Peer-reviewed veterinary case report
How enflicoxib and its metabolites block COX-2 in dog blood
By Solà, Josep et al.·Published in Journal of veterinary pharmacology and therapeutics·2022·Barcelona Science Park, Spain·View original on PubMed →
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Original publication title: Selective inhibition of cyclooxygenase-2 by enflicoxib, its enantiomers and its main metabolites in vitro in canine blood.
- Species:
- dog
Plain-English summary
A study looked at enflicoxib, a medication used for pain and inflammation in dogs with osteoarthritis. Researchers tested how well enflicoxib and its components worked to inhibit certain enzymes (COX-1 and COX-2) that contribute to pain and inflammation. They found that while enflicoxib and one of its forms were effective, the metabolite (a breakdown product) showed the best results in inhibiting COX-2. However, the overall therapeutic effect in dogs may not be significant. This means that while enflicoxib can help, its effectiveness might vary from dog to dog.
People also search for: dog osteoarthritis treatment enflicoxib · canine pain relief medication · COX-2 inhibitors for dogs
Abstract
Enflicoxib is approved for the treatment of pain and inflammation in canine osteoarthritis. The objective of this work was to assess the mechanistic basis of enflicoxib therapy investigating the COX inhibitory activity of enflicoxib (racemate), its enantiomers and its main metabolites using the canine whole blood assay. The (R)-(+)-Enflicoxib enantiomer and metabolite M8 (hydroxylated pyrazoline) did not induce significant COX inhibition. Enflicoxib and its (S)-(-)-Enflicoxib enantiomer inhibited COX-1 and COX-2 with variable degree of preferential isoform inhibition, but no significant therapeutic effect is anticipated in vivo. The pyrazol metabolite showed the highest COX-2 inhibition and was the most selective (ICCOX-1/ COX-2 ratio: 19.45). As the pyrazol metabolite shows saturable binding to red blood cells, its in vivo concentrations in plasma are lower than in whole blood. Accordingly, when applying the red blood cell partitioning, the respective ICand ICfor COX-2 inhibition decreased from 2.8 µM (1129 ng/ml) and 13.4 µM (5404 ng/ml) to 0.2 µM (80.7 ng/ml) and 1.2 µM (484 ng/ml) and the selectivity ratio increased to close to 55. The corrected pyrazol metabolite ICand ICare well within the plasma levels described in treated dogs.
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Search related cases →Original publication on PubMed: https://pubmed.ncbi.nlm.nih.gov/35038171/