ASPIRIN: The Wonderful Pill |PharmD India

It's been 100 years since the Bayer Company introduced aspirin. It was greeted as a miracle drug then and a century later, continues to astound scientists with its many health benefits.

Although best known for its role in relieving headache and other kinds of pain, studies over the past several decades have shown aspirin can play a role in helping to prevent and treat heart attacks and may reduce risk of colon cancer.

1) How Aspirin Works

- The use of salicylates, the chemical root of aspirin, goes back to the 5th century B.C., when Hippocrates used the bark of the willow tree to treat fevers and pain. It's come a long way since.

2) Potential Hazards

- Should you take one a day? Balance the benefits and risks.

3) Aspirin Timeline

- Great moments in the history of America's favorite remedy.

4) The Best Pain Reliever?

- Aspirin, acetaminophen or ibuprofen? It all depends on what ails you.

The use of salicylates, the chemical root of aspirin, goes back to the 5th century B.C., when Hippocrates used the bark of the willow tree to treat fevers and pain. Despite widespread use of willow bark, its active ingredient, salicin, wasn't discovered until 1828. In the 1830s, salicin was refined into two similar medicinal compounds, salicylic acid and sodium salicylate. Unfortunately, these remedies had side effects that made them unattractive as pain relievers, including nausea, ringing in the ears and severe stomach irritation.

In 1897, in an attempt to ease his father's suffering from rheumatoid arthritis, Felix Hoffmann, a chemist working for Bayer, discovered a milder formulation called acetylsalicylic acid (ASA). This compound was called "Aspirin" —"A" from acetyl, "spir" from the spirea family of plants from which salicin was derived and "in" referring to a common ending in drug nomenclature.

Aspirin was immediately heralded as an excellent medication for controlling fever and reducing pain, especially from arthritis and headache. Plus, in the 1950s, some physicians began to prescribe aspirin for prevention of heart attacks because of its observed blood-thinning ability. Remarkably, no one knew how aspirin worked.

In 1971, the mystery was, for the most part, solved by British pharmacologist John Vane. Although many scientists believe that there is still much to discover about aspirin, careful experimentation has revealed that aspirin controls body compounds called prostaglandins.

Prostaglandins are hormone-like substances produced in small quantities throughout the body. There are many different types of prostaglandins, and each performs a different function. Some cause inflammation, redness and swelling in response to an injury or illness. Others are responsible for the general "housekeeping" of the body — keeping things running smoothly by protecting the gastrointestinal lining, for example.

Aspirin works by decreasing the production of prostaglandins. Because prostaglandins are involved in so many different body functions, aspirin can have many different types of effects on the body, both positive and negative. Aspirin can:

Reduce fever by inhibiting prostaglandins that work to raise body temperature.
Relieve headache and other pain by inhibiting prostaglandins responsible for inflammation and by dampening pain sensations. Even with all the other treatments available, aspirin is still considered quite effective against migraine headaches and arthritis.
Reduce swelling by inhibiting prostaglandins that respond to injury sites.
Reduce risk of heart attack and ischemic stroke. Aspirin inhibits prostaglandins that are responsible for platelets sticking together to form blood clots. Aspirin or other types of platelet inhibitors are usually prescribed for patients who are known to have or are at risk of blockages in the blood vessels that supply blood to the heart (coronary artery disease). Patients who have had a stroke or transient ischemic attack (TIA, or "mini-stroke") will usually take aspirin or another anticlotting medicine to prevent future stroke.
Treat heart attacks (myocardial infarctions). Heart attack patients who are treated immediately with aspirin have better outcomes and a reduced risk of second heart attacks and strokes.
Potentially reduce the risk of colon cancer. Although the data are not conclusive, there is some evidence that regular use of aspirin reduces the risk of developing colon cancer and precancerous polyps. The optimal dosage required is not yet known, but at least one study has found that just 80 milligrams of aspirin a day, the equivalent of one "baby aspirin," is enough to reduce production of certain prostaglandins suspected to be involved in tumor formation.

One of the most confusing questions at the drug store is what pain reliever to use — aspirin, acetaminophen, ibuprofen or another type?

Each pain reliever is chemically distinct, and we all respond differently to them depending on our own body chemistry and the particular problem we are experiencing. An individual may respond to one pain reliever but not to another.

Work closely with your pharmacist or physician to determine which medication in which dosages might be best for you. Whichever pain reliever you choose, don't exceed the dosage recommended on the label without consulting your doctor.

Here are some basic differences:

Acetaminophen

· Controls pain well and can bring down a fever.

· Gentler on the stomach than aspirin.

· Does not control inflammation.

· Can cause liver damage if taken in high doses, especially in people who drink large amounts of alcohol regularly.

Aspirin (any brand)

· Controls pain, inflammation and fever.

· Should not be taken by people with nasal polyps and asthma or anyone taking a blood-thinning medication without medical advice.

· Should not be given to children who may have a viral illness.

· Harshest on the stomach. Can cause gastric irritation, ulcers and bleeding.

Ibuprofen

· Controls pain, inflammation and fever.

· Works well against menstrual cramps.

· Can cause gastric irritation and bleeding.

· Interferes with blood clotting but to a lesser degree than aspirin.

Great Moments in Aspirin's History

400 BC: Hippocrates uses willow bark on patients to reduce fevers and pain. Willow bark is later found to contain salicin, the same active component as aspirin.
1763: The Royal Society of London publishes an article by the Rev. Edward Stone, "Account of the success of the Bark of the Willow in the Cure of Agues," officially reporting what had been folklore for centuries.
1828: The active ingredient in willow bark, salicin, is chemically separated.
1839: French chemists synthesize salicylic acid from salicin, which is later used medically.
1853: French chemist Charles Frederic Gerhardt first creates a crude form of acetylsalicylic acid, but its medical uses are not yet recognized.
1897: German chemist Felix Hoffmann modifies salicylic acid to acetylsalicylic acid to make it less harsh on the stomach. Since he worked for Bayer, the company got the patent.
1899: Acetylsalicylic acid is named Aspirin by Bayer. By November of this year, Aspirin is in wide-spread use.
1917: Bayer's patent on Aspirin runs out, allowing other companies to sell acetylsalicylic acid. Bayer retains the trademarked name, "Aspirin."
1920: Bayer loses its trademark of the name "Aspirin" in court. This reduces "aspirin" to a generic word for any brand of acetylsalicylic acid.
1950: Dr. Lawrence L. Craven of California describes his observations about aspirin's action as a blood-thinner, and begins prescribing daily doses to his patients as a means of preventing heart attacks.
1971: British pharmacologist John R. Vane discovers aspirin's mechanism of action — that it inhibits the production of hormone-like substances in the body called prostaglandins.
1982: Sir John R. Vane is co-winner of the Nobel Prize in Medicine for his discoveries concerning prostaglandins.
1988: Results of the Physicians' Health Study show that aspirin significantly reduced risk of first heart attack.
1990s: Studies show regular use of aspirin may reduce risk of colon cancer.
2005: Research shows that aspirin reduces the risk of stroke in healthy women, although no clear benefit is seen for prevention of heart attack.