Prostaglandin antagonist

A prostaglandin antagonist is a hormone antagonist acting upon one or more prostaglandins, a subclass of eicosanoid compounds which function as signaling molecules in numerous types of animal tissues.

NSAIDs are perhaps the best-known prostaglandin antagonists; they suppress the signaling function of prostaglandins, which are important mediators of pain, fever, and inflammation responses, by inhibiting the cyclooxygenase enzymes and thereby reducing prostaglandin synthesis. Corticosteroids inhibit phospholipase A2 production by boosting production of lipocortin, an inhibitor protein. Relatively new NSAIDs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of the COX-2 isoform of cyclooxygenase. The development of these drugs allowed the circumvention of the negative gastrointestinal side effects of NSAIDs while still effectively reducing inflammation.

Adverse effects

NSAIDs have been shown to increase the risk of myocardial infarction when taken on a chronic basis for at least 18 months. One emerging hypothesis that may explain these cardiovascular effects is that coxibs create an imbalance in circulating TxA2 (thromboxane A2) and PGI2 (prostacyclin) levels. An increase in the ratio of TxA2/PGI2 could lead to increased platelet aggregation and dysregulation of platelet homeostasis.[1]

The GI and renal systems of patients who are treated with NSAIDS for a long period of time may experience unwanted side effects compared to patients who are treated for shorter durations. Studies on NSAIDS have shown that it can cause acute kidney injury by inhibiting prostaglandin production. The decreased levels of prostaglandins increases the risks of interstitial nephritis since there is lower blood flow to the kidneys. However, the risks of NSAIDs induced kidney failure is higher in people which diabetes or cardiovascular disease.[2]

See also

References
  1. Cheng, Y.; Austin, S. C.; Rocca, B.; Koller, B. H.; Coffman, T. M.; Grosser, T.; Lawson, J. A.; Fitzgerald, G. A. (2002). "Role of prostacyclin in the cardiovascular response to thromboxane A2". Science. 296 (5567): 539–41. Bibcode:2002Sci...296..539C. doi:10.1126/science.1068711. PMID 11964481.
  2. Harirforoosh, Sam; Asghar, Waheed; Jamali, Fakhreddin (2013). "Adverse effects of nonsteroidal antiinflammatory drugs: an update of gastrointestinal, cardiovascular and renal complications". Journal of Pharmacy & Pharmaceutical Sciences. 16 (5): 821–847. doi:10.18433/J3VW2F. ISSN 1482-1826. PMID 24393558.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.