| Defining the COX inhibitor selectivity of NSAIDs: implications for understanding toxicity. | |
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MedLine Citation:
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PMID: 22111779 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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The hypothesis that the anti-inflammatory activity of NSAIDs derives from COX inhibition is well established. It also underpins the accepted mechanism of the gastrointestinal and renal toxicity of NSAIDs. However, in terms of NSAID-induced cardiovascular toxicity, is COX inhibition then guilty by association? Multiple experimental models of COX-1/COX-2 inhibition have enabled ranking of the relative inhibitory activity of NSAIDs. Inhibition is expressed as an IC(50) value and the index of COX selectivity as the ratio of the IC(50) value for COX-2 and COX-1. These data informed the 'imbalance hypothesis' that the cardiovascular risk of NSAIDs results from an imbalance in the detrimental actions of COX-1-derived thromboxane A(2) and the beneficial actions of COX-2-derived prostacyclin (PGI(2)). Data derived from in vitro models used to generate NSAID IC(50) values are discussed in the context of the difficulties in defining COX selectivity and hence understanding the toxicity of NSAIDs in current clinical use. |
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Authors:
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Kathleen M Knights; Arduino A Mangoni; John O Miners |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Expert review of clinical pharmacology Volume: 3 ISSN: 1751-2441 ISO Abbreviation: Expert Rev Clin Pharmacol Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2011-11-24 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101278296 Medline TA: Expert Rev Clin Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 769-76 Citation Subset: IM |
Affiliation:
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Department of Clinical Pharmacology, Flinders University, Bedford Park, Adelaide, 5042 Australia. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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