AUTORADIOGRAPHIC AND BIOCHEMICAL OBSERVATIONS ON THE DISTRIBUTION OF NON-STEROID ANTI-INFLAMMATORY DRUGS

  • 1 January 1981
    • journal article
    • research article
    • Vol. 250  (2) , 180-194
Abstract
A comparison was made of the distribution of some new [R 803 [.alpha.-methyl-3-phenyl-7-benzofuranacetic acid], diflunisal, chlorosalicylic acid meseclazone, sulindac, benzoxaprofen and fenclofenac] radioactively-labeled non-steroid anti-inflammatory (NSAI) drugs or pro-drugs with their respective progenitors and/or standard acidic NSAI drugs (i.e., aspirin, indomethacin and phenylbutazone), using whole body autoradiography and scintillation counting in rats. Whether the distribution of the new NSAI drugs may contribute to changes in their side, or therapeutic effects compared with the older drugs was studied. All the NSAI drugs accumulated in those tissues wherein the principal therapeutic and side-effects are manifest. The accumulation in inflamed tissues occurs regardless of the structural type of NSAI drugs, i.e., with specific accumulation occurring in this tissue of the acidic drugs or their acidic metabolites. New aspects of the distribution of the acetyl moiety of aspirin are reported which may be significant in relation to the side effects induced by this drug.

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