Aspirin

 

V. Vemuri

 

I do not have statistics to back me. But, I contend that women consume lot more pain relievers than men. Aside from menstrual cramps, they seem to get more headaches. The women in my office consume aspirin by the bottle. Americans consume over 16, 000 tons of aspirin a year. That is about 80 million pills.

Aspirin has a fascinating history. Back in the fourth century B. C., Hippocrates was aware of the capacity of willow (Salix alba) leaves for relieving pain and fever. Hundreds of years later, in 1763, Rev. Edmund Stone of Chipping-Norton of Oxfordshire observed the same with willow bark and reported it to the Royal Society.

According to German chemist Paul Ehrlich, the story of how aspirin entered our lives can be told in terms of four G's: Geduld (patience), Geschick (skill), Geld (money) and Gluck (luck). Nearly half a century after Rev. Stone tasted willow bark, French and German pharmocologists, driven by national rivalry, found the active ingredient in willow bark. Unfortunately, the process was so expensive that people found it cheaper to chew the leaves. Fortunately, humanity entered the golden age of chemistry. It was the Italian Raffaele Piria who gave the name l'acide salicylique or salicylic acid.

As was the case with much of 19th-century chemistry, French and British scientists were slightly ahead in the chemistry of natural products, but the Germans held the edge in synthetic chemistry. Forced to compete with the French and British chemists in the production of dyes for the burgeoning textile industry, the Germans responded with their synthetic aniline dyes. By 1888 they captured 80 percent of the world market. It is during this German stampede India's indigo industry went belly-up. In response, when the British landlords tried to pass their losses to their Indian tennants, Mohandas Gandhi marched into Champaran and became the Mahatma to the Indian masses. It is also this German heritage that forces us to write acetylsalicylic as one word rather than "acetyl salicylic."

In 1860 Professor Hermann Kolbe and his students at Marburg University synthesized acetylsalicylic acid in the laboratory. In 1874 one of these students, Friedrich von Heyden, established a factory in Dresden to produce synthetic salicylates. Doctors began to use salicylic acid for the treatment of acute rheumatic fever, gout and chronic poly arthritis. But pure salicylic acid was found to have disturbing side effects such as nausea and vomiting. What was needed, clearly, was a buffering agent. Felix Hoffman, a young chemist working in the Friedrich Bayer laboratories, found the answer in acetylsalicylic acid. Hoffman's search for a safe and effective pain reliever was personally inspired. Suffering from the crippling effects of rheumatoid arthritis, Felix's father became an invalid and Felix was desperately looking for a way to relieve his father's suffering. His answer is acetylsalicylic acid. Bayer's director decided to name the drug Aspirin, a from acetyl and spirin from the German Spirsaure, "because acetylsalicylic acid is hard to pronounce, hard to remember and impossible to patent." Thus the German scientists won the aspirin war, but the German politicians lost the war in the battle field.

During World War I, the U. S. government seized many German properties. At the end of the war, these were auctioned off and Sterling Drug Inc., an American pharmaceutical company, bought one of them. As it took an inventory of what it had bought, the company found out that it had acquired the rights to a little-known medicine whose patent was held by Friedrich Bayer Co. of Dusseldorf. The thing they had picked up was Aspirin.

We do not capitalize aspirin anymore. Like other trade names such as cellophane, linoleum and xerox, it has become a generic word. Even doctors, who generally use scientific names while prescribing medications, do not call it acetylsalicylic acid any more, they simply call it aspirin. Perhaps it is the most widely used drug in the world today. In the United States you can buy about 400 tablets for a dollar.

Berton Roueche, in his book "The Incurable Wound" thus sings in praise of aspirin: "There are no countries in which (aspirin) is unknown, unappreciated, or unavailable. It is, in fact, the most widely used drug on earth. It is also the cheapest... one of the safest, and, among drugs of a comparable nature... without much doubt the best. Some authorities go further than that. They consider it the most useful drug in the armamentarium of medicine."

There are several remarkable things about this drug. For starters, even now, scientists do not know how the drug works. Or, why it works. While it is clear that this amazing drug can block pain, reduce fever and suppress joint inflammation, researchers are convinced that the processes by which it does all these things are totally unrelated. However, some clues are beginning to emerge. Renal physiologists noticed that large doses of salicylates promote the excretion of uric acid by the kidneys. This property explains the utility of aspirin and other salicylates in treating gout. The first satisfactory mechanism for the action of aspirin was proposed in 1971 by John Vane, who received the Nobel Prize in 1982. Vane demonstrated that aspirin, among others, inhibited the synthesis of prostaglandins which, in turn, are known to be responsible for inflammation, redness and heat (fever). The persuasive aspect of this hypothesis is the convincing manner in which it explained the most troublesome side effect of aspirin-like drugs - stomach irritation and ulceration. These drugs cause this irritation because they block the synthesis of prostaglandins that the stomach lining needs to regulate the overproduction of acids. Another side effect of aspirin is interference with the clotting of blood by inhibiting the platelet aggregation. This discovery was the basis for using aspirin to prevent strokes and heart attacks: carefully calibrated doses can interfere with the production of platelet-aggregating thromboxane. Now, upon doctor's advise, hundreds of thousands of people, all over the world, take aspirin to treat or prevent strokes and heart attacks.

Another mind boggling property of aspirin can be appreciated by looking carefully at how it reduces fever. If you have a fever of 103 degrees and you take prescribed doses of aspirin at regular intervals, your temperature starts to decline - say to 102.7, to 101.9, to 99.6 - until it reaches your normal body temperature. There its effects will stop. If you continue to take aspirin, it will have no further effect in reducing your temperature - not even by tenth of a degree. Nobody knows why.

 


rvemuri@ucdavis.edu
Thursday he 8th, May 1997