A synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic, and antipyretic activities. Ketorolac non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2. The inhibition of COX-2, up-regulated at sites of inflammation, prevents conversion of arachidonic acid to pro-inflammatory prostaglandins. The inhibition of COX-1 by this agent prevents the normal steady-state production of prostaglandins that play housekeeping roles in the protection of the gastrointestinal tract, the regulation of renal blood flow, and platelet aggregation. As a result, the inhibition of COX-1 may be associated with gastrointestinal toxicity, nephrotoxicity, and the inhibition of platelet aggregation.
Definition (MSH)
A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)
Definition (PDQ)
A synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. Ketorolac, a non-selective inhibitor of the cyclo-oxygenase (COX) enzyme, prevents the synthesis of prostaglandins and thromboxanes from arachidonic acid. COX enzymes exist in two isoforms; inhibition of the COX-2 enzyme produces the anti-inflammatory and analgesic whereas, inhibition of the COX-1 enzyme is associated with gastrointestinal side effects, nephrotoxicity and platelet de-aggregatory effects. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40569&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40569&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1219" NCI Thesaurus)
Concepts
Organic Chemical (T109)
, Pharmacologic Substance (T121)