Limelight:
The little pill that could
By
Lubna Abdel-Aziz
Barring a catastrophic asteroid collision with earth, the discovery of a magic pill to cure all our ills would secure the future of human life on our planet. It may sound far-reaching but it is not beyond the realm of scientific possibility. Though we are not there yet, we have indeed come pretty close.
It is not the scientific frenzy of the 20th century that got us there -- we have been there for centuries, but it was only 100 years ago next month that such a drug was offered for sale to the public in the form of a "tiny little pill". It was born in Germany, and next week the Bayer Company of Germany along with the rest of the world celebrates the centennial of the birth of this "tiny little pill" on 3 October 1903. They named it Aspirin.
A German dyestuff company -- Bayer -- had used the drug as an effective remedy for fever and headaches since 1897, but one chemist saw more potential in that tiny pill. Felix Hoffman was hard at work developing the drug to relieve his father's suffering from acute rheumatism. He finally managed to acetylate the phenol group of a compound called Salicylic Acid. He did not know then that he had produced the most successful medicine in modern history.
For centuries people in various parts of the world had used the bark of the willow to relieve pain. Clay tablets from Sumeria describe the use of willow leaves to treat rheumatism, a disease that has plagued the human race at least since the flowering of the great river cultures of the Middle East. The Ancient Egyptians knew the powers of the willow and the myrtle and had their own magic potions of pain relief, derived from these magic leaves.
Man was familiar with the basic ingredients of aspirin as far back as the fifth century BC. Hypocrites, the father of medicine, is said to have used ground willow bark to ease aches and pains. Extracts from the leaves and bark of the willow, myrtle and a number of other plants rely for their effects on the presence of salicylic acid, and organic compound composed of seven carbon, six hydrogen and three oxygen atoms. By the late 1800s salicylates had become the standard drug for the treatment of arthritis.
Edward Stone, a vicar at Chipping Norton in Oxfordshire, is generally recognised as the man who gave the first scientific description of the effects of the willow bark. In 1763 he wrote a letter to the Earl of Macclesfield, then president of the Royal Society in London in which he describes treating patients suffering from ague (fever) -- "20 grains (approximately one gramme) of powdered willow bark in a dram of water every four hours." Maybe it is true what many scientists and nutritionists believe, that all our ills are caused by what we put in our stomachs and all their cures exist in nature -- if we can find them!
Stone's interest in willows was due to the ancient "Doctrine of Signatures", whereby the cause of a disease offers a clue to its treatment. Stone writes: "As this tree delights in a moist or wet soil, where agues chiefly abound, the general maxim that many natural maladies carry their cures along with them or that their remedies lie not far from their causes was so very apposite to this particular case that I could not help applying it, and that this might be the intention of Providence here, I must own, had some little weight with me".
In 1829, Henri Leroux, a French pharmacist, obtained a compound of salicylic acid, known as salicin in crystalline form for the first time, and Raffaele Pine, an Italian pharmacist then succeeded in splitting it up to obtain the acid in its pure form. Reports of its beneficial properties spread quickly and demand grew in Germany. Hermann Kolbe, professor of chemistry at Marburg University succeeded in making it artificially in 1859. This allowed salicylic acid to be produced on an industrial scale, and by 1874 a factory in Dresden was able to sell it at a 10th of the price of material extracted from willow. However salicylic acid had unpleasant side-effects. Most notably it irritated the stomach and many patients were simply unable to tolerate its unpleasant taste. One such patient was the father of Felix Hoffman and it was his father's complaints that stimulated the younger Hoffman to play around with salicylic acid in order to produce something as effective as a treatment for rheumatism, but more acceptable to his father. Head of Bayer Laboratories, Heinrich Dresden tested Hoffman's new compound on himself. He then set up a series of animal experiments. Never before had a drug been tested on animals in an industrial setting. It's anti- inflammatory and analgesic effects became evident.
Soon after, people were eager to be tested, and it was not long before Bayer realised it had a major discovery on its hands. The first mass marketing of any drug was launched. The company sent out information about aspirin to 30,00 physicians, and in 1903 the drug was made available to the public. Although many of its foreign rights were confiscated by Germany's enemies after WW-1, the Bayer company still leads the world in aspirin production, selling 11 billion tablets every year.
In 1971, John Vane of the Royal College of Surgeons was awarded both a Nobel Prize and a knighthood for his discovery that aspirin suppresses the production of local hormones known as prostaglandins. These are found in most tissues of the body, suppressing the formation of blood clots that trigger heart attacks and strokes. The Physicians Health Study organised by Charles Hennekens of Harvard University and published in 1989 involved more than 22,000 healthy American doctors. It showed that an aspirin a day reduces the incidence of heart attacks by half, and that the drug can also prevent thrombosis and strokes. This was followed by a so-called 'meta-analysis' of clinical trials of aspirin in 1994 by Richard Peto and Roy Collins of Oxford University. They reviewed the results of 300 published trials of aspirin involving 140,000 patients, the largest number of patients ever reviewed at one time. The results were definitive. If people under 70 who were at risk of heart disease were to take aspirin regularly, the number of deaths from heart attacks across the world would be reduced by 100,000 a year. Today, many people, including doctors begin their day with an aspirin.
A decade ago, a Boston University study based on data from experimental animals, concluded that some cancers particularly bowel cancer, might be prevented by a regular dose of aspirin. Since then, 15--20 studies have been carried out and they support the same conclusion -- the reduction being somewhere between 30 per cent and 50 per cent. Aspirin is believed to interfere with the biochemical mechanisms that cause cells lining the bowels to become cancerous.
Replacing the "apple a day" theory, aspirin indeed has kept many doctors away, saved many lives, and certainly relieved millions upon millions of fevers, aches and pains. It has been unstoppable, going from strength to strength, and despite competition from paracitamol and ibuprofen, aspirin still outshines and outsells them both. A life-saver for those at risk for heart attacks and strokes, preventing the blood clots that cause them, it is now considered a preventive of one of the nastier types of cancer as well. With 100 glorious years behind it, the future may be even more thrilling for this tiny miracle of pharmaceutical ingenuity -- the world's first truly synthetic drug. It is man's safest, not to mention cheapest pain reliever of all time.
In film vernaculum, aspirin, the most successful medicine in history, takes top billing as the biggest blockbuster drug in the world. Happy birthday and three cheers for the little pill that performs modern miracles, proving once again that 'big things come in small packages!'
