modelTacrolimus

Diagram of Tacrolimus

Extends from Pharmacolibrary.Drugs.ATC.D.D11AH01.

Information

name:Tacrolimus
ATC code:D11AH01
route:oral
compartments:2
dosage:5mg
volume of distribution:1.52L
clearance:0.038L/h/kg
other parameters in model implementation

Tacrolimus is a calcineurin inhibitor with potent immunosuppressive properties. It is primarily used to prevent organ transplant rejection and to treat autoimmune diseases such as atopic dermatitis. It is approved for clinical use worldwide.

Pharmacokinetics

Pharmacokinetic model for adult healthy volunteers and transplant recipients; both sexes. Oral administration; data primarily referenced from studies on liver and kidney transplant patients.

References

  1. Martial, LC, et al., & Moes, DJAR (2021). Population pharmacokinetics and genetics of oral meltdose tacrolimus (Envarsus) in stable adult liver transplant recipients. British journal of clinical pharmacology 87(11) 4262–4272. DOI:10.1111/bcp.14842 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33786892

  2. Teng, F, et al., & Wei, H (2022). Population pharmacokinetics of tacrolimus in Chinese adult liver transplant patients. Biopharmaceutics & drug disposition 43(2) 76–85. DOI:10.1002/bdd.2311 PUBMED:https://pubmed.ncbi.nlm.nih.gov/35220592

  3. Kamp, J, et al., & Moes, DJAR (2023). Meltdose Tacrolimus Population Pharmacokinetics and Limited Sampling Strategy Evaluation in Elderly Kidney Transplant Recipients. Pharmaceutics 16(1) –. DOI:10.3390/pharmaceutics16010017 PUBMED:https://pubmed.ncbi.nlm.nih.gov/38276495

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)