modelSitagliptin
Extends from Pharmacolibrary.Drugs.ATC.A.A10BH01.
Information
| name: | Sitagliptin | |
| ATC code: | A10BH01 | route: | oral |
| compartments: | 1 | |
| dosage: | 100 | mg |
| volume of distribution: | 198 | L |
| clearance: | 15.7 | L/hr |
| other parameters in model implementation | ||
Sitagliptin is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor used to improve glycemic control in adults with type 2 diabetes mellitus. It is usually administered orally as a once-daily tablet, often in combination with other antidiabetic drugs. Sitagliptin is approved and widely used today in clinical practice.
Pharmacokinetics
Pharmacokinetic parameters reported for healthy adult subjects after a single oral dose of sitagliptin 100 mg tablet.
References
Herman, GA, et al., & Wagner, JA (2006). Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes. The Journal of clinical endocrinology and metabolism 91(11) 4612–4619. DOI:10.1210/jc.2006-1009 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16912128
Zhou, C, et al., & Shao, F (2024). Safety, tolerability, pharmacokinetics and pharmacokinetic-pharmacodynamic modeling of cetagliptin in patients with type 2 diabetes mellitus. Frontiers in endocrinology 15 1359407–None. DOI:10.3389/fendo.2024.1359407 PUBMED:https://pubmed.ncbi.nlm.nih.gov/38529396
Chen, X, et al., & Hu, P (2016). An open-label, multiple-dose study to assess the pharmacokinetics and tolerability of sitagliptin/metformin fixed-dose combination (FDC) tablet in healthy Chinese adult subjects. International journal of clinical pharmacology and therapeutics 54(9) 705–711. DOI:10.5414/CP202646 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27390052
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)