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Abstract
Aspirin, a medicine that dates back to the times of ancient Sumeria and Egypt, has played a vital role in helping with inflammation and pain. Felix Hoffman is responsible for what we know aspirin is today. At first, it was salicylic acid, and it was too harsh on the stomach to be taken. Felix modified the hydroxy group and this allowed it to not cause people’s stomachs to get upset. In modern times aspirin is not just used for pain and inflammation relief. Aspirin can be beneficial in the prevention of heart disease. Aspirin is one of the oldest pain and inflammation-reducing medicines. Aspirin is categorized as a nonsteroidal, anti-inflammatory drug. This family of drugs also includes ibuprofen. The nonsteroidal anti-inflammatory drugs prostaglandins from being produced by the cyclooxygenase enzymes. Prostaglandins have many important functions. They are responsible for inflammation, which is important for healing but also causes pain and fever. Although aspirin has many benefits such as pain inflammation and fever, the risks cannot be simply overlooked. Aspirin can be very harmful if not taken correctly or if taken on a daily schedule.
Aspirin has a long history dating back more than 2000 years ago. A synthetic substance derived from salicylic acid which is found naturally occurring in the bark of the willow tree, aspirin has many positive uses for patients with a number of different ailments. Along with the positive uses of aspirin, there are also risks and dangers, and side effects. Aspirin is part of the non-steroidal anti-inflammatory (NSAID) family of drugs that has been studied and researched many times over.
History of aspirin
From as early as 1500 BC, willow was being utilized for medicinal purposes by ancient civilizations such as the Sumerians and the Egyptians. Sometime around 400 BC, Hippocrates used willow leaf tea to help women and the pain experienced in childbirth. Fast forward to 1763. The Royal Society released a report containing the specifics of a five-year study of the use of the willow bark in powered form that was able to cure a fever. In 1828, Joseph Buchner was successful in the extraction of the active ingredient from willow. He named the substance salicin. Charles Frederic Gerhardt found that he was able to change the components the salicylic acid because he introduced an acetyl group in place of a hydroxyl group. His changes made him one of the first to develop aspirin, but this new compound was very unstable and prevented him from developing it any further (Goldberg, 2009). Felix Hofmann has also been accredited for the development of aspirin as it known today. Arthur Eichengrün, the manager of chemical research at Bayer, assigned Felix to innovate aspirin. He took this task personally since his father was suffering from rheumatism and couldn’t ingest the salicylic acid without throwing up. He altered the salicylic acid chemically by modifying the hydroxyl group on the benzine ring. This allowed aspirin to be absorbed without intense gastrointestinal distress. After the stomach processed the new molecule, it converted back to salicylic acid. This provided the medical benefits of aspirin (Connelly, 2014).
The components and properties of aspirin
The chemical name for aspirin is acetylsalicylic acid. It is an odorless, colorless or white, crystalline powder that has a bitter taste. Aspirin melts at a point of 275°, while the boiling point is 284°. Its density is 1.4g/cm³ and its molecular weight is 180.16 g/mol. Aspirin is created by combining salicylic acid and acetic acid. The chemical formula for salicylic acid is C7H6O3, and the chemical formula for acetic acid is CH3COOH. C9H8O4 is the chemical formula for acetylsalicylic acid, so it contains nine carbons to eight hydrogens to four oxygens, at that ratio. Aspirin also has 3 functional groups within the compound, which are the carboxylic acid group, ester group, and the aromatic group, also known as a benzene ring. The groups work together to form the compound and give it the characteristics that aspirin has (Baarnseweg & Dijk, 1990).
How aspirin works
Aspirin acts as an acetylating agent. Therefore, it inactivates cyclooxygenase and reduces the production of prostaglandin. Prostaglandin is a hormone-like substance that is produced on sites of damage or infection in the human body. The prostaglandins cause inflammation, fever, and pain. This only happens because of aspirin’s acetyl group. It bonds to Ser529 at the active site of the cyclooxygenase enzyme. Ser529 plays an important role in immune and inflammatory responses. As aspirin interacts with Arg120, it blocks access of arachidonic acid to the hydrophobic channel to Tyr385. The arg120 is found at the beginning of the hydrophobic channel, which is where prostaglandin is synthesized. Therefore, aspirin stops the production of prostaglandin (Mekaj, Daci, & Mekaj, 2015).
