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Detection of human intestinal bacterial overgrowth by sulfasalazine

, : Detection of human intestinal bacterial overgrowth by sulfasalazine. Journal of Clinical Pharmacology 18(11-12): 549-555

Bacterial overgrowth in some areas along the upper gastrointestinal tract in man can be detected by measuring the rate of appearance of sulfapyridine in the urine after an oral dose of sulfasalazine, a drug which is biotransformed to sulfapyridine and 5-aminosalicyclic acid only by intestinal bacteria. When a single 2.0 g oral dose of sulfasalazine was given to 4 normal subjects and 2 patients having jejunal diverticulum, the ratio of sulfapyridine excreted in the urine in the 1st 24 h to that in the 2nd 24 h averaged 0.36 (range 0.2-0.42) in normals and 5.3 in patients having the blind loop. This difference in the patterns of sulfapyridine excretion was not due to difference in acetylator phenotype since each of the subjects studied (4 normal volunteers and 2 blind-loop patients) was a rapid acetylator (63.3-69.0% acetylation of sulfapyridine). A similar difference was also observed in the blood concentration-time profile of sulfapyridine in a male blind-loop patient who gave consent to the studies. When he received a single oral dose of 2.0 g sulfasalazine before the operation, the peak plasma level of sulfapyridine was reached within 7-12 h, whereas 6 mo. after the operation, i.e., when he became normal, the peak plasma sulfapyridine concentration was reached within 12-24 h. The pattern of blood sulfapyridine concentration-time profile in this blind-loop patient after the operation was the same as in normal subjects. The presence of jejunal diverticulum is associated with significant alteration in the kinetics of urinary excretion of bacterial-dependent metabolites of sulfasalazine. This change can serve as the basis for a new method of detecting overgrowth of intestinal bacteria in man.


PMID: 31370

DOI: 10.1002/j.1552-4604.1978.tb01584.x

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