modelEsketamine
Extends from Pharmacolibrary.Drugs.ATC.N.N01AX14.
Information
| name: | Esketamine | |
| ATC code: | N01AX14 | route: | intravenous |
| compartments: | 2 | |
| dosage: | 0.25 | mg |
| volume of distribution: | 2.7 | L |
| clearance: | 14.6 | mL/min/kg |
| other parameters in model implementation | ||
Esketamine is the S-enantiomer of ketamine, a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist. It is used as an anesthetic agent and, more recently, as an antidepressant for treatment-resistant depression. Esketamine nasal spray is approved for use in adults with treatment-resistant depression in combination with another oral antidepressant.
Pharmacokinetics
Pharmacokinetic model parameters obtained from healthy adult subjects after single-dose intravenous administration.
References
Perez-Ruixo, C, et al., & Perez-Ruixo, JJ (2021). Population Pharmacokinetics of Esketamine Nasal Spray and its Metabolite Noresketamine in Healthy Subjects and Patients with Treatment-Resistant Depression. Clinical pharmacokinetics 60(4) 501–516. DOI:10.1007/s40262-020-00953-4 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33128208
Jonkman, K, et al., & Dahan, A (2017). Pharmacokinetics and Bioavailability of Inhaled Esketamine in Healthy Volunteers. Anesthesiology 127(4) 675–683. DOI:10.1097/ALN.0000000000001798 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28759464
Kamp, J, et al., & Olofsen, E (2020). Pharmacokinetics of ketamine and its major metabolites norketamine, hydroxynorketamine, and dehydronorketamine: a model-based analysis. British journal of anaesthesia 125(5) 750–761. DOI:10.1016/j.bja.2020.06.067 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32838982
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 |
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)