modelH02CA03
Extends from Pharmacokinetic.Models.PK_1C_enteral.
Information
| name: | Ketoconazole | |
| ATC code: | H02CA03 | route: | oral |
| compartments: | 1 | |
| dosage: | 200 | mg |
| volume of distribution: | 11 | L |
| clearance: | 0.044 | L/min |
| other parameters in model implementation | ||
Ketoconazole is a synthetic imidazole antifungal agent primarily used for the treatment of fungal infections. It inhibits fungal steroid synthesis, particularly ergosterol, by blocking the cytochrome P450-dependent enzyme lanosterol 14-α-demethylase. Due to its risk of hepatotoxicity and adrenal insufficiency, oral ketoconazole is largely discontinued or restricted and is now rarely used systemically but still approved in some countries for severe systemic mycoses when other antifungals are unavailable.
Pharmacokinetics
Pharmacokinetic parameters in healthy adult volunteers after single oral dose.
References
David, OJ, et al., & Schmouder, RL (2012). Clinical pharmacokinetics of fingolimod. Clinical pharmacokinetics 51(1) 15–28. DOI:10.2165/11596550-000000000-00000 PUBMED:https://pubmed.ncbi.nlm.nih.gov/22149256
Harris, RZ, et al., & Padhi, D (2007). Pharmacokinetics of cinacalcet hydrochloride when administered with ketoconazole. Clinical pharmacokinetics 46(6) 495–501. DOI:10.2165/00003088-200746060-00003 PUBMED:https://pubmed.ncbi.nlm.nih.gov/17518508
Noh, YH, et al., & Bae, KS (2012). Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers. Clinical therapeutics 34(5) 1182–1194. DOI:10.1016/j.clinthera.2012.04.001 PUBMED:https://pubmed.ncbi.nlm.nih.gov/22534255
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)