modelTolbutamide
Extends from Pharmacolibrary.Drugs.ATC.V.V04CA01.
Information
| name: | Tolbutamide | |
| ATC code: | V04CA01 | route: | oral |
| compartments: | 1 | |
| dosage: | 500 | mg |
| volume of distribution: | 11 | L |
| clearance: | 100 | mL/min |
| other parameters in model implementation | ||
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 Although tolbutamide has largely been replaced by second-generation sulfonylureas and other agents, it may still be seen in certain contexts or older studies.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
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
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
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
Parameters
| Type | Name | Default | Description |
|---|---|---|---|
| Modelica.Units.SI.Mass | weight (from PK_1C) | 75 | patient weight (kg) |
| Modelica.Units.SI.SpecificVolume | VdPerKg (from PK_1C) | 0.9 | Volume of distribution (L/kg) |
| Modelica.Units.SI.MassFraction | F (from PK_1C) | 0.8 | bioavailiability (0-1) |
| Pharmacolibrary.Types.Clearance | Cl (from PK_1C) | 20 | clearance |
| Modelica.Units.SI.Time | adminTime (from PK_1C) | 60 | first administration time (s) |
| Modelica.Units.SI.Time | adminDuration (from PK_1C) | 600 | administration duration (s) |
| Modelica.Units.SI.Time | adminPeriod (from PK_1C) | 8*60*60 | period of administration (default 8 hours)(s) |
| Pharmacolibrary.Types.Mass | adminMass (from PK_1C) | 1000 | administration mass (mg) |
| Integer | adminCount (from PK_1C) | 8 | number of dose administered (1) |
| Pharmacolibrary.Types.Volume | Vd (from PK_1C) | VdPerKg*weight | Volume of distribution (m3) |
| Pharmacolibrary.Types.MassConcentration | Cmin (from PK_1C) | 0.004 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Cmax (from PK_1C) | 0.008 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Ctox_peak (from PK_1C) | 0.012 | toxicity peak level |
| Pharmacolibrary.Types.MassConcentration | Ctox_trough (from PK_1C) | 0.006 | toxicity trough level |
| Pharmacolibrary.Types.TransferRate | ka (from PK_1C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_1C_enteral) | 600 | delay between oral administration and absorption (default 10min) |
Connectors
| Type | Name | Default | Description |
|---|---|---|---|
| Types.ConcentrationOutput | C_central (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | centralCPort (from PK_1C) |
Components
| Type | Name | Default | Description |
|---|---|---|---|
| Pharmacokinetic.NoPerfusedTissueCompartment | central (from PK_1C) | ||
| Pharmacokinetic.ClearanceDrivenElimination | elim (from PK_1C) | ||
| Sources.PeriodicDose | periodicDose (from PK_1C) | ||
| Modelica.Units.SI.Time | t1_2 (from PK_1C) | elimination half-life |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)