modelClofazimine
Extends from Pharmacolibrary.Drugs.ATC.J.J04BA01.
Information
| name: | Clofazimine | |
| ATC code: | J04BA01 | route: | oral |
| compartments: | 2 | |
| dosage: | 100 | mg |
| volume of distribution: | 1050 | L |
| clearance: | 0.48 | L/h |
| other parameters in model implementation | ||
Clofazimine is a riminophenazine antibiotic primarily used for the treatment of leprosy (Hansen's disease), especially for multibacillary forms and as part of multidrug therapy. It is also occasionally used off-label for some mycobacterial infections. Clofazimine is approved and used in several countries but is not approved for all mycobacterial infections. Its use is limited due to side effects such as skin discoloration and gastrointestinal symptoms.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy male volunteers, following oral administration of clofazimine at steady state.
References
Zhang, CX, et al., & Arnold, SLM (2022). Pharmacokinetics and Pharmacodynamics of Clofazimine for Treatment of Cryptosporidiosis. Antimicrobial agents and chemotherapy 66(1) e0156021–None. DOI:10.1128/AAC.01560-21 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34748385
Stadler, JAM, et al., & Wasserman, S (2023). Clofazimine for the treatment of tuberculosis. Frontiers in pharmacology 14 1100488–None. DOI:10.3389/fphar.2023.1100488 PUBMED:https://pubmed.ncbi.nlm.nih.gov/36817137
Zhang, CX, et al., & Arnold, SLM (2024). Clofazimine pharmacokinetics in HIV-infected adults with diarrhea: Implications of diarrheal disease on absorption of orally administered therapeutics. CPT: pharmacometrics & systems pharmacology 13(3) 410–423. DOI:10.1002/psp4.13092 PUBMED:https://pubmed.ncbi.nlm.nih.gov/38164114
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)