.Pharmacolibrary.Drugs.V_Various.V04C_OtherDiagnosticAgents.V04CA01_Tolbutamide.Tolbutamide

Information

name:Tolbutamide
ATC code:V04CA01
route:oral
n-compartments1

Tolbutamide is a first-generation sulfonylurea oral hypoglycemic agent, once widely used for the treatment of type 2 diabetes mellitus. It acts by stimulating insulin release from pancreatic beta cells. Although tolbutamide has largely been replaced by second-generation sulfonylureas and other agents, it may still be seen in certain contexts or older studies.

Pharmacokinetics

Pharmacokinetic parameters reported for healthy adult subjects following a single oral dose.

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


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