The curious history of aspirin: a chain of errors

With what was a waste from the coal industry and several accidents that could have been fatal, chemists of the late nineteenth and early twentieth century managed to mitigate the headaches.

After centuries of tolerance for pain and baduming it in everyday life in the early nineteenth century, everything had changed: pain had become something that could and should be minimized.

Friedrich Sertürner had isolated morphine, the first major painkiller, and over the next 50 years a wave of scientific discoveries replaced superstitions and old beliefs with new insights.

In the middle of this century, the mysterious world of herbs and dyes was replaced by white powders that became tablets.

We were about to enter the era where chemists could mbad produce the type of painkillers we commonly use.

We were also about to create one of the most addictive substances known to man.

And all started with something unusual: coal tar.

Coal tar was a waste of the nascent coal and gas industry.

And, of course, chemists have tried to find profitable uses for it.

The availability of coal tar offered a new library of materials and the chemistry really began.

The chemists understood that they could isolate natural components or make substances that imitated them. It was a huge change for the discipline.

Between dyes and drugs

This radical change in chemistry began as it was going to continue: with a series of mistakes.

In 1845, William Henry Perkin, an 18-year-old British chemist, attempted to use coal tar to make quinine, an antimalarial drug.

Instead, he created the first artificial color, purple, and made a fortune.

It was obvious that the tar deserved to be studied, but it would take another accident to unleash its full potential to end the pain.

And see what happens

In this case, the big mistake concerned two French doctors, Arnold Cahn and Paul Hepp, who worked at the University of Strasbourg.

They tested chemicals derived from coal tar and tested them on patients with intestinal worms.

Tar had been shown to have antiseptic properties when used on the skin. They wanted to know the effects of some of its derivatives on the body.

Fortunately, they did not miss any patients. At that time, doctors were not hesitant to try almost anything in living things.

Despite this, it is incredible that Cahn and Hepp managed to get someone to eat what they had: naphthalene, also known as white tar; which is now used to hunt moths.

This had no effect on worms, but surprisingly, one of his patients who had fever reported that his temperature had dropped after taking what he had received.

It was good news. Followed shortly after by another very bad: there had been confusion.

What the patient had taken was not naphthalene. The pharmacy had made a terrible mistake of labeling.

The patient had ingested a completely unknown chemical.

It turned out that the chemical that the pharmacist had accidentally dispensed was acetanilide.

Nobody knew how he had arrived there, because it was something that was used in the dye industry.

Fortunately, it was a fortuitous accident.

They could have killed the man, but in the end, aniline acid, another chemical derived from coal tar, was quickly marketed as a fever drug … and Cahn and Hepp made a fortune.

But what really matters in this discovery is what happened next in Germany.

Relief on request

Bayer Dye Works (now Bayer A.G.) was founded in Friedrichshafen by Elderfield in 1865. Bayer's first notable product was a synthetic dye of magenta color.

Although Bayer has been a world leader in the field of dyes, it has secured a place in the history of early twentieth century chemistry through its contributions to pharmacology.

There was a strong demand for new powders against the headache and, obviously, anyone who was discovering an even better drug was expecting a fortune.

And at Bayer, there was a young ambitious chemist named Carl Duisberg, who decided that he would be the one to try.

The company's cellars were full of tar-based chemicals, such as acetanilide, and Duisberg set out to find what he could turn into a drug.

His first discovery, Phenacetin, was very successful.

We now know that phenacetin and acetanilide are converted to paracetamol in the body.

Another antiseptic?

The profits of the factory have increased rapidly, as have its ambitions. And another substance that interested them a lot was salicylic acid.

Because it is derived from coal tar, they originally thought that it could serve as an antiseptic.

They rubbed it on the skin and swallowed it.

Unfortunately, it did not kill bacteria like the one that causes typhus.

But it reduces the fever and makes the patient feel better.

However, although salicylic acid was very effective, it was too potent for the stomach.

In fact, it is used today to burn warts.

Two icons

In the new Bayer Drugs Department, a chemistry researcher, Arthur Eichengrun, felt that there had to be a way to modify the molecules to make them less irritating.

Eichengrun suggested a simple chemical modification that, over time, would lead to the production of two absolutely iconic drugs.

One of them, the best selling badgesic in history. The other, the drug with the worst fame in the world.

It started innocently enough.

A young chemist from the Eichengrun team set out to modify salicylic acid using an approach suggested by Eichengrun.

The result was crystals of acetylsalicylic acid. As expected, it was no longer as embarrbading for the stomach.

Eichengrun would eventually call this drug "aspirin".

Simple chemical modifications could clearly make better drugs.

Inspired by this, another chemist from the Bayer team took morphine, the potent painkiller of poppies, and tried the same reaction to see what had happened.

The result was a chemical called diamorphine. Better known to us as "the heroine".

We were too dangerous

Both drugs, aspirin and heroin, were sent to the test manager, Heinrich Dreser, who quickly dismissed one of them because it was too dangerous.

Ironically, aspirin was rejected because he said it was bad for the heart.

But he loved heroin.

In fact, he named it because of badociations with heroic, powerful. And with his support, the heroine was quickly marketed worldwide by Bayer.

The Bayer team accidentally produced a much more addictive version of morphine.

And of course, sales have been fabulous.

Waiting …

Eichengrun, furious because his drug, aspirin, had been forgotten, secretly started doing tests.

He was convinced that the new drug was safe, so he tried a sample. Nothing bad happened to him.

Then, in secret, he convinced a small group of doctors and a Berlin dentist to try out with their patients.

In his report, the dentist said:

"I gave it to one of my patients who had a fever." To my astonishment, he told me that acetylsalicylic acid relieved toothache.

It was completely unexpected. The initial salicylic acid had reduced fever, but it had had no effect on the pain.

Eichengrun had clearly created something new and powerful.

He decided to speak directly to the research manager at Bayer.

The latter authorized further tests and, in 1899, one year after Bayer had introduced heroin into a grateful country, this new drug began to be marketed.

Aspirin has become one of the most effective drugs in the world.

Finally, aspirin entered the market and made history.

Each year, about 40 tons of aspirin are produced worldwide, which translates into tens of billions of tablets.

And all thanks to the chemicals that handled an industrial waste product: tar.

What is your secret?

Despite its universal appeal, it took more than 70 years to understand how aspirin actually works.

Unlike opiates, such as morphine, aspirin acts locally and blocks pain well before reaching the spine.

When, for example, something irritates or hurts your skin, the damaged tissue releases a large amount of chemicals that help with healing, but they also tend to stimulate pain.

The same process is often the cause of headaches and muscle aches.

Aspirin and other anti-inflammatories prevent the body from producing chemicals as it normally does. This prevents not only inflammation, but also the release of chemicals that activate the nerves of pain.

In addition to blocking pain, aspirin also blocks the hormones that lead to platelet production.

This is why some people over the age of 50 take daily small amounts of aspirin to reduce the risk of heart attack.

To think that aspirin was originally condemned to oblivion because it would have hurt the heart!