modelC02KX02
Extends from Pharmacokinetic.Models.PK_1C_enteral.
Information
| name: | Ambrisentan | |
| ATC code: | C02KX02 | route: | oral |
| compartments: | 1 | |
| dosage: | 10 | mg |
| volume of distribution: | 19 | L |
| clearance: | 3.4 | L/h |
| other parameters in model implementation | ||
Ambrisentan is an endothelin receptor antagonist used primarily for the treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and delay clinical worsening. It is an orally active, selective endothelin type A (ETA) receptor antagonist and is currently approved for use in several countries.
Pharmacokinetics
Pharmacokinetic parameters in healthy adult subjects following single oral administration.
References
Cárdenas, KPC, et al., & Pendela, M (2020). Bioequivalence and Tolerability of Ambrisentan: A Pharmacokinetic Study in Mexican Healthy Male Subjects. European journal of drug metabolism and pharmacokinetics 45(5) 611–618. DOI:10.1007/s13318-020-00627-3 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32472357
Hill, KD, et al., & Hornik, CP (2020). A Randomized, Controlled Pharmacokinetic and Pharmacodynamics Trial of Ambrisentan After Fontan Surgery. Pediatric critical care medicine : a journal of the Society of Critical Care Medicine and the World Federation of Pediatric Intensive and Critical Care Societies 21(9) e795–e803. DOI:10.1097/PCC.0000000000002410 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32639468
Yokoyama, Y, et al., & Itoh, K (2014). Simultaneous microdetermination of bosentan, ambrisentan, sildenafil, and tadalafil in plasma using liquid chromatography/tandem mass spectrometry for pediatric patients with pulmonary arterial hypertension. Journal of pharmaceutical and biomedical analysis 89 227–232. DOI:10.1016/j.jpba.2013.11.007 PUBMED:https://pubmed.ncbi.nlm.nih.gov/24309556
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)