PMID: 1749708Oct 18, 1991Paper

Pharmacokinetics, N1-glucuronidation and N4-acetylation of sulfamethomidine in humans

Pharmaceutisch Weekblad. Scientific Edition
T B VreeY A Hekster

Abstract

Sulfamethomidine metabolism was studied in 6 volunteers. In humans, only N1-glucuronidation and N4-acetylation take place, leading to the final double conjugate N4-acetylsulfamethomidine N1-glucuronide. The N1-glucuronides were directly measured by high pressure liquid chromatography. Fast and slow acetylators show a similar half-life for sulfamethomidine (26 +/- 6 h) and its conjugates sulfamethomidine (26 +/- 6 h) and N4-acetylsulfamethomidine (36 +/- 16 h). Approximately 50-60% of the oral dose of sulfamethomidine is excreted in the urine, leaving 40-50% for excretion into bile and faeces. The main metabolite of sulfamethomidine is its N1-glucuronide, which accounts for 36 +/- 7% of the dose, followed by N4-acetylsulfamethomidine (16 +/- 8%). N1-glucuronidation results in a 75% decrease in protein binding of sulfamethomidine. N4-acetylsulfamethomidine and its N1-glucuronide showed the same high protein binding of 99%. The renal clearance of N4-acetylsulfamethomidine is 7.9 +/- 2.2 ml/min and approximately 20 times as high as that of the parent drug (0.46 +/- 0.16 ml/min). Total body clearance of sulfamethomidine is 4.5 +/- 0.9 ml/min and the volume of distribution in steady state 10.6 +/- 1.7 1. No measurable plasma concentr...Continue Reading

References

Jan 1, 1991·The Veterinary Quarterly·J F NouwsD Mevius
Apr 27, 1990·Pharmaceutisch Weekblad. Scientific Edition·T B VreeM Shimoda
Jan 1, 1989·Clinical Pharmacokinetics·C A van Ginneken, F G Russel
Apr 1, 1989·Nihon juigaku zasshi. The Japanese journal of veterinary science·T B VreeK Hoji
Sep 1, 1989·Journal of Veterinary Pharmacology and Therapeutics·T B VreeJ F Nouws
Oct 1, 1986·Zentralblatt für Veterinärmedizin. Reihe A·T B VreeJ F Nouws
Sep 1, 1986·Journal of Veterinary Pharmacology and Therapeutics·T B VreeJ F Nouws
Aug 1, 1986·Journal of Pharmaceutical Sciences·P Veng-Pedersen
Oct 1, 1986·Nihon juigaku zasshi. The Japanese journal of veterinary science·Y Takahashi
Feb 1, 1986·Nihon juigaku zasshi. The Japanese journal of veterinary science·Y Takahashi
Jan 1, 1985·European Journal of Clinical Pharmacology·U AbshagenG Neugebauer
Jan 1, 1972·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S R Walker, R T Williams
Oct 1, 1968·The Biochemical Journal·J W BridgesR T Williams
Jan 1, 1969·The Biochemical Journal·J W BridgesR T Williams
Jun 1, 1970·The Biochemical Journal·R H AdamsonR T Williams
Sep 1, 1965·The Biochemical Journal·J W BridgesR T Williams
Sep 1, 1984·Journal of Pharmaceutical Sciences·J W HubbardD Smith
Jan 1, 1963·Toxicology and Applied Pharmacology·F J DICARLOG E PHILLIPS

Citations

Aug 21, 1992·Pharmaceutisch Weekblad. Scientific Edition·F MoolenaarD K Meijer
Oct 16, 1992·Pharmaceutisch Weekblad. Scientific Edition·T B VreeY A Hekster
Oct 1, 1991·The Veterinary Quarterly·T B VreeA Peeters
Nov 1, 1992·The Annals of Pharmacotherapy·T B VreeP G Anderson
Feb 14, 1998·Nature·C Bargmann
Nov 23, 2016·Environmental Science and Pollution Research International·Lu YangPeter Christie

Related Concepts

Sulfamethomidine
Acetylation
Glucuronic Acids
Half-Life
Kidney
Total Body Clearance Rate
Plasma Protein Binding Capacity
Sulfanilamides

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Lipidomics & Rhinovirus Infection

Lipidomics can be used to examine the lipid species involved with pathogenic conditions, such as viral associated inflammation. Discovered the latest research on Lipidomics & Rhinovirus Infection.

Alzheimer's Disease: MS4A

Variants within the membrane-spanning 4-domains subfamily A (MS4A) gene cluster have recently been implicated in Alzheimer's disease in genome-wide association studies. Here is the latest research on Alzheimer's disease and MS4A.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Torsion Dystonia

Torsion dystonia is a movement disorder characterized by loss of control of voluntary movements appearing as sustained muscle contractions and/or abnormal postures. Here is the latest research.

Generating Insulin-Secreting Cells

Reprogramming cells or using induced pluripotent stem cells to generate insulin-secreting cells has significant therapeutic implications for diabetics. Here is the latest research on generation of insulin-secreting cells.

Central Pontine Myelinolysis

Central Pontine Myelinolysis is a neurologic disorder caused most frequently by rapid correction of hyponatremia and is characterized by demyelination that affects the central portion of the base of the pons. Here is the latest research on this disease.

Epigenome Editing

Epigenome editing is the directed modification of epigenetic marks on chromatin at specified loci. This tool has many applications in research as well as in the clinic. Find the latest research on epigenome editing here.