The uses and mechanism of action of Ibuprofen

Description

Ibuprofen is an organic compound with the chemical formula C13H18O2. Its chemical name is 2-(4-Isobutylphenyl)propionic Acid. This small molecule is a white to off-white powder and practically insoluble in water, freely soluble in acetone, methanol, and methylene chloride. This drug is the most commonly used and prescribed NSAID. It is a common over-the-counter medication widely used as an analgesic, anti-inflammatory, and antipyretic.

Discovery

The discovery of ibuprofen was spurred by finding an alternative non-corticosteroid pharmacotherapy for rheumatoid arthritis. The disease was the initial impetus for creating what would eventually become known as ibuprofen. Initially patented as 2-(4-isobutylphenyl) propionic acid in 1961 by Dr. Adams and John Nicholson, ibuprofen has become one of the most widely used NSAIDs worldwide.

Uses

Ibuprofen is FDA-approved for use in mild to moderate pain, including menstrual pain (pain that happens before or during a menstrual period). Prescription ibuprofen relieves pain, tenderness, swelling, and stiffness caused by osteoarthritis (arthritis caused by a breakdown of the lining of the joints) and rheumatoid arthritis (arthritis caused by swelling of the lining of the joints). Some common over-the-counter uses for ibuprofen are muscle sprains or strains, joint aches, pain from migraine, sore throat, and pain from colds or cases of flu.

Its most well-known effect, in addition to relieving menstrual cramps in women, is undoubtedly its antipyretic effect. Fever has been reported as a common symptom occurring in COVID-19 illness. This medicine is often used as a fever reducer after contracting COVID-19 fever[2]. Individuals often take over-the-counter antipyretics such as ibuprofen and acetaminophen to reduce fever discomfort. Studies show that ibuprofen demonstrates superior efficacy in fever reduction compared to acetaminophen.

Mechanism of action

The primary mechanism of action of ibuprofen is the non-selective, reversible inhibition of the cyclooxygenase enzymes COX-1 and COX-2 (coded for by PTGS1 and PTGS2, respectively)[2]. COX-1 and COX-2 catalyze the first committed step in the synthesis of prostanoids-prostaglandin (PG)E2, PGD2, PGF2X, PGI2 (also known as prostacyclin), and thromboxane (Tx) A2-from arachidonic acid. Prostanoids produce a diverse array of biological effects through activating prostanoid receptors and play essential roles in various homeostatic and pathologic processes.

References

[1] Jamerson, Brenda D , and T. H. Haryadi . "The Use of Ibuprofen to Treat Fever in COVID-19: A Possible Indirect Association with Worse Outcome?."Medical Hypotheses 144(2020).

[2] Liudmila L Mazaleuskaya. "PharmGKB summary: ibuprofen pathways." Pharmacogenetics and genomics 25 2 (2015): 96–106.