In vitro enantioselective pharmacodynamics of Carprofen and Flunixin‐meglumine in feedlot cattle. Issue 1 (25th April 2013)

• Record Type: Journal Article
• Authors: Miciletta, M.; Cuniberti, B.; Barbero, R.; Re, G.
• Is Part Of: Journal of veterinary pharmacology and therapeutics. Volume 37:Issue 1(2014)
• Page Start: 43
• Page End: 52
• Publication Date: 2013-04-25
• Subjects: Veterinary pharmacology -- Periodicals; Therapeutics -- Periodicals; 636.0895105
• DOI: 10.1111/jvp.12052
• Languages: English
• ISSNs: 0140-7783

Abstract

<abstract abstract-type="main" xml:lang="en" id="jvp12052-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>The activity of the anti‐inflammatory agents Flunixin‐meglumine (FLU), RS (±) Carprofen (CPF) and S (+) CPF on bovine cyclooxygenases (COXs) has been characterized in feedlot calves using an <italic>in vitro</italic> whole blood model. The drugs showed equivalent efficacy in their inhibitory activity on COXs, and the rank order of potency for both COX‐1 and COX‐2 inhibition was FLU &gt; S (+) CPF &gt; RS (±) CPF. Our results indicated that FLU is a nonselective inhibitor of bovine COXs, whereas RS (±) CPF and S (+) CPF exhibited different degrees of preferential inhibition of COX‐2 isoenzyme. The rank order of IC₅₀ COX‐1: IC₅₀ COX‐2 potency ratios was in fact S (+) CPF (51.882) &gt; RS (±) CPF (13.964) &gt; FLU (0.606), and the calculated percentage inhibition of COX‐1 corresponding to COX‐2 inhibition values comprised between 80% and 95% was comprised between 57.697 and 79.865 for FLU, 33.373 and 51.319 for RS (±) CPF, and 0.230 and 4.622 for S (+) CPF, respectively. These findings are discussed in relation to the prediction of the clinical relevance of COX inhibition by the test drugs in cattle.</p> </abstract>