.Pharmacolibrary.Drugs.ATC.A.A10BB03

Information

Tolbutamide is a first-generation sulfonylurea oral hypoglycemic agent, used to treat type 2 diabetes mellitus. It stimulates insulin secretion from the pancreas. Its clinical use has largely been replaced by newer sulfonylureas and other antidiabetic drugs, though it is still approved in some countries.

Pharmacokinetics

Pharmacokinetic parameters reported in healthy adult volunteers after single oral dose administration.

References

1. Kirchheiner, J, et al., & Brockmöller, J (2005). Effect of genetic polymorphisms in cytochrome p450 (CYP) 2C9 and CYP2C8 on the pharmacokinetics of oral antidiabetic drugs: clinical relevance. Clinical pharmacokinetics 44(12) 1209–1225. DOI:10.2165/00003088-200544120-00002 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16372821

2. Xu, H, et al., & McLachlan, AJ (2009). Influence of genetic polymorphisms on the pharmacokinetics and pharmaco-dynamics of sulfonylurea drugs. Current drug metabolism 10(6) 643–658. DOI:10.2174/138920009789375388 PUBMED:https://pubmed.ncbi.nlm.nih.gov/19799532

3. Heinrich, N, et al., & Hoelscher, M (2025). Safety, bactericidal activity, and pharmacokinetics of the antituberculosis drug candidate BTZ-043 in South Africa (PanACEA-BTZ-043-02): an open-label, dose-expansion, randomised, controlled, phase 1b/2a trial. The Lancet. Microbe 6(2) 100952–None. DOI:10.1016/j.lanmic.2024.07.015 PUBMED:https://pubmed.ncbi.nlm.nih.gov/39793592

Revisions

• 06/2025 initial generated model