Title : Aceclofenac spares cyclooxygenase 1 as a result of limited but sustained biotransformation to diclofenac.

Pub. Date : 2003 Sep

PMID : 12966366






3 Functional Relationships(s)
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1 Maximal plasma concentrations of diclofenac after oral administration of aceclofenac (0.39 micromol/L) or diclofenac (1.28 micromol/L) were sufficient for a greater than 97% inhibition of COX-2 (50% inhibitory concentration, 0.024 micromol/L) and a 46% (aceclofenac treatment) or 82% inhibition (diclofenac treatment) of COX-1 (50% inhibitory concentration, 0.43 micromol/L). aceclofenac mitochondrially encoded cytochrome c oxidase II Homo sapiens
2 Although 100 mg aceclofenac yielded diclofenac concentrations substantially lower than 75 mg diclofenac, these were sufficient for a sustained block of COX-2 but caused a minor and shorter inhibition of COX-1 than 75 mg diclofenac. aceclofenac mitochondrially encoded cytochrome c oxidase II Homo sapiens
3 In conclusion, both COX-1-sparing and COX-2-inhibitory actions of aceclofenac may rest in its limited but sustained biotransformation to diclofenac. aceclofenac mitochondrially encoded cytochrome c oxidase II Homo sapiens