modelR06AX12
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | Terfenadine | |
| ATC code: | R06AX12 | route: | oral |
| compartments: | 2 | |
| dosage: | 60 | mg |
| volume of distribution: | 11 | L |
| clearance: | 960 | ml/min |
| other parameters in model implementation | ||
Terfenadine is a non-sedating antihistamine that was formerly used to treat allergic rhinitis and other allergy symptoms. It acts as an H1 receptor antagonist. Due to its association with QT prolongation and risk of serious arrhythmias (notably Torsades de Pointes), terfenadine has been withdrawn or discontinued in many countries and is no longer approved for clinical use.
Pharmacokinetics
Pharmacokinetic parameters in healthy adult subjects following oral administration.
References
Lalonde, RL, et al., & Gaudreault, J (1996). Population pharmacokinetics of terfenadine. Pharmaceutical research 13(6) 832–838. DOI:10.1023/a:1016036624935 PUBMED:https://pubmed.ncbi.nlm.nih.gov/8792418
Paton, DM, & Webster, DR (1985). Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clinical pharmacokinetics 10(6) 477–497. DOI:10.2165/00003088-198510060-00002 PUBMED:https://pubmed.ncbi.nlm.nih.gov/2866055
Wilkinson, GR (1996). Cytochrome P4503A (CYP3A) metabolism: prediction of in vivo activity in humans. Journal of pharmacokinetics and biopharmaceutics 24(5) 475–490. DOI:10.1007/BF02353475 PUBMED:https://pubmed.ncbi.nlm.nih.gov/9131486
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)