From opium to ibuprofen – the history of pain relief

From opium to ibuprofen – the history of pain relief

An inseparable part of every person’s life is pain. It is not surprising, therefore, that painkillers have been used since the inception of the first civilizations. For centuries, in the fight against ailments, people turned to prayers and victims, and organic drugs – opioids – were also used on the agenda. Today, medicine has gone much further, and instead of the inventions of alchemists and highly addictive means, we have safer drugs, for example ibuprofen. The road to this, however, was full of ups and downs.

Cultivated around 3400 years ago BC opium was one of the first substances that was used as an extremely powerful analgesic. Used by the Sumerians, Assyrians, Babylonians and Egyptians, the drug was noticed even in India, where he came along with the troops of Alexander the Great. Opium was also used as a hypnotic and sedative, which was obtained by drying the milk juice from immature poppy capsules. It owed its strength to m.in. occurring in the composition of morphine, already known in ancient Greece. This is where her name comes from, given in honor of Morpheus’ dream god.

The next step in the evolution of painkillers was the discovery of the sixteenth-century scholar Paracelsus, called the father of modern medicine. He determined that the alkaloids contained in opium better dissolve in alcohol than in water and in this form are absorbed faster by the body. Less than a century later, the British Thomas Sydenham popularized the drink of Paracelsus, who under the name “laudanum” mastered almost the entire continent. This specific mixture of cinnamon, opium, sherry, saffron and cloves has been used for more than 250 years to relieve the symptoms of a wide spectrum of diseases, causing numerous cases of addictions, mainly among the poorer. This was because laudanum as a drug was not covered by the excise duty for alcohol, and often treated as a substitute for strong drinks. Almost throughout the 19th century, the demand for opium grew and it became such a desirable commodity that trade disputes led China and the British Empire to a series of bloody conflicts known in history as opium wars.

Not the first and not the last time measures that were intended to relieve pain, changed their destiny. The same happened with morphine chemically isolated by Frierrich Serturner in 1804. Its strong action and not fully known side effects caused that it was used on the agenda during the Civil War, leading to the permanent dependence of many wounded soldiers. Interestingly, one of them was the later creator of Coca-Cola. The drink produced with the addition of cocaine and caffeine was supposed to be a mild means of dealing with morphine addiction.

The production of heroin, which since 1874 has been used as a chronic pain relief compound – was intended to be less addictive than other available substances. And although thirty years later, the US government banned the addition of opioids to food products, on the eve of World War II, an analogous mistake made by IG Farben’s laboratory workers. Instead of a safe alternative to heroin, which was intended to be administered during surgery, they invented several times stronger than morphine and therefore extremely addictive methadone. Fortunately, drugs with narcotic effects were not the only answer to the fight against pain. Apart from them, aspirin and paracetamol were also getting more and more popular.

Aspirin

The road to the invention of aspirin was not straightforward, but the beginning of the use of its protoplast – salicylic acid – dates back to about the fifteenth century BC. Egyptian scrolls from that period mention the healing effect of the fluid contained in the willow bark, probably from there the knowledge of acid came to Greece, where its use was recommended by Hippocrates and Cornelius Pliny. Similarly to the drugs with narcotic effects, also in this matter the breakthrough occurred only in the nineteenth century. In 1829, it was possible to isolate salicin from an organic compound, and less than ten years later hydrolysis of salicin and oxidation of saligenin to salicylic acid was performed. Over the next decades, scientists and pharmacists tried to obtain a stable form of the acetylsalicylic acid compound, but this was not until the German chemist Felix Hoffmann in 1897. The drug sold under the name “Aspirin” was the first analgesic obtained in a completely synthetic way. Currently, this moment is considered a symbolic beginning of the pharmaceutical industry, and the popular Aspirin continues to enjoy unflagging popularity to this day. Unfortunately, the high risk of adverse reactions in the gastrointestinal tract and the impossibility of administering the drug to children under 12 years of age, prompted the search for milder action substances.

Paracetamol – an alternative to aspirin

Paracetamol was synthesized for the first time in 1878 in the US at Johns Hopkins University by American chemist Harmon Northrop Morse, it hit the market in 1955 thanks to two American researchers. They promoted paracetamol as an alternative to aspirin – without side effects in the gastrointestinal tract, possible to administer to children in case of fever. Interestingly, the first trade name (“Tylenol Children’s Elixir”) indicated exactly to the group of recipients. When, a year later, the drug came to the United Kingdom, it was also disseminated among the elderly, who – as advertised – “did not cause stomach irritation”. Unfortunately, in the 1960s, there were reports of side effects. Too often taken paracetamol damaged the liver, as well as contributed to the severity of asthma symptoms. However, the drug used in accordance with the recommendations, at appropriate doses was not harmful, and its sales systematically increased (in 1978-88 in the US more than fivefold) .Iupuprofen – anti-inflammatory and antipyretic Trouble with liver damage, associated with excessive use of paracetamol, contributed indirectly to develop a more effective and less aggravating drug. This is how ibuprofen was developed, developed by Boots in the early 1960s. British company employees found that the anti-inflammatory properties of acetylsalicylic acid were associated with the presence of the carboxylic acid group. After testing 6,000 other carboxylic acids that were supposed to perform similar functions, they developed a substance initially named “Brufen”. Her anti-inflammatory action was twice as strong as the popular aspirin. Ibuprofen turned out to be a hit, and among other drugs, it was distinguished by a combination of many desirable actions. It was not only effective against pain, but also acted antipyretic and anti-inflammatory. Ibuprofen, like paracetamol, can be used in children. It shows a much lower risk of side effects in the proper functioning of the liver, while betraying only slightly higher than paracetamol risk of adverse reactions in the gastrointestinal tract.