modelEflornithine

Diagram of Eflornithine

Extends from Pharmacolibrary.Drugs.ATC.L.L01XX79.

Information

name:Eflornithine
ATC code:L01XX79
route:intravenous
compartments:1
dosage:400mg
volume of distribution:0.25L
clearance:350ml/min
other parameters in model implementation

Eflornithine is an irreversible inhibitor of ornithine decarboxylase, used in the treatment of African trypanosomiasis (sleeping sickness) due to Trypanosoma brucei gambiense. It was also formerly used topically for the reduction of unwanted facial hair. Eflornithine is generally administered intravenously for the treatment of sleeping sickness and is not widely approved or used for other major indications today.

Pharmacokinetics

Pharmacokinetic parameters estimated from published data for adult patients with late-stage African trypanosomiasis treated with intravenous eflornithine.

References

  1. Amilon, C, et al., & Jansson-Löfmark, R (2022). Population Pharmacodynamic Modeling of Eflornithine-Based Treatments Against Late-Stage Gambiense Human African Trypanosomiasis and Efficacy Predictions of L-eflornithine-Based Therapy. The AAPS journal 24(3) 48–None. DOI:10.1208/s12248-022-00693-2 PUBMED:https://pubmed.ncbi.nlm.nih.gov/35338410

  2. Johansson, CC, et al., & Jansson-Löfmark, R (2013). Population pharmacokinetic modeling and deconvolution of enantioselective absorption of eflornithine in the rat. Journal of pharmacokinetics and pharmacodynamics 40(1) 117–128. DOI:10.1007/s10928-012-9293-x PUBMED:https://pubmed.ncbi.nlm.nih.gov/23307171

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

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)

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

Revisions

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