Literature DB >> 487686

Pharmacokinetics of N1-acetyl- and N4-acetylsulphamethoxazole in man.

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

Abstract

The pharmacokinetics of N1-acetylsulphamethoxazole and N4-acetylsulphamethoxazole in man are described. N1-Acetylsulphamethoxazole is deacetylated to sulphamethoxazole and acetylated to N4-acetylsulphamethoxazole. N4-Acetylsulphamethoxazole is excreted almost unchanged in the urine. The renal excretion rate is independent of the urine flow and urinary pH. N4-Acetylsulphonamides are less lipid soluble and more acidic than their corresponding parent sulphonamides.

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Year:  1979        PMID： 487686     DOI： 10.2165/00003088-197904040-00004

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


  15 in total

1.  ABSORPTION AND EXCRETION OF DRUGS. XX. SOME PHARMACOKINETIC ASPECTS OF ABSORPTION AND EXCRETION OF SULFONAMIDES. (2). ABSORPTION FROM RAT SMALL INTESTINE.

Authors:  T KOIZUMI; T ARITA; K KAKEMI
Journal:  Chem Pharm Bull (Tokyo)       Date:  1964-04       Impact factor: 1.645

2.  Pharmacokinetic analysis of renal handling of sulfamethizole.

Authors:  R Hori; K Sunayashiki; A Kamiya
Journal:  J Pharm Sci       Date:  1976-03       Impact factor: 3.534

3.  The simultaneous quantitative determination of total, 'active', acetylated and conjugated sulfonamide in biological fluids.

Authors:  J Rieder
Journal:  Chemotherapy       Date:  1976       Impact factor: 2.544

4.  Some physico-chemical properties of amphetamine and related drugs.

Authors:  T B Vree; A T Muskens; J M van Rossum
Journal:  J Pharm Pharmacol       Date:  1969-11       Impact factor: 3.765

5.  The polymorphic acetylation of sulphapyridine in man.

Authors:  H Schröder; D A Evans
Journal:  J Med Genet       Date:  1972-06       Impact factor: 6.318

6.  Determination of plasma and renal clearance of cefuroxime and its pharmacokinetics in renal insufficiency.

Authors:  R van Dalen; T B Vree; J C Hafkenscheid; J S Gimbrère
Journal:  J Antimicrob Chemother       Date:  1979-05       Impact factor: 5.790

7.  Quantitative determination of the bacteriostatically active fraction of sulfonamides and the sum of their inactive metabolites in the body fluids.

Authors:  J Rieder
Journal:  Chemotherapy       Date:  1972       Impact factor: 2.544

8.  Determination of procainamide acetylator status.

Authors:  J J Lima; W J Jusko
Journal:  Clin Pharmacol Ther       Date:  1978-01       Impact factor: 6.875

9.  Determination of trimethoprim and sulfamethoxazole (co-trimoxazole) in body fluids of man by means of high-performance liquid chromatography.

Authors:  T B Vree; Y A Hekster; A M Baars; J E Damsma; E V Kleijin
Journal:  J Chromatogr       Date:  1978-07-01

10.  Sulphadimidine acetylation test for classification of patients as slow or rapid inactivators of isoniazid.

Authors:  K V Rao; D A Mitchison; N G Nair; K Prema; S P Tripathy
Journal:  Br Med J       Date:  1970-08-29
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  9 in total

1.  Clinical pharmacokinetics of co-trimoxazole (trimethoprim-sulphamethoxazole).

Authors:  R B Patel; P G Welling
Journal:  Clin Pharmacokinet       Date:  1980 Sep-Oct       Impact factor: 6.447

2.  Effects of methoxy groups in the NI-substituent of sulfonamides on the pathways of elimination in man. The acetylation-deacetylation equilibrium and mechanisms of renal excretion of sulfisomidine, sulfamethomidine and sulfadimethoxine.

Authors:  T B Vree; Y A Hekster; M W Tijhuis; M Baakman; M J Oosterbaan; E F Termond
Journal:  Pharm Weekbl Sci       Date:  1984-08-24

3.  Isolation and identification of 4-hydroxysulfamerazine and preliminary studies on its pharmacokinetics in dogs.

Authors:  T B Vree; M W Tijhuis; J F Nouws; Y A Hekster
Journal:  Pharm Weekbl Sci       Date:  1984-04-27

4.  Distribution of trimethoprim and sulphamethoxazole in blood during treatment with co-trimoxazole.

Authors:  A Nowak; A Klimowicz; M Kadyków
Journal:  Eur J Clin Pharmacol       Date:  1985       Impact factor: 2.953

5.  The effect of the molecular structure of closely related N1-substituents of sulfonamides on the pathways of elimination in man. The acetylation-deacetylation equilibrium and renal clearance related to the structure of sulfadiazine, sulfamerazine and sulfadimidine.

Authors:  T B Vree; Y A Hekster; M W Tijhuis; M Baakman; T J Janssen; E F Termond
Journal:  Pharm Weekbl Sci       Date:  1983-04-29

6.  Pharmacokinetics of cefradine, sulfamethoxazole and trimethoprim and their metabolites in a patient with peritonitis undergoing continuous ambulatory peritoneal dialysis.

Authors:  M Martea; Y A Hekster; T B Vree; A J Voets; J H Berden
Journal:  Pharm Weekbl Sci       Date:  1987-04-24

7.  Deterioration of kidney function by high doses of co-trimoxazole in man.

Authors:  T B Vree; M Martea; Y A Hekster; E F Termond; R Van Klaveren; J W Lammers; J H Berden
Journal:  Pharm Weekbl Sci       Date:  1987-04-24

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

Authors:  T B Vree; W J O'Reilly; Y A Hekster; J E Damsma; E van der Kleijn
Journal:  Clin Pharmacokinet       Date:  1980 May-Jun       Impact factor: 6.447

9.  Pharmacokinetics and mechanism of renal excretion of short acting sulphonamides and N4-acetylsulphonamide derivatives in man. Structural requirements of sulphonamides for active tubular secretion.

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
  9 in total

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