modelJ05AR10
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | LopinavirAndRitonavir | |
| ATC code: | J05AR10 | route: | oral |
| compartments: | 2 | |
| dosage: | 400 | mg |
| volume of distribution: | 23.7 | L |
| clearance: | 4.6 | L/h |
| other parameters in model implementation | ||
Lopinavir and ritonavir is a fixed-dose combination of antiretroviral drugs used in the treatment and prevention of HIV/AIDS. Lopinavir inhibits the HIV-1 protease, while ritonavir acts mainly as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A-mediated metabolism of lopinavir, thereby increasing lopinavir plasma concentrations. This combination is approved and is a common part of highly active antiretroviral therapy (HAART) regimens used today.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy adult subjects (both sexes) after oral administration of lopinavir/ritonavir 400 mg/100 mg twice daily in tablet formulation.
References
Zhang, C, et al., & Denti, P (2012). Population pharmacokinetics of lopinavir and ritonavir in combination with rifampicin-based antitubercular treatment in HIV-infected children. Antiviral therapy 17(1) 25–33. DOI:10.3851/IMP1915 PUBMED:https://pubmed.ncbi.nlm.nih.gov/22267466
Moltó, J, et al., & Valle, M (2008). Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults. Clinical pharmacokinetics 47(10) 681–692. DOI:10.2165/00003088-200847100-00005 PUBMED:https://pubmed.ncbi.nlm.nih.gov/18783298
Thakur, A, et al., & Chan, JCY (2020). Physiologically-Based Pharmacokinetic Modeling to Predict the Clinical Efficacy of the Coadministration of Lopinavir and Ritonavir against SARS-CoV-2. Clinical pharmacology and therapeutics 108(6) 1176–1184. DOI:10.1002/cpt.2014 PUBMED:https://pubmed.ncbi.nlm.nih.gov/32767755
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)