modelA04AD12
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | Aprepitant | |
| ATC code: | A04AD12 | route: | oral |
| compartments: | 2 | |
| dosage: | 125 | mg |
| volume of distribution: | 82 | L |
| clearance: | 62.3 | L/h |
| other parameters in model implementation | ||
Aprepitant is a selective neurokinin-1 (NK1) receptor antagonist used for the prevention of acute and delayed nausea and vomiting associated with chemotherapy and for the prevention of postoperative nausea and vomiting. It is an approved, orally administered antiemetic drug.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy adult subjects after oral administration.
References
Nakade, S, et al., & Miyata, Y (2008). Population pharmacokinetics of aprepitant and dexamethasone in the prevention of chemotherapy-induced nausea and vomiting. Cancer chemotherapy and pharmacology 63(1) 75–83. DOI:10.1007/s00280-008-0713-y PUBMED:https://pubmed.ncbi.nlm.nih.gov/18317761
Nijstad, AL, et al., & Huitema, ADR (2023). A simple extemporaneous oral suspension of aprepitant yields sufficient pharmacokinetic exposure in children. Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners 29(4) 899–904. DOI:10.1177/10781552221089243 PUBMED:https://pubmed.ncbi.nlm.nih.gov/35377726
Yang, MJ, et al., & Li, XN (2020). Comparison of Pharmacokinetics of Aprepitant in Healthy Chinese and Caucasian Subjects. Drug design, development and therapy 14 1219–1226. DOI:10.2147/DDDT.S243924 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32273684
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.Volume | Vdp (from PK_2C) | VdpPerKg*weight | Volume of distribution (m3) |
| Modelica.Units.SI.SpecificVolume | VdpPerKg (from PK_2C) | 0.9 | Volume of distribution peripheral(l/kg) |
| Pharmacolibrary.Types.Clearance | k12 (from PK_2C) | 1 | intercompartmental C-P clearance |
| Pharmacolibrary.Types.Clearance | k21 (from PK_2C) | 1 | intercompartmental P-C clearance |
| Pharmacolibrary.Types.TransferRate | ka (from PK_2C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_2C_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) | ||
| Interfaces.ConcentrationPort_b | peripheralCPort (from PK_2C) | ||
| Pharmacolibrary.Types.ConcentrationOutput | C_peripheral1 (from PK_2C) |
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 | |
| Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSym | transfer (from PK_2C) | ||
| Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartment | peripheral (from PK_2C) |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)