Secondary metabolism of theophylline biotransformation products in man‐ route of formation of 1‐methyluric acid.

DJ Birkett, JO Miners, J. Attwood

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    53 Citations (Scopus)

    Abstract

    The route of formation of 1‐methyluric acid (1MU) from theophylline has been investigated by i.v. administration of 1‐methylxanthine (1MX) before and after allopurinol treatment and of 1,3‐dimethyluric acid (1,3DMU) to healthy male volunteers. 1,3DMU was recovered unchanged in urine and was not demethylated to 1MU. By contrast after administration of 1MX the major part of the dose was recovered as 1MU. After allopurinol this was reversed with most of the 1MX dose being excreted unchanged and only a minor amount as 1MU. The results show that 1MU derived from theophylline is formed by an initial 3‐demethylation to 1MX and then a rapid xanthine oxidase mediated 8‐oxidation. No 1MU is formed by 3‐demethylation of 1,3DMU. 1983 The British Pharmacological Society

    Original languageEnglish
    Pages (from-to)117-119
    Number of pages3
    JournalBritish Journal of Clinical Pharmacology
    Volume15
    Issue number1
    DOIs
    Publication statusPublished - Jan 1983

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