Ibuprofen (Motrin®, Caldolor®, Advil®)

Overview

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) and non-selective cyclooxygenase inhibitor indicated for the treatment of mild-moderate pain, fever, and arthritis.  Its analgesic, antipyretic, and anti-inflammatory properties are thought to be mediated through inhibition of the cyclooxygenase-2 (COX-2) enzyme.  COX-2 is upregulated by cells during the inflammatory response, resulting in increased production of PGE2 and leading to tissue inflammation, fluid extravasation, pyrexia, pain, and vasodilation.  Inhibition of prostaglandin synthesis by ibuprofen blocks inflammatory signaling pathways and decreases pain and body temperature.

Ibuprofen is available over-the-counter in the United States, and via prescription at higher doses.  It is approved for the treatment of rheumatoid and osteoarthritis, primary dysmenorrhea, fever reduction and mild-moderate pain.  It is also used off-label for several conditions including systemic lupus erythematosis and acute gout flares.  Ibuprofen use is generally well-tolerated but increases risk of gastric and duodenal bleeding and perforation, as well as potentially fatal thromboembolic events such as myocardial infarction and stroke.

It has been suggested that several of the adverse effects associated with ibuprofen use arise due to blockade of the COX-1 enzyme.  Whereas COX-2 expression is associated with tissue inflammation, COX-1 appears to be expressed constitutively, catalyzing the production of thromboxanes and prostaglandins required for normal physiological processes.  Inhibition of COX-1 by ibuprofen decreases gastric acid secretion and leads to loss of integrity of the gastric mucosa, increasing susceptibility to gastrointestinal erosions, ulcers, and perforations.

In Plain English

Ibuprofen blocks the enzyme responsible for making molecules (prostaglandins) that cause pain sensation, swelling, and fever during injury or illness.

Clinical Considerations

ibuprofen

Figure 1.  Ibuprofen clinical considerations at a glance

Evidence Basis

Ibuprofen in the News

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 21.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.
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