Comparative pharmacokinetics of caffeine and its primary demethylated metabolites paraxanthine, theobromine and theophylline in man.

A. Lelo, DJ Birkett, RA Robson, JO Miners

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    Abstract

    The pharmacokinetics of caffeine (CA), paraxanthine (PX), theobromine (TB) and theophylline (TP) were studied in six healthy male volunteers after oral administration of each compound on separate occasions. The total plasma clearances of CA and PX were similar in value (2.07 and 2.20 ml min‐1 kg‐1, respectively) as were those for TP and TB (0.93 and 1.20 ml min‐1 kg‐1, respectively). The unbound plasma clearances of CA and PX were also similar in magnitude (3.11 and 4.14 ml min‐1 kg‐1, respectively) as were those of TP and TB (1.61 and 1.39 ml min‐1 kg‐1, respectively). The half‐lives of TP and TB (6.2 and 7.2 h, respectively) were significantly longer than those of CA and PX (4.1 and 3.1 h, respectively). The volume of distribution at steady state of TP (0.44 l kg‐1) was lower than that of the other methylxanthines (0.63‐ 0.72 l kg‐1). The unbound volume of distribution of TP (0.77 l kg‐1) was however the same as that of TB (0.79 l kg‐1) whereas the unbound volume of distribution of PX (1.18 l kg‐1) was similar to that of CA (1.06 l kg‐1). 1986 The British Pharmacological Society

    Original languageEnglish
    Pages (from-to)177-182
    Number of pages6
    JournalBritish Journal of Clinical Pharmacology
    Volume22
    Issue number2
    DOIs
    Publication statusPublished - Aug 1986

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