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Literature DB >> 7389236

Determination of the acetylator phenotype and pharmacokinetics of some sulphonamides in man.

T B Vree, W J O'Reilly, Y A Hekster, J E Damsma, E van der Kleijn.

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.

Entities: Chemical Species

Mesh：

Substances：
Sulfonamides

Year: 1980 PMID： 7389236 DOI： 10.2165/00003088-198005030-00006

Source DB: PubMed Journal: Clin Pharmacokinet ISSN： 0312-5963 Impact factor: 6.447

48 in total

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Journal: Clin Pharmacokinet Date: 1979 Jul-Aug Impact factor: 6.447

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12 in total

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Authors: M E Sharp; S M Wallace; K W Hindmarsh; M A Brown
Journal: Eur J Clin Pharmacol Date: 1981 Impact factor: 2.953

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Authors: M Hildebrand; W Seifert
Journal: Eur J Clin Pharmacol Date: 1989 Impact factor: 2.953

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Authors: C Astbury; C Beyeler; H A Bird
Journal: Rheumatol Int Date: 1995 Impact factor: 2.631

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Authors: A E Pontiroli; A Calderara; L Bonisolli; P Maffi; A De Pasqua; A Margonato; G Radaelli; G Gallus; G Pozza
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Authors: A J van der Ven; M A Mantel; T B Vree; P P Koopmans; J W van der Meer
Journal: Br J Clin Pharmacol Date: 1994-08 Impact factor: 4.335

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Authors: T B Vree; Y A Hekster; J E Damsma; M Tijhuis; W T Friesen
Journal: Eur J Clin Pharmacol Date: 1981 Impact factor: 2.953