In December 2022, the number of people infected with the new coronavirus surged, and the anti-inflammatory painkiller ibuprofen suddenly became a hot commodity.
Stuart Adams, the inventor of ibuprofen, would be 100 this year if he were alive. Four years ago, on January 30, 2019, Adams died at the Queen’s Medical Center in the United Kingdom. In the past 60 years since the advent of ibuprofen, it has been the most commonly used, high-quality and cheap antipyretic, analgesic and anti-inflammatory drug for people all over the world.
But the inventor, who would go to the pharmacy to buy ibuprofen when he had a headache, did not know that ibuprofen would become a “new Internet celebrity” during the ravages of the new crown virus after his death.
Medicines for Pain Relief
People will get sick at different stages in their life. If they are sick, they will have physical pain, and even if they are not sick, they will still have pain. However, there are differences in the degree of pain, which can be simply divided into mild pain, moderate pain and severe pain. If there are painkillers, people will feel better, have a stronger tolerance to the disease, and be able to fight against the disease better.
There are many types of analgesics. So far, there are roughly several types of analgesics invented by humans. One is non-steroidal, the mechanism of action is to inhibit the synthesis of prostaglandins, ibuprofen and acetaminophen belong to this category. The second is central analgesics, which play an analgesic role by anesthesizing the central nervous system. Common ones include morphine and tramadol. The third is antispasmodic analgesics, which relieve pain mainly by relieving muscle smooth muscle spasm, mainly anisodamine, belladonna tablets, etc. Fourth, anti-anxiety painkillers, such as diazepam and estazolam.
When a person is sick, cell tissue is damaged and inflammation occurs. The occurrence of pain has a lot to do with the inflammatory response. The main manifestations of inflammation are redness, swelling, heat, pain and dysfunction. Redness and swelling are mainly caused by vasodilation and increased permeability, while heat and pain are mainly caused by inflammatory mediators such as prostaglandins, serotonin, and bradykinin. Ibuprofen achieves pain relief by inhibiting the production of prostaglandins and other pain-causing substances during inflammation.
Ibuprofen is effective for chronic dull pain, pain caused by inflammation or tissue damage, and postoperative pain, but not for acute sharp pain, various severe trauma pain, and visceral smooth muscle pain. Now, on the World Health Organization’s drug list, ibuprofen is suitable for fever, mild and moderate pain (including pain after surgery), menstrual pain, osteoarthritis, toothache, headache, and pain caused by kidney stones. It is also suitable for pain caused by juvenile idiopathic arthritis, rheumatoid arthritis, pericarditis and patent ductus arteriosus.
However, the research and development and appearance of ibuprofen has gone through a long period of time and twists and turns.
Dedicated to planting flowers for ten years and one sword
The inventor of ibuprofen is Stuart Adams, but since he is a lifelong employee of Boots in the UK, the invention and patent of this drug belong to professional behavior, and the inventor and patent owner belong to Boots and Adams .
On April 16, 1923, the family of a railway worker in Byfield, Northamptonshire, England added another child. He was Adams. Before him, there were two older brothers and one older sister in his family. In the following years, Adams had another a younger brother. Of the five siblings, only Adams went on to achieve outstanding results.
Due to the poverty of his family, Adams attended Byfield Township School when he started school. In 1933, Adams moved with his parents to Doncaster, South Yorkshire, where he studied at Doncaster Grammar School. In 1937, Adams went to Mazzie Grammar School, but finally dropped out of school when Adams was 16 years old (1939) because his family could not afford the tuition.
Afterwards, Adams did a 3-year apprenticeship at Mazi’s Boots chain (drugstore) and became a pharmacist. This process led Adams to develop an interest in pharmacology. On the one hand, Adams was willing to learn, and on the other hand, his hard work won the trust of Boots, which sponsored him to study pharmacy at the University of Nottingham, UK. In 1945 Adams received a bachelor’s degree in medicine.
After graduation, Adams returned to Boots to work and participated in the company’s research on the development of penicillin. Five years later, Adams won a £600 scholarship from the Royal Society of Medicine to fund his PhD in Pharmacology at the University of Leeds. In 1952, Adams completed his studies and returned to Boots’ research and development group. In 1953, after graduating from his Ph.D., Adams turned to the study of painkillers. Therefore, the research on ibuprofen is not completely “unintentional planting”, but partly the work of “intentional planting” by Adams and his company.
At the time, Adams and company began researching treatments for rheumatoid arthritis. The disease caused severe pain to patients, and the main drugs that could relieve this pain at that time were corticosteroids and high doses of aspirin, but these drugs had unbearable side effects.
Hangover Headache Trials
Although ibuprofen was the intentional work of Adams and the company’s team, it also experienced many unintentional moves, and it took a long time. This also proves that the research and development of a new drug or vaccine requires more than “two tens”, that is, more than 10 years and more than US$1 billion in funding.
To sidestep the side effects of high-dose aspirin, Adams turned to other pain-relieving chemicals. After 1953, Adams found two aspirants to assist in the research, one was Dr. John Nicholson, a chemist, and the other was Colin Burrows, a technician.
The research team tested more than 600 compounds day and night during the 6 years in the suburbs of Nottingham. Only 4 of them reached the clinical trial stage, but all of them fell short due to relatively large side effects in the trial. However, in the late 1950s, Adams’ team discovered that the side effects of previous compounds were greater because they were absorbed in large quantities by various tissues in the body. Therefore, side effects can only be avoided by making the drug dose both small and effective.
So they shifted their focus from acetic acid to propionic acid. When they started working on a family of compounds called phenylpropionic acids, Adams’ team discovered a compound called p-isobutylphenylisopropionic acid that not only relieves pain, but also has few side effects. After hundreds of tests on animals and humans, they confirmed that it was more than three times as potent as aspirin, had far fewer side effects, and could also treat fevers.
