Determination of the Acetylator Phenotype and Pharmacokinetics of Some Sulphonamides in Man

Overview

Journal Clin Pharmacokinet

Specialty Pharmacology

Date 1980 May 1

PMID 7389236

Citations 13

Authors

T B Vree

W J OREILLY

Y A Hekster

J E Damsma

E van der Kleijn

Affiliations

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Abstract

The pharmacokinetics of sulphamethizole, sulphamethoxazole, sulphadiazine, sulphapyridine and sulphadimidine have been studied in man. Renal clearance values of the metabolite N4-acetylsulphonamide are 6 to 20 times higher than those of the corresponding parent compound. The renal clearance of sulphonamides is dependent on the urine flow. N4-Acetylsulphonamide concentration-time profiles for plasma and urine have been constructed for the sulphonamides. The percentage N4-acetylsulphonamide-time profiles for plasma are excellent tools for establishing the acetylator phenotype, while those constructed from urine samples are less useful. Evidence is obtained that sulphadimidine is metabolically processes by 2 different isoenzymes, while sulphadiazine, sulphapyridine and sulphamethoxazole are processes by 1 acetylating isoenzyme. Sulphamethizole is acetylated to very little extent.

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