modelTolbutamide
Extends from Pharmacolibrary.Drugs.ATC.A.A10BB03.
Information
| name: | Tolbutamide | |
| ATC code: | A10BB03 | route: | oral |
| compartments: | 1 | |
| dosage: | 500 | mg |
| volume of distribution: | 12.5 | L |
| clearance: | 1.6 | L/h |
| other parameters in model implementation | ||
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 Its clinical use has largely been replaced by newer sulfonylureas and other antidiabetic drugs, though it is still approved in some countries.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
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)