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Modulation of Thiopurine Metabolism in Native Human Erythrocytes

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The Use of Resealed Erythrocytes as Carriers and Bioreactors

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 326))

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Abstract

Thiopurines are widely used in therapeutic protocols as antineoplastic or immunosuppressive agents.1 The half-life of these drugs in plasma is relatively short due to the rapid metabolic degradation. There are two major pathways in this process. The first involves methylation of the sulfhydryl group and subsequent oxidation of the methylated derivatives. The second pathway requires the enzyme xanthine oxidase, which is present in relatively large amounts in liver and oxidizes thiopurines to thiouric acid, a noncytostatic metabolite. Xanthine-oxidase inhibition by allopurinol greatly prevents metabolic inactivation of thiopurines but it increases toxicity as well, and there is no apparent improvement in the therapeutic index.

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© 1992 Springer Science+Business Media New York

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Salerno, C., Lucano, A., Crifò, C. (1992). Modulation of Thiopurine Metabolism in Native Human Erythrocytes. In: Magnani, M., DeLoach, J.R. (eds) The Use of Resealed Erythrocytes as Carriers and Bioreactors. Advances in Experimental Medicine and Biology, vol 326. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3030-5_29

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  • DOI: https://doi.org/10.1007/978-1-4615-3030-5_29

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-6321-7

  • Online ISBN: 978-1-4615-3030-5

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