CAFFEINE AS A POTENTIAL INDICATOR FOR ACETYLATOR STATUS

  • 1 February 1987
    • journal article
    • research article
    • Vol. 12  (1) , 47-56
Abstract
The identification of patients as ''fast acetylators'' or ''slow acetylators'' is used in clinical practice to help recognize those at risk from toxicity and in guiding the dosage of N-acetylated drugs. Caffeine has been proposed as a marker for drug acetylation on the basis of a ratio of urinary metabolites (5-acetylamino-6-formylamino-3-methyl uracil and 1-methylxanthine, AFMU:MX) determined by high-performance liquid chromatography. The caffeine test was studied in 26 subjects by reference to the use of sulphamidine as the test substance. The distribution of urinary AFMU:MX ratios allowed assignment of subjects to ''slow'' and ''fast'' acetylator status (AFMU:MX < 2.1 and > 2.3 respectively). The results showed accordance with those from the sulphadimidine test with the exception of one subject. The possible interference of concurrent administration of sulphadimidine (as an example of a drug known to undergo metabolism by N-acetylation) was also studied in 11 of the subjects. The interference was found to be small (apparent mean bias 11%) but of possible clinical significance.

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