modelSaquinavir

Diagram of Saquinavir

Extends from Pharmacolibrary.Drugs.ATC.J.J05AE01.

Information

name:Saquinavir
ATC code:J05AE01
route:oral
compartments:2
dosage:600mg
volume of distribution:161L
clearance:31.8L/h
other parameters in model implementation

Saquinavir is a protease inhibitor used as an antiretroviral agent in the treatment of HIV-1 infection. It was one of the first protease inhibitors approved for use but is now less commonly used due to newer agents with improved safety and efficacy. It is used in combination antiretroviral therapy for managing HIV/AIDS.

Pharmacokinetics

Pharmacokinetic parameters reported for HIV-infected adult patients, both male and female, under steady-state conditions receiving oral saquinavir-hardshell capsules 600 mg three times daily.

References

  1. Dickinson, L, et al., & Aarons, LJ (2008). Population pharmacokinetics of ritonavir-boosted saquinavir regimens in HIV-infected individuals. The Journal of antimicrobial chemotherapy 62(6) 1344–1355. DOI:10.1093/jac/dkn399 PUBMED:https://pubmed.ncbi.nlm.nih.gov/18824460

  2. Acosta, EP, et al., & Mofenson, L (2001). Pharmacokinetics of saquinavir-SGC in HIV-infected pregnant women. HIV clinical trials 2(6) 460–465. DOI:10.1310/PUY3-5JWL-FX2B-98VU PUBMED:https://pubmed.ncbi.nlm.nih.gov/11742433

  3. Dailly, E, et al., & Jolliet, P (2005). No significant influence of saquinavir hard-gel capsule administration on pharmacokinetics of lopinavir in combination with ritonavir: a population approach. Therapeutic drug monitoring 27(6) 782–784. DOI:10.1097/01.ftd.0000177663.89103.58 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16306855

Parameters

TypeNameDefaultDescription
Modelica.Units.SI.Massweight (from PK_1C)75patient weight (kg)
Modelica.Units.SI.SpecificVolumeVdPerKg (from PK_1C)0.9Volume of distribution (L/kg)
Modelica.Units.SI.MassFractionF (from PK_1C)0.8bioavailiability (0-1)
Pharmacolibrary.Types.ClearanceCl (from PK_1C)20clearance
Modelica.Units.SI.TimeadminTime (from PK_1C)60first administration time (s)
Modelica.Units.SI.TimeadminDuration (from PK_1C)600administration duration (s)
Modelica.Units.SI.TimeadminPeriod (from PK_1C)8*60*60period of administration (default 8 hours)(s)
Pharmacolibrary.Types.MassadminMass (from PK_1C)1000administration mass (mg)
IntegeradminCount (from PK_1C)8number of dose administered (1)
Pharmacolibrary.Types.VolumeVd (from PK_1C)VdPerKg*weightVolume of distribution (m3)
Pharmacolibrary.Types.MassConcentrationCmin (from PK_1C)0.004minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCmax (from PK_1C)0.008minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCtox_peak (from PK_1C)0.012toxicity peak level
Pharmacolibrary.Types.MassConcentrationCtox_trough (from PK_1C)0.006toxicity trough level
Pharmacolibrary.Types.VolumeVdp (from PK_2C)VdpPerKg*weightVolume of distribution (m3)
Modelica.Units.SI.SpecificVolumeVdpPerKg (from PK_2C)0.9Volume of distribution peripheral(l/kg)
Pharmacolibrary.Types.Clearancek12 (from PK_2C)1intercompartmental C-P clearance
Pharmacolibrary.Types.Clearancek21 (from PK_2C)1intercompartmental P-C clearance
Pharmacolibrary.Types.TransferRateka (from PK_2C_enteral)0.016666666666666666first order absorption rate
Modelica.Units.SI.TimeTlag (from PK_2C_enteral)600delay between oral administration and absorption (default 10min)

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)
Interfaces.ConcentrationPort_bperipheralCPort (from PK_2C)
Pharmacolibrary.Types.ConcentrationOutputC_peripheral1 (from PK_2C)

Components

TypeNameDefaultDescription
Pharmacokinetic.NoPerfusedTissueCompartmentcentral (from PK_1C)
Pharmacokinetic.ClearanceDrivenEliminationelim (from PK_1C)
Sources.PeriodicDoseperiodicDose (from PK_1C)
Modelica.Units.SI.Timet1_2 (from PK_1C)elimination half-life
Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSymtransfer (from PK_2C)
Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartmentperipheral (from PK_2C)

Revisions

  • 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)