Aspirin And Modern Health

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INTRODUCTION

Aspirin, also known as acetylsalicylic acid (ASA), is a medication used to reduce pain, fever, or inflammation. Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, pericarditis, and rheumatic fever. Aspirin given shortly after a heart attack decreases the risk of death. Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk. It may also decrease the risk of certain types of cancer, particularly colorectal cancer. For pain or fever, effects typically begin within 30 minutes. Aspirin is a nonsteroidal anti-inflammatory drug (NSAID) and works similarly to other NSAIDs but also suppresses the normal functioning of platelets.
One common adverse effect is an upset stomach. More significant side effects include stomach ulcers, stomach bleeding, and worsening asthma. Bleeding risk is greater among those who are older, drink alcohol, take other NSAIDs, or are on other blood thinners. Aspirin is not recommended in the last part of pregnancy. It is not generally recommended in children with infections because of the risk of Reye syndrome. High doses may result in ringing in the ears.
A precursor to aspirin found in leaves from the willow tree has been used for its health effects for at least 2,400 years. In 1853, chemist Charles Frédéric Gerhardt treated the medicine sodium salicylate with acetyl chloride to produce acetylsalicylic acid for the first time. For the next fifty years, other chemists established the chemical structure and came up with more efficient production methods. In 1897, scientists at the Bayer company began studying acetylsalicylic acid as a less-irritating replacement medication for common salicylate medicines. By 1899, Bayer had named it “Aspirin” and sold it around the world. Aspirin’s popularity grew over the first half of the twentieth century leading to competition between many brands and formulations. The word Aspirin was Bayer’s brand name; however, their rights to the trademark were lost or sold in many countries.
Aspirin is one of the most widely used medications globally, with an estimated 40,000 tonnes (44,000 tons) (50 to 120 billion pills) consumed each year. It is on the World Health Organization’s List of Essential Medicines. As of 2014, the wholesale cost in the developing world is US$0.002 to US$0.025 per dose. As of 2015, the cost for a typical month of medication in the United States is less than US$25.00. It is available as a generic medication. In 2017, it was the 42nd most commonly prescribed medication in the United States, with more than 17 million prescriptions.

Aspirin

 Usages:

Drug Bank = BD00945

Drug Use:

Aspirin is widely used to relieve mild to moderate pain, fever or inflammation. Also used to treat Kawasaki disease, pericarditis and rheumatic fever. Aspirin is given shortly after heart attack to decrease the risk of death. Aspirin is also served to treat muscle aches, toothaches, headaches, flu, common cold, and swelling. Aspirin also used for acne and callus treatment.

Aspirin is served as swallowable tablets or suppositories.

Chemical properties:

Aspirin is weakly acidic white crystal-like substance. At 25’c temperature, the dissociation constant (pKa) of aspirin is 3.5

Aspirin is stable in dry air although in moisture air, it gradually to acetic acids and salicylic acid.

It decomposes rapidly in solutions of ammonia acetate.

Aspirin (C9H8O4, IUPAC name: 2-Acetoxybenzoic Acid) is an acetyl derivative of salicylic acid.

 

Physical Properties:

Molecular weight         180.16 g/mol

Melting point               136’c

Boiling point                140’c

Solubility in water        3 g/l

Crystal structure         Polymorphism

 

Aspirin Synthesis:

Aspirin is prepared from salicylic acid reacting with acetic anhydride. This process is carried out  in the presence of little amount of strong acid as catalyst to speed up the reaction.

Aspirin is made in an esterification reaction. With an acid derivate, acetic anhhydride, Salicylic acid is treated causing the salicylic acid’s hydroxyl group turns into an ester (-OH → -OCO-). This reaction yields acetic acid and aspirin as byproduct.

For this reaction, sulfuric acid (sometimes phosphoric acid) is used as catalyst in a very small amount.

 

Eating fruits and vegetables provides benzoic acid in animal body. And animal body makes it’s own salicylic acid.

Industrial Production of aspirin:

For large scale acetylsalicylic acid manufacturing, mostly batch process operation is followed. Where the salicylic acid is reacted with excess of acetic anhydride. And strong acid catalyst like phosphoric acid is used. Aspirin is one of the most manufactured medicine for long time.

Aspirin is mostly sold as tablet form, to produce it, to the active ingredient (acetylsalicylic acid) corn starch and water are added as both filler and binding agent. A little lubricant is added while mixing and while the tablets are compressed.

 

 

History of Aspirin:

Use of aspirin can be dated as long as human civilization goes back in time. In an ancient Egyptian medical script (Ebers Papyrus, BCE 1443), the use of willow and myrtle (salicylate – rich plant) is found to treat fever and pain.

400BC, ancient Greek physician, Hippocrates referred tea from willow leaf to women as reliver of childbirth pain.

In 1763 The Royal Society published a report about experiments of using dried willow bark to cure fevers, a five years research conducted by Edward Stone. And in that same year Aspirin broke into the European market.

Although the modern aspirin we know was first discovered in the late 1890 by German chemist Felix Hoffmann and Bayer in the form of acetylsalicylic acid. And in 1899 Bayer distributed a powder containing acetylsalicylic acid (a modification of salicylic acid, in which the phenol group is replaced by ester) to physicians to give to patients as pain reliever. And he named this powder Aspirin.

In 1982 The Nobel Prize was given to John Vane, pharmacology professor at University of London for his publication of research the action mechanism of aspirin in 1971.

In 1998 the results from hypertension optimal treatment trial shows that aspirin reduces major cardiovascular events and prevent heart attack. And in 2005 WHS (Women’s Health Study) suggested that aspirin lowers the stroke risk.

 Since The discovery of modern Aspirin, it is one of the most sold drugs all over the world. Till this day, over 10 billion standard Aspirin tablets are produced and consumed which equivalent to 35,000 metric tons of Aspirin.

