modelTacrolimus

Diagram of Tacrolimus

Extends from Pharmacolibrary.Drugs.ATC.L.L04AD02.

Information

name:Tacrolimus
ATC code:L04AD02
route:oral
compartments:2
dosage:5mg
volume of distribution:1.61L
clearance:0.038L/h/kg
other parameters in model implementation

Tacrolimus is an immunosuppressant macrolide used primarily to prevent organ transplant rejection and to treat certain autoimmune diseases. It acts by inhibiting calcineurin, thus suppressing T-lymphocyte activation. It is approved and remains widely used in clinical practice, particularly for kidney, liver, and heart transplant recipients.

Pharmacokinetics

Pharmacokinetic model parameters reported for adult kidney transplant recipients following oral administration in the early post-transplant period, population containing both sexes.

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)