Excretion of tolbutamide metabolites in young and old subjects.

Eur J Clin Pharmacol

Department of Pharmaceutics, College of Pharmacy and Pharmacal Sciences, Howard University, Washington, D.C. 20059.

Published: September 1990

Tolbutamide (1 g/70 kg) was administered as a single intravenous dose to 31 healthy, non-smoking, drug-free males between 23 and 87 years old and the total amounts of hydroxy and carboxytolbutamide excreted in 24 h were measured. There was a significant decrease in the urinary recovery of both metabolites with age. The reason for these findings is not known at the present time and may be associated with the decrease in creatinine clearance observed in these subjects or other changes in the pharmacokinetics of tolbutamide which are currently being investigated.

Download full-text PDF

Source
http://dx.doi.org/10.1007/BF02336696DOI Listing

Publication Analysis

Top Keywords

excretion tolbutamide
4
tolbutamide metabolites
4
metabolites young
4
young subjects
4
subjects tolbutamide
4
tolbutamide g/70
4
g/70 administered
4
administered single
4
single intravenous
4
intravenous dose
4

Similar Publications

As the prevalence of diabetes rises, the use of antidiabetic drugs becomes more frequent. Thus, focusing on the effects of these drugs on water-sodium balance and electrolyte regulation is necessary. This review discusses the effects and the mechanisms behind them.

View Article and Find Full Text PDF

Evaluation of Drug-Drug Interaction Potential of Enarodustat (JTZ-951) Using a Cytochrome P450 Probe Cocktail.

Clin Pharmacol Drug Dev

July 2023

Drug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Division, Japan Tobacco Inc., Osaka, Japan.

The drug interaction potential of enarodustat (doses: 25, 50 mg) on the activity of cytochrome P450 (CYP) 1A2, 2C9, 2C19, 2D6, and 3A4 was evaluated after once-daily administration for 15 days in a phase 1 multiple-ascending-dose study in healthy subjects. Probe substrates specific for the enzymes, i.e.

View Article and Find Full Text PDF

Pharmacokinetic characterization plays a vital role in drug discovery and development. Although involving numerous laboratory animals with error-prone, labor-intensive, and time-consuming procedures, pharmacokinetic profiling is still irreplaceable in preclinical studies. With physiologically based pharmacokinetic (PBPK) modeling, the profiles of drug absorption, distribution, metabolism, and excretion can be predicted.

View Article and Find Full Text PDF

Tolbutamide is an oral anti-hyperglycaemic agent used to treat non-insulin-dependent diabetes mellitus with species-dependent metabolic profiles. In this study, we investigated tolbutamide metabolism in chimeric TK-NOG mice transplanted with human hepatocytes (humanised-liver mice).Substantial 4-hydroxytolbutamide and 4-carboxytolbutamide production was observed in hepatocytes from humanised-liver mice (Hu-Liver cells) and humans, whereas 4-carboxytolbutamide production was not detected in mouse hepatocytes.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!