Presented by:    Dealla M.Cahow                2/25/03 

Bayer

Aspirin (OTC)(RX)

ASA. Acetylsalicylic Acid

  


 

History

Aspirin is considered a salicylate derived from Salic Acid.Chinese physicians and Greek physicians such as Hippocretes have used salicylates since 400 BC.The bark and leaves of the willow tree, abundant in salicylic acid was prescribed for pain relief.

The compound acetylsalicylic acid (ASA) may have been originally synthesized by a French Chemist Charles Frederic Gerhardt in 1853. This product was acetosalicylic anhydride, which was similar to ASA. Johann Kraut synthesized ASA in a purer form in 1869.

In 1897, Felix Hoffmann was a chemist who workedfor Bayer pharmaceuticals. He was determined to find relief for his father who suffered from severe arthritis, hence he developed acetylsalicylic acid.

Although Hoffmann is thought to have discovered aspirin, this is debatable, as he may have rediscovered Gerhardt’s formula.

Description

Aspirin is classified as a nonsteroidal anti-inflammatory drug (NSAID). Aspirin is a nonnarcotic analgesic, an anti-inflammatory and an antipyretic. Chemically it is 2-(Acetyloxy) benzoic acid.

Mechanism

As an anti-inflammatory, antipyretic and analgesic drug, aspirin inhibits prostaglandin

synthesis. Prostaglandins are hormones derived from modified fatty acids and respond to tissue injury by releasing chemicals locally in response 

to the injury, which includes redness, heat, swelling, pain and loss of function. 

Indications

Aspirin is the most widely used drug in the world. It is used for the temporary relief of pain for headaches, menstrual pain, muscle aches, pain and fever due to colds, dental related pain, such as toothaches, as well as dental procedures related to pain. 

Recently, the FDA has recommended that aspirin be used to treat transient ischemic attack (TIA) or mini-strokes, heart attacks, and other vascular conditions previously treated by medical procedures such as coronary bypass operations and angioplasty. Furthermore, the FDA recommends aspirin therapy for rheumatologic diseases, such rheumatoid arthritis, juvenile rheumatoid arthritis, osteoarthritis, spondylarthropathies, and arthritis and pleurisy associated with systemic lupus. 

Contraindications

Aspirin should not be taken by:

·Patients who are hypersensitive to aspirin or nonsteroidal anti-inflammatory, including including patients who are allergic to aspirin.

·Patients with gastrointestinal problems including persistent or reoccurring stomach

problems.

·Children or teenagers should not use aspirin for chicken pox or flu symptoms unless a doctor is consulted. Reye syndrome is a rare but serious illness and has been reported to be associated with aspirin. 

·Patients with asthma.

·Women should not use aspirin during the last 3 months of pregnancy unless she has been specifically directed to do so by her doctor.Aspirin may cause problems in the unborn child or complications during delivery. 

·Blood clotting disorders such as hemophilia.

·Uncontrolled high blood pressure.

·Severe liver or kidney disease.


Dosage

A usual adult Dose including children 12 years and over: One or two tablets/caplets 325 to 650 mg with water. May be repeated every four hours as necessary up to 12 tablets/caplets a day or as directed by a doctor. Do not give aspirin to children under 12 unless directed by a doctor.

Administration & cost

Aspirin is administered orally or rectally, and its average cost is it cost approximately $3.00 for 100 tablets of a 325 mg 5 grain dosage. Respectively it cost approximately $8.00 for 100 tablets of a 650 mg 5 grain dosage. 

Precautions and side effects

Overdose

Aspirin can be fatal at 200 to 500 mg/kg. Symptoms include CNS stimulation with vomiting, hyperpnea, 

This quickly progresses to depression, coma, respiratory failure, and collapse. Severe electrolyte imbalance also takes place. 

Although aspirin is a drug commonly used in many house- holds, admissions to hospitals due to aspirin poisoning occur often. Moreover, when people intentionally poison themselves, aspirin is a preferred drug. Children overdosing on Aspirin have been significantly reduced in the United States and the United Kingdom because of the child-resistant packaging required by law. However, children currently continue to overdose on aspirin and consequently need medical attention.

Side effects

Aspirin side effects is said to be uncommon, but may cause the following: 

·Gastrointestinal upset and pain, asthma, rash, kidney disease, coagulation problems, rebound headaches

·Ringing in the ears, loss of hearing, bloody or black stools, wheezing, difficulty breathing, dizziness mental confusion, drowsiness, skin rash, vomiting
 
Warning

Aspirin at dosages of 1,000 milligrams per day has been associated with small increases in blood pressure, blood urea nitrogen, and serum uric acids levels. Patients who are on long-term aspirin therapy should be seen by a physician regularly to determine changes in these meausurements. 

Drug interactions

·Anticoagulants

·Hypoglycemic Agents

·Urocosuric Agents: Aspirin may decrease the effects of probenecid sulfinpyrazone, and phenylbutazone. 

·Spironolactone

·Alcohol: Has a synergistic effect with aspirin in causing gastrointestinal bleeding

·Corticosteroids: Concomitant administration with aspirin may increase the risk of gastrointestinal ulceration. 

·Nosteroidal Anti-inflammatory Agents: Aspirin is contraindicated in patients who are hypersensitive to NSAIDS. 

·Urinary Alkalizers: Decrease aspirin effectiveness by increasing the rate of salicylate renal excretion. 

·Phenobarbital: Decrease aspirin effectiveness by increasing the rate of salicylate renal excretion.

·Phenytoin: aspirin may increase Serum phenytoin levels. 

·Propranolol: May decrease aspirin’s anti-inflammatory action by competing for the same receptors.

·Antacids: Enteric Coated Aspirin should not be given concurrently with antacids, since an increase in the pH of the stomach may affect the enteric coating of the tablets. 

References
Andermann, A., (1996). Physicians, fads, and

pharmaceuticals: A history of aspirin . In

Crossroads where medicine and humanities

meet.[Online]. Available: http:// www. 

Mcgill.ca/mjm/issues/v02n02/aspirin.html.

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Aspirin (2003). Medlineplus Health

Information.,[Online] Available: http://

www.nlm.nih.gov/medlineplus/druginfo/

medmasters/a682878.html.[2003, 

February 11]

Aspirin(2002). ). RxList [Online]. Available:

http:// www.rxlist.com/ cgi/generic/ 

asa_ids.htm [2003, February 11]

Gruenwald, J., (2000). PDR for herbal

medicines, ( 2nd ed.). (pp. 511-513, 808-809)

Montvale, NJ: Medical Economics Company 

New prescribed uses of aspirin: Questions and

Answers (2001). U.S. Food and Drug

Administration Center for Drug 

Evaluation and Research. [Online]. Available:

http: www.fda.gov/cder/news/aspirin/aspirin

QA.htm[2003, February 22]

Warrel, D.A., Weatherall D.J., & Ledingham,

J.G.G., (Eds.). (1987). Oxford textbook of

medicine(2nd ed.). (Vols. 1-12). New York:

Oxford University Press.