Action of Aspirin

An Aspirin tablet contains 300-400 mg of aspirin with a starch binder with other ingredients, such as caffeine, buffer and filler. In animal body it is broken down to the basic form, salicylic acid in a very small amount and then absorbed into blood stream.

Aspirin prevents blood clotting by preventing the formation of prostaglandin, a natural substance in animal body. The main function of aspirin is to work as enzyme inhibitor to cycloxygenase1 and cyclooxygenase 2 enzymes, which are responsible for producing prostaglandin.

Aspirin is non-selective and irreversible inhibitor for both COX-1 (PTGS1) and COX-2 (PTGS2), two different cyclooxygenases responsible to produce prostaglandins, most of which are pro-inflammatory and thromboxane. Which cause blood clotting. Aspirin transfer it’s acetyl group to the enzyme and prevents it’s activity.

Aspirin also prevents strokes and heart attacks by lowering the synthesis of thromboxane, the chemical substance responsible for making platelets sticky. When aspirin is served, it inhibit platelets to form thromboxane and thus blood can not clot which can block artery.

Aspirin works as pain reliver. When nerve system sends a certain electric signal to brain, the patient senses pain. When getting injure, the damaged tissue releases prostaglandins, a chemical which like a hormone cause the tissue swell. Prostaglandins also intensify the electric signal from the injured tissue to brain. This increases the pain the patient feels. Serving aspirin causes the prevention of the enzymes responsible for prostaglandins. That results less pain and less swelling.

Aspirin also restore hair after chlorine damage and it shows dandruff controlling properties.

wide range of patients, aspirin therapy reduces by about one quarter the risk of subsequent occlusive vascular events, with comparable reductions in men and women

So, we see Aspirin works on patient body in various ways. And that is the reason aspirin is served as cure for many diseases. Aspirin can treat more than 50 health disorders.

The anti-blood clotting mechanisms improve the blood flow to the brain and it may reduce the risk of developing Alzheimer’s disease.

Some studies show that aspirin reduces risks of kidney failure for diabetic patients, reduce the risk of cancer, reduces the risk of blindness and breast cancer.

Aspirin also can be used to relief from pain and irritation of bug stings. For that the aspirin tablet is rubbed on wet. skin.

Aspirin and Health concerns:

Sometimes serving aspirin sometimes cause Nausea, Vomiting, Heartburn. Also, aspirin might cause stomach ulcers or stomach bleeding.

Sometimes aspirin might worsen asthma, and overdose of aspirin might cause hyperventilation. So asthma must be taken under consideration before suggesting aspirin.

The bleeding risk is greater while a patient goes through surgery or accidents, as Aspirin prevents the blood clotting agent formation.

Some patients also might be allergic to aspirin (NSAID-non-steroidal anti-inflammatory drug), which cause them experiencing rash, swelling eyes, face, throat and difficulty in berating. So, the doctor must know about the patient’s allergies before prescribing aspirin or in case any medicine with an allergy effect.

Aspirin and Reye’s syndrome:   Reye’s syndrome is rare but fatal disorder that damages the brain and liver. This effect mostly seen in children, but it might happen at any age. Providing Aspirin treatment to a child who recently had gone through a viral infection like flu or chickenpox increases the risk of Reye’s syndrome. That’s why it’s better not to give aspirin to a child or teenager with flu symptoms, fever, or chicken pox.

People who regularly take aspirin and drink alcohol or serve drug, they might have big risk of stomach bleeding.

If someone taking aspirin, need a surgical procedure or dental work, they must discuss with the surgeon or dentist that you take daily aspirin and how much. Because aspirin risks excessive bleeding during surgery.

Aspirin Increases the risk of tinnitus. Who serves high dose of aspirin sometimes experience tinnitus (feeling like ringing in the ear)

Aspirin (as well as other non-steroidal anti-inflammatory -NAIDS) drugs, are not recommended during pregnancy, especially in the last trimester. As aspirin affects blood clotting, it may increase the risk of bleeding in the mother or fetus.

NSAIDS may also affect the ability of a blood vessel in the baby’s heart to close.

Patient with bleeding disorder such as haemophilia might not suit aspirin treatment. 

Aspirin might increase the risk of gastrointestinal bleeding or haemorrhagic stroke.

Because of the Reye’s syndrome, aspirin is not suitable for children under 16. Howeve3r, a specialist may prescribe aspirin for a child under supervision if they have Kawasaki disease and to prevent blood clotting from forming after heart surgery.

Also, one should not stop serving aspirin or any medicine without discussing with their doctor.

 

Conclusion:

The industrial production of low-priced aspirin lowered the death rate by few percent. That is the reason, Aspirin was called the wonder drug. Still to date, t is served to cure numerous types of disorders and diseases. So, this remedy is one of the most necessary things around the world. There was a proverb, ‘An aspirin a day, keep diseases away’.

However, the patients and the doctors must be considerate about the potential side effects of aspirin. Because ‘An aspirin a day’ is not for everyone.

Aspirin is one of the most served drug so research must be carried on to keep the production of aspirin up with the demand to make sure this cure will be available to everyone. Also, the purpose of the research should be making this most served drug safer.

References:

 

Sunitha V. Ittaman and MD,* Jeffrey J. VanWormer. The Role of Aspirin in the Prevention of Cardiovascular Disease. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4317158/

 

Jaqui Walker,1 Pippa Hutchison. Aspirin: 120 years of innovation.   https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5834311/

Selamat detang ke portal rasmi myhealh Kementerian Kesihatan Malaysia

http://www.myhealth.gov.my/en/aspirin-2/

 

Wikipedia       https://en.wikipedia.org/wiki/Aspirin

You might be interested in more science blogs.

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