modelDarifenacin

Diagram of Darifenacin

Extends from Pharmacolibrary.Drugs.ATC.G.G04BD10.

Information

name:Darifenacin
ATC code:G04BD10
route:oral
compartments:2
dosage:15mg
volume of distribution:163L
clearance:40L/h
other parameters in model implementation

Darifenacin is a selective muscarinic M3 receptor antagonist used to treat symptoms of overactive bladder, such as urinary incontinence, urgency, and frequency. It is approved for clinical use and is commonly administered orally.

Pharmacokinetics

Pharmacokinetics in healthy adult volunteers after repeated oral administration.

References

  1. Kerbusch, T, et al., & Karlsson, MO (2003). Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability. British journal of clinical pharmacology 56(6) 639–652. DOI:10.1046/j.1365-2125.2003.01967.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/14616424

  2. McFerren, SC, & Gomelsky, A (2015). Treatment of Overactive Bladder in the Elderly Female: The Case for Trospium, Oxybutynin, Fesoterodine and Darifenacin. Drugs & aging 32(10) 809–819. DOI:10.1007/s40266-015-0301-x PUBMED:https://pubmed.ncbi.nlm.nih.gov/26391900

  3. Kerbusch, T, et al., & Karlsson, MO (2004). Assessment of the relative in vivo potency of the hydroxylated metabolite of darifenacin in its ability to decrease salivary flow using pooled population pharmacokinetic-pharmacodynamic data. British journal of clinical pharmacology 57(2) 170–180. DOI:10.1046/j.1365-2125.2003.01988.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/14748816

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)