Within in the human body, aspirin is absorbed with expedience in the stomach and intestine by means passive diffusion. Passive diffusion is the movement of molecules across a membrane without the need of energy. It requires no energy because it is moving from an area of high concentration to low concentration. In the case of aspirin, the membrane is the stomach lining and the lining of the intestine. Aspirin is converted into salicylate acid in the stomach, in the blood, in the intestinal mucosa, and mostly in the liver. Salicylate is the anti-inflammatory and pain-reducing agent of aspirin. Salicylate then spreads throughout the body at a rapid rate. It attaches to albumin in the plasma. Albumin is a protein within the plasma that transports fatty acids, hormones, and other compounds. Aspirin is mainly metabolized in by the liver and it occurs by hepatic conjunction with glycine or glucuronic acid. Glycine helps prevent the unpleasant side effects of aspirin. The conjunction with glycine occurs most often. in cases of low-dose aspirin use, it is estimated that 90% salicylate metabolism happens through the glycine pathway. The salicylate the human body does not use is secreted through urination. This accounts for 10% of the complete elimination of salicylate in the body (Aspirin Pharmacokinetics, n.d).
The benefits of aspirin
Aspirin has many medical benefits. The drug can be used to combat mild to moderate pain. This is helpful with things like headaches, toothaches, and menstrual cramping. Aspirin can also be used to fight cold and flu-like symptoms. Aspirin fights these symptoms by reducing fever, which benefits able to feeling better. Additionally, aspirin is beneficial as an inflammation reducer (“Aspirin for Pain Relief”, 2018). Acute Inflammation is good; it is the body’s natural defense and it encourages healing. On the other hand, when the inflammation is chronic, it can damage the body instead of healing it. So, in cases of chronic inflammation aspirin can be very advantageous (Hobson, 2017).
One of the main benefits of aspirin is the prevention of cardiovascular disease and reducing the risks of heart attack and stroke with high-risk patients. Aspirin can reduce myocardial infarctions, strokes, and heart attacks by around 25% regardless of the age and sex of the high-risk patients. High-risk patients are identified by several factors: high blood pressure, high cholesterol, whether or not her or she smokes, the patient’s age, and their family history (Szczeklik, 2006).
The risks of aspirin
Although aspirin can be very benefit able, the health risk cannot be overlooked. First of all, the preventative qualities related to cardiovascular disease can cause a bleeding stroke because of the thinning of the blood. Another major risk of is gastrointestinal bleeding. It causes gastrointestinal bleeding because it blocks all the helpful substances that protect the stomach lining. As a result, it causes an upset stomach and bleeding in the stomach and intestine. The bleeding can get extremely serious and could cause hospitalization, with a blood transfusion. Allergic reactions can also occur with taking any amount of aspirin. An aspirin allergic reaction can be very serious. The symptoms include itchy rashes, flushing or blushing, and blocked nose, and asthma. Asthma can be very severe and cause an asthma attack, which could cause death (Whiteman, 2015).
Aspirin continues to be one of the most popular drugs in the world. With its properties that aide in reducing pain, fever, and inflammation, aspirin additionally helps to reduce the risk of heart attacks in some people. The chemical properties of aspirin make it a versatile drug that is affordable and effective for many ailments. From its beginnings in the willow tree, aspirin has developed into a drug that has withstood time and some controversy.
References
- ASPIRIN PHARMACOKINETICS. (n.d.). Retrieved from https://sepia2.unil.ch/pharmacology/index.php?id=83
- Connelly, D. (26 September 2014). History of aspirin. The Pharmaceutical Journal. Retrieved April 3, 2019.
- Goldberg, D. R. (2009, Summer). Aspirin turn of a century miracle drug. Distillations.
- Hobson, K. (2017, July 21). Is inflammation bad for you or good for you? Retrieved April 3, 2019, from https://www.npr.org/
- Mekaj, Y. H., Daci, F.T., & Mekaj, A. Y. (2015). New insights into the mechanisms of action of aspirin and its use in the prevention and treatment of arterial and venous thromboembolism. Therapuetics and clinical risk management, 11, 1449-1456. Doi:10.214/TCRM.S92222
- Should you take a daily aspirin for your heart? (2019, January 09). Retrieved April 3, 2019, from https://www.mayoclinic.org/diseases-conditions/heart-disease/in-depth/daily-aspirin-therapy/art-20046797
- Szczeklik, A. (n.d.). The History of Aspirin: The Discoveries That Changed Contemporary Medicine. Retrieved from http://www.pas.va/content/dam/accademia/pdf/acta18.pdf
- Whiteman, H. (2015, October 29). Aspirin: is it really a ‘wonder drug’? Retrieved from https://www.medicalnewstoday.com/articles/301766.php
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