PMID: 6483571Aug 24, 1984Paper

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

Pharmaceutisch Weekblad. Scientific Edition
T B VreeE F Termond

Abstract

Sulfisomidine, sulfamethomidine, sulfadimethoxine and their corresponding N4-acetyl derivatives were administered to man. The percentages of acetylation and deacetylation and those of protein binding, the half-lives of elimination and the apparent and true renal clearance values were measured. No acetylation phenotype could be demonstrated in these compounds. Methoxy substitution in the NI-pyrimidine group of sulfisomidine affects predominantly the renal clearance value and mechanism of the parent compound but has no influence on the renal clearance of the N4-acetyl derivatives. The renal clearance value of sulfisomidine is 232 +/- 33 ml/min, of sulfamethomidine 21.60 +/- 16.4 ml/min and of sulfadimethoxine 10.87 +/- 10.44 ml/min. The renal clearance values of the corresponding N4-acetylsulfonamide derivatives are 314 +/- 91 ml/min, 342 +/- 63 ml/min and 202 +/- 65 ml/min respectively. Tubular reabsorption, caused by methoxy substitution in the NI-pyrimidine ring, lowers the rate of elimination and increases the half-life. The half-life of sulfisomidine is 8.5 +/- 0.5 h, of sulfamethomidine 27.8 +/- 5.3 h and of sufadimethoxine 34.6 +/- 10.4 h.

References

Nov 15, 1975·Life Sciences·P Nielsen, F Rasmussen
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Citations

Apr 27, 1990·Pharmaceutisch Weekblad. Scientific Edition·T B VreeM Shimoda
Oct 18, 1991·Pharmaceutisch Weekblad. Scientific Edition·T B VreeY A Hekster
Sep 1, 1989·Journal of Veterinary Pharmacology and Therapeutics·T B VreeJ F Nouws
May 1, 1993·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·S RatnaK S Pang
Jan 1, 1992·Biopharmaceutics & Drug Disposition·T B VreeT Miura

Related Concepts

Sulfamethomidine
Acetylation
Dealkylation
Half-Life
Kidney
Structure-Activity Relationship
Deposul
Sulfanilamides
Sulfisomidine Sodium
Sulfonamides

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