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- W2068165078 abstract "Amethocaine, a local anaesthetic of the ester class, produces effective percutaneous anaesthesia of the skin when applied as a novel preparation. The metabolism of the drug by cutaneous esterases was investigated using enzymatic extracts of porcine and human whole skin, and of human epidermis. Analysis of the incubation mixture indicated the production of p-(butyl)aminobenzoic acid, confirming that metabolism of the substrate occurred via cleavage of the ester side chain. In all cases, the rate of metabolic transformation was slow, requiring about 24 h for a 50% reduction in substrate concentration. There was evidence that amethocaine, but not its metabolite, was bound to proteinaceous components of the cutaneous extracts. Given the prolonged in vivo anaesthetic activity of amethocaine percutaneous anaesthetic preparations, the ability of the skin to metabolise the drug is likely to be of significance in determining the duration of anaesthetic activity but is too slow to influence speed of onset of the anaesthetic effect. The lack of systemic toxicity with percutaneous amethocaine may be explained by a combination of slow drug release from the stratum corneum and metabolism by cutaneous esterases." @default.
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- W2068165078 date "1990-07-01" @default.
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- W2068165078 title "The metabolism of amethocaine by porcine and human skin extracts: influence on percutaneous anaesthesia" @default.
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- W2068165078 doi "https://doi.org/10.1016/0378-5173(90)90025-y" @default.
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