th Century that salicin was identified as the substance in willow plants capable of relieving pain.

Once salicin was successfully extracted, it was converted into salicylic acid and purified for human consumption. While it was effective, having it was an unpleasant experience as it was rather harsh on people’s stomach.

By the middle of the 19th Century, French chemist Charles Gerhardt found a way to neutralise it by combining acetyl chloride with the sodium salt of salicylic acid. His research, however, stopped there and no product resulted from it. It was left to Hoffmann to do that by the end of the century.

Drawn towards medicines

Born in 1868 in Ludwigsburg in Germany, Hoffman was the son of a manufacturer in the town. After finishing school, Hoffman aimed to become a pharmacist. He was so fascinated when working in a number of pharmacies in various cities around Germany that he decided to broaden his knowledge in the field of chemistry.

He studied the subject in the University of Munich, graduating in 1893. Based on the recommendation of one of his professors, Adolf von Baeyer, who eventually went on to win the Nobel Prize, Hoffman joined the newly created pharmaceutical research department at the Bayer Company.

Legend has it that Hoffman was seeking a medicine to ease his father’s rheumatic pains. It was with this aim that he added the acetyl group to different molecules in the summer of 1897. Bayer’s first medicines had been produced by acetylating molecules and it worked for Hoffman as well when he finally succeeded on August 10, 1897.

Following Hoffman’s success in acetylating salicylic acid to produce acetylsalicylic acid in a pure and stable form, its efficacy as a pain-relieving, fever-reducing, and anti-inflammatory substance was established beyond doubt. Knowing they had a winner in their hands, Bayer fast-tracked testing and production before launching it under the trade name Aspirin – A for acetyl and spirin from spiraea – in 1899.

Aspirin’s success

While Germany denied a patent for this development, the U.S. awarded a patent for Hoffmann and the Bayer Company on February 27, 1900. This led to a Bayer monopoly on aspirin in the U.S. from 1900-1917, when the rights were finally given up as part of Germany’s concessions in the Treaty of Versailles. The treaty, in fact, also brought about the freedom to use the word ‘aspirin’ for the drug, which had until then been a trade name that could be used by Bayer only.

With prescriptions made unnecessary and over-the-counter buying made possible, aspirin became the go-to drug as a painkiller for nearly 50 years. Hoffman, however, never made huge gains from his discovery and led a largely quiet life until his death in Switzerland in 1946.

It was only in the 1970s that aspirin was replaced first by paracetamol, which was later joined by ibuprofen, in the war against pain. Aspirin, however, wasn’t going anywhere. As aspirin came to be better understood in the 1970s, it was clear that it could do more than just relieve pain.

It is now used to reduce the risk of heart attack and stroke, apart from treating migraines, muscle pain, and even some cancers. Thousands of tonnes of aspirin in the form of millions of tablets are consumed by people throughout the world each year.

This is despite the fact that there is some amount of controversy surrounding its usage, especially when taken as a preventive drug. There are even a number of bans in certain countries that range from not allowing it to be treated as an over-the-counter drug without prescription to an outright ban on administering it to children in certain other places.

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