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Science and Environment

Aspirin: From bitter powder to wonder drug

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Acetyl salicylic acid, more popularly known as aspirin, is a known analgesic (relieves minor aches and pains), antipyretic (reduces fever), and anti-inflammatory (reduces inflammation to remedy pain).

Through the years, it has also been found to have antiplatelet (“blood-thinning”) effect, and is recommended in low-doses to prevent heart attacks and stroke.

In 5th century B.C., Greek physician Hippocrates, who was later recognized as the father of modern medicine, wrote about a bitter powder extracted from the bark of a willow tree that could remedy headaches and other bodily pains, even fever.

On the basis of Hippocrates’ writings, some scientists took notice of the importance of this pain-relieving compound. In 1828, a professor of pharmacy at the University of Munich, Johann Buchner, found a way to isolate the compound from the plant, which caused its pain-relieving effect. It was a yellow, bitter and “needle-like” crystal, which he called salicin.

By 1829, Henry Lenoux, a French chemist invented a procedure to isolate more salicin from tree barks. He took 1.5 kg of a willow bark and acquired almost 30g of salicin from it.

In 1838, Raffaele Piria, an Italian chemist based at Sorbonne in Paris split the compound into sugar and a sweet-smelling compound. This sweet-smelling compound underwent the process of hydrolysis and oxidation. Piria called the resulting acid as salicylic acid, which was the purest form of the compound that caused pain relief.

But the problem with the purest form, however effective it was to relieve pain, was that it could not be tolerated in the stomach. And so, a German chemist named Charles Frederic Gerhardt in 1853 attempted to neutralize the strong attribute of the acid. He made use of sodium (sodium salicylate) and acetyl chloride, which resulted in acetylsalicylic acid. However, Gerhardt, despite his success in neutralizing the acid, did not persist in marketing his work.

Gerhardt’s work then became the basis of another German chemist named Felix Hoffman who rediscovered the procedure and tried it with his own father who was suffering from arthritis. In his amazement, the formula worked and so he started convincing his company to finance the drug.

Soon after, the company agreed to finance the production of the acid, which was patented on March 6, 1889. The company also came up with the name popular even at present: Aspirin.

The “a” came from the acetyl chloride used in neutralizing, “spir” came from spiraea ulmaria (the scientific name of the tree they derived the substance from) and “in” was just a trend as a medicine name ending during the time.

Since that day, the use of aspirin as a pain reliever and subsequently as a blood-thinning agent became popular. Today, aspirin is a recommended daily treatment to reduce the risk of cardiovascular events like heart attack and stoke.

Aspirin is usually taken in 81 mg form or more on a daily basis until recently when several clinical trials found the adverse effect of high doses of aspirin in patients.

High aspirin doses were found to cause hemorrhagic stroke or stroke caused by bleeding brain blood vessels, according to Dr. Joann Manson, lead investigator of a review of six clinical trials involving 70,000 participants at the Brigham and Women’s Hospital.

“We wanted to find out whether there was strong evidence favoring higher or lower doses of aspirin,” said Dr. Charles Campbell, assistant professor of medicine at the University of Kentucky.

Campbell was the lead investigator in another review of 11 clinical trials, involving 47,000 participants, that compared the effects of high and low dosage of aspirin.

Campbell and his team found that a lower dose of aspirin had a comparable beneficial effect to higher doses but with reduced risk for adverse effects.

“People should evaluate their need for aspirin with their physician… But they shouldn’t take any more than an 81 mg chewable or baby aspirin a day,” said Campbell.

A low dose aspirin that is made to suit daily administration with minimal adverse events is available in the country. It is a heart-shaped aspirin manufactured by Filipino-owned Pascual Laboratories Inc. and is available in leading drugstores nationwide. Patients are advised to consult their doctor for the best medicine for their condition.

ACID

ASPIRIN

BRIGHAM AND WOMEN

CHARLES FREDERIC GERHARDT

DR. CHARLES CAMPBELL

DR. JOANN MANSON

PLACE

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