modelCiclosporin

Diagram of Ciclosporin

Extends from Pharmacolibrary.Drugs.ATC.L.L04AD01.

Information

name:Ciclosporin
ATC code:L04AD01
route:oral
compartments:2
dosage:300mg
volume of distribution:3.96L
clearance:0.37L/h/kg
other parameters in model implementation

Ciclosporin (also known as cyclosporine) is a calcineurin inhibitor immunosuppressant primarily used to prevent organ transplant rejection and to treat autoimmune diseases such as rheumatoid arthritis and psoriasis. It is approved for use in many countries and remains an important drug in transplant medicine.

Pharmacokinetics

Pharmacokinetic parameters in healthy adult volunteers following oral administration; parameters are population means reported in published literature.

References

  1. Fruit, D, et al., & Prémaud, A (2013). Ciclosporin population pharmacokinetics and Bayesian estimation in thoracic transplant recipients. Clinical pharmacokinetics 52(4) 277–288. DOI:10.1007/s40262-013-0037-x PUBMED:https://pubmed.ncbi.nlm.nih.gov/23400901

  2. Ling, J, et al., & Chen, R (2022). Population pharmacokinetics of ciclosporin in allogeneic hematopoietic stem cell transplant recipients: C-reactive protein as a novel covariate for clearance. Journal of clinical pharmacy and therapeutics 47(4) 483–492. DOI:10.1111/jcpt.13569 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34779003

  3. Wilhelm, AJ, et al., & Swart, EL (2012). Population pharmacokinetics of ciclosporin in haematopoietic allogeneic stem cell transplantation with emphasis on limited sampling strategy. British journal of clinical pharmacology 73(4) 553–563. DOI:10.1111/j.1365-2125.2011.04116.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/21988410

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)