PMID: 11604271Oct 18, 2001Paper

Kinetic phenotypic diagnosis of N-acetylation polymorphism in patients based on ratio of urinary metabolites of salicylazosulfapyridine

International Journal of Pharmaceutics
K YokogawaK Miyamoto

Abstract

We found that N-acetylation polymorphism can be evaluated from the disposition kinetics of sulfapyridine (SP) and 5-aminosalicylic acid (5-ASA) and their acetylated metabolites generated by N-acetyltransferase (NAT2) after oral administration of salicylazosulfapyridine (SASP). In 126 Japanese subjects, the homozygote of NAT2*4 was the most frequent (40%), followed by heterozygotes of NAT2*4 and mutant genes (28% NAT2*4/*6A, 15% NAT2*4/*7B, and 2% NAT2*4/*5B). Combinations of mutant genes accounted for 16%. When the relationship between the molar ratio of N-acetyl-SP (Ac-SP)/SP or N-acetyl-5-ASA(Ac-5-ASA)/5-ASA in serum and five genotypes of polymorphic NAT2* was examined in patients who received multiple doses of SASP, the molar ratios of Ac-SP/SP, rather than Ac-5-ASA/5-ASA tended to decrease according to the classification of genotype. We calculated the pharmacokinetic parameters in healthy subjects with various genotypes of polymorphic NAT2* after a single p.o. administration of SASP, according to a model of the SP metabolic pathways. The molar ratios of Ac-SP/SP in serum and urine were simulated using these parameters, and the molar ratio of Ac-SP/SP in urine at 4 days after the first administration could be categorized int...Continue Reading

References

Dec 1, 1977·Clinical Pharmacology and Therapeutics·T R BatesH J Pieniaszek
Aug 1, 1986·Annals of Internal Medicine·N H ShearW Kalow
Jul 1, 1972·Clinical Pharmacology and Therapeutics·H Schröder, D E Campbell
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Nov 1, 1981·Journal of Pharmacobio-dynamics·K YamaokaT Uno
May 1, 1997·Clinical Pharmacology and Therapeutics·K OkumuraY Tanigawara

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Citations

Jun 8, 2002·Pharmacogenomics·Peter Meisel

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