modelXimelagatran
Extends from Pharmacolibrary.Drugs.ATC.B.B01AE05.
Information
| name: | Ximelagatran | |
| ATC code: | B01AE05 | route: | oral |
| compartments: | 1 | |
| dosage: | 36 | mg |
| volume of distribution: | 18 | L |
| clearance: | 3.6 | L/hr |
| other parameters in model implementation | ||
Ximelagatran is an oral direct thrombin inhibitor anticoagulant, formerly used for prevention of stroke and venous thromboembolism, as well as for the treatment of deep vein thrombosis. It was withdrawn from the market due to hepatotoxicity concerns and thus is not approved or used today.
Pharmacokinetics
Pharmacokinetic parameters from healthy adult volunteers (both sexes) under fasting conditions after oral administration.
References
Eriksson, UG, et al., & Eriksson, BI (2003). Pharmacokinetics of melagatran and the effect on ex vivo coagulation time in orthopaedic surgery patients receiving subcutaneous melagatran and oral ximelagatran: a population model analysis. Clinical pharmacokinetics 42(7) 687–701. DOI:10.2165/00003088-200342070-00006 PUBMED:https://pubmed.ncbi.nlm.nih.gov/12844328
Bååthe, S, et al., & Eriksson, UG (2006). Population pharmacokinetics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in atrial fibrillation patients receiving long-term anticoagulation therapy. Clinical pharmacokinetics 45(8) 803–819. DOI:10.2165/00003088-200645080-00004 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16884319
Wolzt, M, et al., & Eriksson, UG (2005). Pharmacokinetics and pharmacodynamics of ximelagatran. Seminars in vascular medicine 5(3) 245–253. DOI:10.1055/s-2005-916163 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16123911
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)